Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0TKVCB
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| ADC Name |
Loncastuximab tesirine
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| Brand Name |
Zynlonta
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| Synonyms |
loncastuximab tesirine; ADCT-402; RB4v1.2-SG-3249; Zynlonta; loncastuximab tesirine-lpyl; MT-2111; Lonca
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| Organization |
ADC Therapeutics (Originator);Tanabe Pharma Corporation;Swedish Orphan Biovitrum;Spirogen (Top20 MNC);Overland Pharmaceuticals
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| Drug Status |
Approved in 2021
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| Drug-to-Antibody Ratio |
2.3
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| Structure |
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| Antibody Name |
Loncastuximab
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Antibody Info | ||||
| Antigen Name |
B-lymphocyte antigen CD19 (CD19)
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Antigen Info | ||||
| Payload Name |
SG3199 (SC-DR002)
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Payload Info | ||||
| Therapeutic Target |
Human deoxyribonucleic acid (hDNA)
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Target Info | ||||
| Linker Name |
Mal-PEG8-Val-Ala-PABC
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Linker Info | ||||
| Conjugate Type |
Random Cysteines
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| Combination Type |
tesirine
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| Absorption |
For loncastuximab tesirine, mean Cmax=2995 (ug/L) during cycle 1, mean Cmax=3155 (ug/L) during cycle 2; AUC=15,245-22,823 (day x ug/L).
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| Distribution |
The monoclonal antibody portion of loncastuximab tesirine-lpyl is catabolized into small peptides. In vitro studies show that the small molecule cytotoxin portion, SG3199, is metabolized by CYP3A4/5. The half-life of loncastuximab tesirine-lpyl was 7.06-12.5 days at steady-state.
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| Metabolism |
The monoclonal antibody portion of loncastuximab tesirine-lpyl is catabolized into small peptides. In vitro studies show that the small molecule cytotoxin portion, SG3199, is metabolized by CYP3A4/5. The half-life of loncastuximab tesirine-lpyl was 7.06-12.5 days at steady-state.
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| Toxicity |
The main excretion pathways of SG3199 have not been formally studied in humans. SG3199 is thought to be minimally excreted by the kidneys. The mean clearance of loncastuximab tesirine-lpyl were 0.499 L/day (after a single dose) and 0.275 L/day (at steady-state).
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| Special Approval(s) |
Priority review (FDA); Accelerated approval (FDA); Orphan drug (FDA); Orphan drug (EMA)
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The indication landscape of This ADC(2027 Update)
The clinical trial pipeline of This ADC(2027 Update)
| Indication | Phase 1 | Phase 1/2 | Phase 2 | Phase 2/3 | Phase 3 | New Drug Application | Approved | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Acute lymphoblastic leukemia |
1 Trials
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| Chronic lymphocytic leukemia |
1 Trials
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| Diffuse large b-cell lymphoma |
2 Trials
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1 Trials
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6 Trials
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| Follicular lymphoma |
1 Trials
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2 Trials
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| Mantle cell lymphoma |
1 Trials
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1 Trials
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| Unspecific non-hodgkin lymphoma |
2 Trials
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5 Trials
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ADC-specific functional property(2027 Update)
Binding Affinity
| Dissocation Constant (Kd) | Binding Target | Description | Reference |
|---|---|---|---|
| Undisclosed |
CD19
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CD19-expressing Ramos cells exposed to ADCT-402 (1 hour at 4°C) showed prominent cell surface binding
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[1]
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Bystander Killing Effect
| Bystander Killing Effect | Description | Reference |
|---|---|---|
| yes |
Ramos cells were treated with ADCT-402 for 1, 2, or 3 days, and the media was transferred onto CD192 Karpas-299 cells for 96 hours. The ADCT-402 conditioned medium induced a bystander effect after 1 day of pretreatment, as shown by a decrease in survival percentage in Karpas-299 cells compared to nonconditioned medium (100% to 86). This effect was stronger after 2 or 3 days of pretreatment, with a further decrease in survival percentage (80% and 65%, P =0.001). Conversely, conditioned medium from ADCT-402-treated CD192 NCI-N87 cells did not induce a bystander effect on Karpas-299 cells, regardless of preincubation time.
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[1]
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General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Maximum Observed Concentration (Cmax) | 1776 | ng/mL |
After loncastuximab tesirine treatment with the recommended dose regimen, the Cmax are 2911 ng/mL; the Cmax at steady state are 1776 ng/mL.
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[1], [2] |
| Area Under the Concentration-Time Curve (AUC) | 16882 | ng*day/mL |
After loncastuximab tesirine treatment with the recommended dose regimen, the AUC in cycle 2 are 21,665 ng·day/mL; the AUC at steady state are 16,882 ng·day/mL
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[1], [2] |
| Maximum Observed Concentration (Cmax) | 2841 | ng/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 1,
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[3] |
| Maximum Observed Concentration (Cmax) | 3258 | ng/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 2,
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[3] |
| Area Under the Concentration-Time Curve (AUC) | 10329 | ng*day/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 1,
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[3] |
| Area Under the Concentration-Time Curve (AUC) | 16547 | ng*day/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 2,
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[3] |
| Maximum Observed Concentration (Cmax) | 2430 | ng/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 1.
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[3] |
| Maximum Observed Concentration (Cmax) | 2734 | ng/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 2.
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[3] |
| Maximum Observed Concentration (Cmax) | 1694 | ng/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 3.
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[3] |
| Area Under the Concentration-Time Curve (AUC) | 15850 | ng*day/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 1.
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[3] |
| Area Under the Concentration-Time Curve (AUC) | 23913 | ng*day/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 2.
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[3] |
| Maximum Observed Concentration (Cmax) | 659 | ng/mL |
Loncastuximab tesirine 60 ug/kg once Q3W and ibrutinib 560 mg/day, Administered to patients with R/R B-cell malignancies in cycle 1.
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[3] |
| Maximum Observed Concentration (Cmax) | 761 | ng/mL |
Loncastuximab tesirine 60 ug/kg once Q3W and ibrutinib 560 mg/day, Administered to patients with R/R B-cell malignancies in cycle 2.
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[3] |
| Maximum Observed Concentration (Cmax) | 2995 | ug/L |
PK parameters were available to be calculated from 85 patients, cycle 1
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[4] |
| Area Under the Concentration-Time Curve (AUC) | 15245 | day*ug/L |
PK parameters were available to be calculated from 85 patients, cycle 1
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[4] |
| Maximum Observed Concentration (Cmax) | 3155 | ug/L |
PK parameters were available to be calculated from 85 patients, cycle 2
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[4] |
| Area Under the Concentration-Time Curve (AUC) | 22823 | day*ug/L |
PK parameters were available to be calculated from 85 patients, cycle 2
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[4] |
| Maximum Observed Concentration (Cmax) | 250 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 15 ug/kg
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[5] |
| Area Under the Concentration-Time Curve (AUC) | 638 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 15 ug/kg
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[5] |
| Area Under the Concentration-Time Curve (AUC) | 407 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 15 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 384 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 30 ug/kg
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[5] |
| Area Under the Concentration-Time Curve (AUC) | 2276 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 30 ug/kg
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[5] |
| Area Under the Concentration-Time Curve (AUC) | 1945 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 30 ug/kg
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[5] |
| Maximum Observed Concentration (Cmax) | 525 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 60 ug/kg
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[5] |
| Area Under the Concentration-Time Curve (AUC) | 1006 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 4520 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 60 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 705 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1349 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2430 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 90 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 2218 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 120 ug/kg
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[5] |
| Area Under the Concentration-Time Curve (AUC) | 10154 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 7539 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 120 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 2841 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10329 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 7361 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 150 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 3546 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 24720 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 14660 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 200 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 329 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 15 ug/kg
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[5] |
| Area Under the Concentration-Time Curve (AUC) | 936 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1030 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 15 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 1145 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2812 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3264 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 30 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 486 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 602 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10545 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 60 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 1183 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3183 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3227 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 90 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 2368 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 13522 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 15223 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 120 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 3258 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 16547 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 18049 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 150 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 4160 | ng/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 44880 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 38188 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 200 ug/kg
|
[5] |
| Maximum Observed Concentration (Cmax) | 178 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 15 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 337 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 15 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 2150 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 15 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 1596 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 15 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 258 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 30 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 127 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 30 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 339 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 30 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 735 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 30 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 449 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 60 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 43 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 60 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 661 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 60 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 50.6 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 60 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 1058 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 90 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 671 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 90 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 1813 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 90 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 3370 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 90 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 1291 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 120 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 3907 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 120 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 1515 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 120 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 8744 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 120 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 2145 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 150 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 688 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 150 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 3033 | ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 150 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 7553 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 150 ug/kg
|
[7] |
| Maximum Observed Concentration (Cmax) | 2268 | ng/mL |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 15916 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2,area under the concentration-time curve from time zero to last quantifiable concentration
Click to Show/Hide
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 16788 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2, area under the concentration-time curve from zero to end of dosing interval tau
|
[8] |
| Maximum Observed Concentration (Cmax) | 2746 | ng/mL |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 24268 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2,area under the concentration-time curve from time zero to last quantifiable concentration
Click to Show/Hide
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 23780 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2, area under the concentration-time curve from zero to end of dosing interval tau
|
[8] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 16882 | ng*day/mL |
After loncastuximab tesirine treatment with the recommended dose regimen, the AUC in cycle 2 are 21,665 ng·day/mL; the AUC at steady state are 16,882 ng·day/mL
|
[1], [2] |
| Volume of Distribution (Vd) | 7.11 | L |
The mean volume of distribution is 7.11 L.
|
[1], [2] |
| Area Under the Concentration-Time Curve (AUC) | 10329 | ng*day/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 1,
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 16547 | ng*day/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 2,
|
[3] |
| Volume of Distribution (Vd) | 6.37 | L |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 1,
|
[3] |
| Volume of Distribution (Vd) | 6.62 | L |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 2,
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 15850 | ng*day/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 1.
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 23913 | ng*day/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 2.
|
[3] |
| Volume of Distribution (Vd) | 4.24 | L |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cyclesAdministered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 1.
|
[3] |
| Volume of Distribution (Vd) | 6.4 | L |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 2.
|
[3] |
| Volume of Distribution (Vd) | 5.52 | L |
Loncastuximab tesirine 60 ug/kg once Q3W and ibrutinib 560 mg/day, Administered to patients with R/R B-cell malignancies in cycle 1.
|
[3] |
| Volume of Distribution (Vd) | 7.85 | L |
Loncastuximab tesirine 60 ug/kg once Q3W and ibrutinib 560 mg/day, Administered to patients with R/R B-cell malignancies in cycle 2.
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 15245 | day*ug/L |
PK parameters were available to be calculated from 85 patients, cycle 1
|
[4] |
| Volume of Distribution (Vd) | 7.19 | L |
PK parameters were available to be calculated from 85 patients, cycle 1
|
[4] |
| Area Under the Concentration-Time Curve (AUC) | 22823 | day*ug/L |
PK parameters were available to be calculated from 85 patients, cycle 2
|
[4] |
| Volume of Distribution (Vd) | 8.34 | L |
PK parameters were available to be calculated from 85 patients, cycle 2
|
[4] |
| Area Under the Concentration-Time Curve (AUC) | 638 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 407 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 15 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 4.43 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2276 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1945 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 30 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 9.76 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1006 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 4520 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 60 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 4.95 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1349 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2430 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 90 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 9.5 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10154 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 7539 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 120 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 5.66 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10329 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 7361 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 150 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 6.37 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 24720 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 14660 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 200 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 8.71 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 936 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1030 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 15 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 3.62 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2812 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3264 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 30 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 8.14 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 602 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10545 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 60 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 8.28 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3183 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3227 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 90 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 7.55 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 13522 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 15223 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 120 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 6.11 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 16547 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 18049 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 150 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 6.62 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 44880 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 38188 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 200 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 8.62 | L |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 200 ug/kg
|
[5] |
| Volume of Distribution (Vd) | 3.86 | L |
Efficacy and Safety Exposure-Response Analysis of Loncastuximab Tesirine in Patients with B cell non-Hodgkin Lymphoma, volume of distribution in the central compartment
|
[6] |
| Volume of Distribution (Vd) | 3.53 | L |
Efficacy and Safety Exposure-Response Analysis of Loncastuximab Tesirine in Patients with B cell non-Hodgkin Lymphoma, volume of distribution in the peripheral compartment
|
[6] |
| Area Under the Concentration-Time Curve (AUC) | 337 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 15 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 1596 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 15 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 127 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 30 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 735 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 30 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 43 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 60 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 50.6 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 60 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 671 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 90 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 3370 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 90 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 3907 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 120 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 8744 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 120 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 688 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 150 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 7553 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 150 ug/kg
|
[7] |
| Volume of Distribution (Vd) | 10.5 | L |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle 1, 90 ug/kg
|
[7] |
| Volume of Distribution (Vd) | 5.61 | L |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle2, 90 ug/kg
|
[7] |
| Volume of Distribution (Vd) | 6.89 | L |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle 1, 120 ug/kg
|
[7] |
| Volume of Distribution (Vd) | 8.33 | L |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle2, 120 ug/kg
|
[7] |
| Volume of Distribution (Vd) | 34.2 | L |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle 1, 150 ug/kg
|
[7] |
| Volume of Distribution (Vd) | 9.45 | L |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle2, 150 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 15916 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2,area under the concentration-time curve from time zero to last quantifiable concentration
Click to Show/Hide
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 16788 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2, area under the concentration-time curve from zero to end of dosing interval tau
|
[8] |
| Volume of Distribution (Vd) | 3.83 | L |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 24268 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2,area under the concentration-time curve from time zero to last quantifiable concentration
Click to Show/Hide
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 23780 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2, area under the concentration-time curve from zero to end of dosing interval tau
|
[8] |
| Volume of Distribution (Vd) | 5.46 | L |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2
|
[8] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 16882 | ng*day/mL |
After loncastuximab tesirine treatment with the recommended dose regimen, the AUC in cycle 2 are 21,665 ng·day/mL; the AUC at steady state are 16,882 ng·day/mL
|
[1], [2] |
| Area Under the Concentration-Time Curve (AUC) | 10329 | ng*day/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 1,
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 16547 | ng*day/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 2,
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 15850 | ng*day/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 1.
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 23913 | ng*day/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 2.
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 15245 | day*ug/L |
PK parameters were available to be calculated from 85 patients, cycle 1
|
[4] |
| Area Under the Concentration-Time Curve (AUC) | 22823 | day*ug/L |
PK parameters were available to be calculated from 85 patients, cycle 2
|
[4] |
| Area Under the Concentration-Time Curve (AUC) | 638 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 407 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2276 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1945 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1006 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 4520 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1349 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2430 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10154 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 7539 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10329 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 7361 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 24720 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 14660 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 936 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1030 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2812 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3264 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 602 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10545 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3183 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3227 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 13522 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 15223 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 16547 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 18049 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 44880 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 38188 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 337 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 15 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 1596 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 15 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 127 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 30 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 735 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 30 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 43 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 60 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 50.6 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 60 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 671 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 90 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 3370 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 90 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 3907 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 120 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 8744 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 120 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 688 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 150 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 7553 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 150 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 15916 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2,area under the concentration-time curve from time zero to last quantifiable concentration
Click to Show/Hide
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 16788 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2, area under the concentration-time curve from zero to end of dosing interval tau
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 24268 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2,area under the concentration-time curve from time zero to last quantifiable concentration
Click to Show/Hide
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 23780 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2, area under the concentration-time curve from zero to end of dosing interval tau
|
[8] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Elimination Half-Life (t1/2) | 7.063-12.5 | days |
The half-life of loncastuximab tesirine-lpyl was 7.06-12.5 days at steady-state.
|
[1], [2] |
| Clearance (CL) | 0.53-0.64 | L/day |
In pharmacokinetic studies, the mean clearance of loncastuximab tesirine-lpyl decreased with time from 0.499 L/day after a single dose to 0.275 L/day at steady-state. One pharmacokinetic study measured a clearance ranging from 0.5-0.64 L/day.
Click to Show/Hide
|
[1], [2] |
| Area Under the Concentration-Time Curve (AUC) | 16882 | ng*day/mL |
After loncastuximab tesirine treatment with the recommended dose regimen, the AUC in cycle 2 are 21,665 ng·day/mL; the AUC at steady state are 16,882 ng·day/mL
|
[1], [2] |
| Clearance (CL) | 1.36 | L/day |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 1,
|
[3] |
| Clearance (CL) | 0.516 | L/day |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 2,
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 10329 | ng*day/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 1,
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 16547 | ng*day/mL |
150 Ug/kg Q3W,Dose-related exposure. Administered to patients with relapsed/refractory (R/R) B-cell malignancies. In Cycle 2,
|
[3] |
| Clearance (CL) | 0.458 | L/day |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 1.
|
[3] |
| Clearance (CL) | 0.311 | L/day |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 2.
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 15850 | ng*day/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 1.
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 23913 | ng*day/mL |
150 Ug/kg Q3W for two cycles, 75 ug/kg Q3W for subsequent cycles,Administered to patients with R/R B-cell malignancies. Dose reduced from 150 ug/kg to 75 ug/kg in cycle 2.
|
[3] |
| Clearance (CL) | 0.893 | L/day |
Loncastuximab tesirine 60 ug/kg once Q3W and ibrutinib 560 mg/day, Administered to patients with R/R B-cell malignancies in cycle 1.
|
[3] |
| Clearance (CL) | 0.705 | L/day |
Loncastuximab tesirine 60 ug/kg once Q3W and ibrutinib 560 mg/day, Administered to patients with R/R B-cell malignancies in cycle 2.
|
[3] |
| Area Under the Concentration-Time Curve (AUC) | 15245 | day*ug/L |
PK parameters were available to be calculated from 85 patients, cycle 1
|
[4] |
| Elimination Half-Life (t1/2) | 7.15 | day |
PK parameters were available to be calculated from 85 patients, cycle 1
|
[4] |
| Clearance (CL) | 0.75 | L/day |
PK parameters were available to be calculated from 85 patients, cycle 1
|
[4] |
| Area Under the Concentration-Time Curve (AUC) | 22823 | day*ug/L |
PK parameters were available to be calculated from 85 patients, cycle 2
|
[4] |
| Elimination Half-Life (t1/2) | 12.5 | day |
PK parameters were available to be calculated from 85 patients, cycle 2
|
[4] |
| Clearance (CL) | 0.5 | L/day |
PK parameters were available to be calculated from 85 patients, cycle 2
|
[4] |
| Area Under the Concentration-Time Curve (AUC) | 638 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 407 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 15 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 1.45 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 15 ug/kg
|
[5] |
| Clearance (CL) | 2.36 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2276 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1945 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 30 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 6.75 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 30 ug/kg
|
[5] |
| Clearance (CL) | 1.07 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1006 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 4520 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 60 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 5.97 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 60 ug/kg
|
[5] |
| Clearance (CL) | 0.621 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1349 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2430 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 90 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 2.54 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 90 ug/kg
|
[5] |
| Clearance (CL) | 3.33 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10154 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 7539 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 120 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 4.67 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 120 ug/kg
|
[5] |
| Clearance (CL) | 1.05 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10329 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 7361 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 150 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 4.46 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 150 ug/kg
|
[5] |
| Clearance (CL) | 1.36 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 24720 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUClast, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 14660 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, AUCinf, 200 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 9.02 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 200 ug/kg
|
[5] |
| Clearance (CL) | 0.998 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 1 for patients with B-NHL receiving a Q3W regimen, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 936 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 1030 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 15 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 3.15 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 15 ug/kg
|
[5] |
| Clearance (CL) | 0.897 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 15 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 2812 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3264 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 30 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 10.4 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 30 ug/kg
|
[5] |
| Clearance (CL) | 0.584 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 30 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 602 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 10545 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 60 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 15.4 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 60 ug/kg
|
[5] |
| Clearance (CL) | 0.389 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 60 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3183 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 3227 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 90 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 7.97 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 90 ug/kg
|
[5] |
| Clearance (CL) | 1.96 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 90 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 13522 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 15223 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 120 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 10.3 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 120 ug/kg
|
[5] |
| Clearance (CL) | 0.529 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 120 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 16547 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 18049 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 150 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 9.77 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 150 ug/kg
|
[5] |
| Clearance (CL) | 0.516 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 150 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 44880 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUClast, 200 ug/kg
|
[5] |
| Area Under the Concentration-Time Curve (AUC) | 38188 | ng*day/mL |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, AUCinf, 200 ug/kg
|
[5] |
| Elimination Half-Life (t1/2) | 16.2 | day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 200 ug/kg
|
[5] |
| Clearance (CL) | 0.387 | L/day |
Pharmacokinetic parameters of loncastuximab tesirine during Cycle 2 for patients with B-NHL receiving a Q3W regimen, 200 ug/kg
|
[5] |
| Clearance (CL) | 0.218 | L/day |
Efficacy and Safety Exposure-Response Analysis of Loncastuximab Tesirine in Patients with B cell non-Hodgkin Lymphoma, linear clearance
|
[6] |
| Clearance (CL) | 0.0441 | L/day |
Efficacy and Safety Exposure-Response Analysis of Loncastuximab Tesirine in Patients with B cell non-Hodgkin Lymphoma, deconjugation clearance
|
[6] |
| Clearance (CL) | 1.16 | L/day |
Efficacy and Safety Exposure-Response Analysis of Loncastuximab Tesirine in Patients with B cell non-Hodgkin Lymphoma, intercompartmental clearance
|
[6] |
| Area Under the Concentration-Time Curve (AUC) | 337 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 15 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 1596 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 15 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 127 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 30 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 735 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 30 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 43 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 60 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 50.6 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 60 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 671 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 90 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 3370 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 90 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 3907 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 120 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 8744 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 120 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 688 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 1, 150 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 7553 | day*ug/L |
Summary of PK exposure in serum of patients on the Q3W dosing regimen, in relapsed/refractory B-cell acute lymphoblastic leukemia, Cycle 2, 150 ug/kg
|
[7] |
| Clearance (CL) | 80.8 | L/d |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle 1, 90 ug/kg
|
[7] |
| Elimination Half-Life (t1/2) | 0.355 | day |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle 1, 90 ug/kg
|
[7] |
| Clearance (CL) | 9.63 | L/d |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle2, 90 ug/kg
|
[7] |
| Elimination Half-Life (t1/2) | 4.96 | day |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle2, 90 ug/kg
|
[7] |
| Clearance (CL) | 84.3 | L/d |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle 1, 120 ug/kg
|
[7] |
| Elimination Half-Life (t1/2) | 0.156 | day |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle 1, 120 ug/kg
|
[7] |
| Clearance (CL) | 31.1 | L/d |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle2, 120 ug/kg
|
[7] |
| Elimination Half-Life (t1/2) | 7.55 | day |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle2, 120 ug/kg
|
[7] |
| Clearance (CL) | 27.4 | L/d |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle 1, 150 ug/kg
|
[7] |
| Elimination Half-Life (t1/2) | 0.713 | day |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle 1, 150 ug/kg
|
[7] |
| Clearance (CL) | 1.57 | L/d |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle2, 150 ug/kg
|
[7] |
| Elimination Half-Life (t1/2) | 3.99 | day |
Summary of PK parameters of patients on the Q3W dosing regimen (≥90 ug/kg),Cycle2, 150 ug/kg
|
[7] |
| Area Under the Concentration-Time Curve (AUC) | 15916 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2,area under the concentration-time curve from time zero to last quantifiable concentration
Click to Show/Hide
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 16788 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2, area under the concentration-time curve from zero to end of dosing interval tau
|
[8] |
| Elimination Half-Life (t1/2) | 8.25 | day |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2
|
[8] |
| Clearance (CL) | 0.464 | L/day |
Summary of pharmacokinetic parameters during cycles 1 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2
|
[8] |
| Area Under the Concentration-Time Curve (AUC) | 24268 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2,area under the concentration-time curve from time zero to last quantifiable concentration
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[8] |
| Area Under the Concentration-Time Curve (AUC) | 23780 | ng*day/mL |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2, area under the concentration-time curve from zero to end of dosing interval tau
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[8] |
| Elimination Half-Life (t1/2) | 13 | day |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2
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[8] |
| Clearance (CL) | 0.321 | L/day |
Summary of pharmacokinetic parameters during cycles 2 for patients treated with loncastuximab tesirine 150 ug/kg Q3Wx 2
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[8] |
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [9] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
48.28%
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| Patients Enrolled |
Relapsed or refractory diffuse large B-cell lymphoma (DLBCL) after two or more multiagent systemic treatments, who had measurable disease and Eastern Cooperative Oncology Group performance status 0-2.
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| Administration Dosage |
Intravenously on day 1 of each 21-day cycle, at 150 ug/kg for two cycles, then 75 ug/kg thereafter, for up to 1 year or until disease relapse or progression, unacceptable toxicity, death, major protocol deviation, pregnancy, or patient, investigator, or sponsor decision.
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| Related Clinical Trial | |||||
| NCT Number | NCT03589469 | Clinical Status | Phase 2 | ||
| Clinical Description | A phase 2 open-label single-arm study to evaluate the efficacy and safety of loncastuximab tesirine in patients with relapsed or refractory diffuse large B-cell lymphoma (DLBCL) (LOTIS-2). | ||||
| Primary Endpoint |
Overall response rate assessed by central review. 70 of 145 patients had complete or partial response (overall response rate 48.28% [95% CI 39.9-56.7]); 35 had complete response and 35 had partial response.
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| Other Endpoint |
Median time to first response (complete response or partial response) was 41.00 days (IQR 38.00-44.00). Median duration of response was 10.30 months (95% CI 6.9-not estimable); 13.40 months (10.30-not estimable) for patients with complete response and 5.70 months (1.70-not estimable) for patients with partial response. The probability of responders maintaining responses for 9 months or longer was 64.0%. Median progressionfree survival was 4.90 months (95% CI 2.90-8.30), median overall survival was 9.90 months (6.70-11.50), and median relapse-free survival was 13.40 months (10.30-not estimable).
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| Experiment 2 Reporting the Activity Date of This ADC | [10] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
59.40%
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| Patients Enrolled |
R/R B-cell non Hodgkin lymphoma (NHL); had failed or were intolerant to established therapies, or for whom no other established treatment options were available.
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| Administration Dosage |
5 to 200 ug/kg; intravenously over 1 hour, once every 3 weeks (one cycle) by a 3+3 dose-escalation design.
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| Related Clinical Trial | |||||
| NCT Number | NCT02669017 | Clinical Status | Phase 1 | ||
| Clinical Description | A phase 1 dose-escalation study to evaluate the tolerability, safety, pharmacokinetics, and antitumor activity of ADCT-402 in patients with relapsed or refractory b-cell lineage non Hodgkin lymphoma (B-NHL). | ||||
| Primary Endpoint |
The MTD was not established during the trial due to the low level of DLTs, 150 ug/kg dose for expansion and phase 2.
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| Other Endpoint |
For loncastuximab tesirine 120 ug/kg,Median Progression-Free Survival (mPFS)=4.80 months.The median PFS OS=11.60 months.
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| Experiment 3 Reporting the Activity Date of This ADC | [11] | ||||
| Efficacy Data | Complete Remission (CR) |
26.70%
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| Patients Enrolled |
Adults (age 18 years) with histologically confirmed relapsed/refractory B-non Hodgkin lymphoma (World Health Organization 2008 classification18 ) who were intolerant to established therapy, for whom established therapy had failed, or for whom no other treatment options were available in the opinion of the investigator were eligible to participate.
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| Administration Dosage |
3 + 3 dose escalation at 15 to 200 ug/kg and dose expansion at 120 and 150 ug/kg; IV infusion over 60 minutes once every 3 weeks (day 1 of each 21-day cycle).
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| Related Clinical Trial | |||||
| NCT Number | NCT02669017 | Clinical Status | Phase 1 | ||
| Clinical Description | A phase 1 dose-escalation study to evaluate the tolerability, safety, pharmacokinetics, and antitumor activity of ADCT-402 in patients with relapsed or refractory B-cell lineage non Hodgkin lymphoma (B-NHL). | ||||
| Primary Endpoint |
The recommended dose of loncastuximab tesirine for Phase 2 is 150 ug/kg Q3W for 2 doses followed by 75 ug/kg Q3W for subsequent doses. The 150 ug/kg dose was selected as a dose with encouraging responses but lower frequency of AEs than observed with the 200 u/kg dose. Overall response rate (ORR) in evaluable patients was 45.60%, including 26.70% complete responses (CR). Median PFS was 3.10 months (95% CI 2.70-4.20) in all patients with B-NHL, 2.8 months (95% CI 1.90-3.80) in patients with DLBCL, 4.80 months (95% CI 1.10-7.80) in patients with MCL, and could not be determined in those with FL due to the low number of events. Median OS was 8.3 months (95% CI 6.70-10.70) in all patients with B-NHL, 7.5 months (95% CI 6.00-9.80) in patients with DLBCL, and was not reached in patients with MCL or FL due to low number of events.
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| Other Endpoint |
PK exposure similarity between loncastuximab tesirine total antibody and PBD-conjugated antibody indicated good stability in serum.Accumulation by Cycle 2 for patients on a Q6W dosing regimen was lower than that of those on Q3W dosing: mean accumulation of 1.22 and 1.33 for PBD-conjugated antibody and total antibody on Q6W regimens compared with 1.72 and 1.74 on Q3W regimens. There was substantial variability in PK exposure and PK parameters assessed for PBD-conjugated antibody, total antibody, and SG3199.
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| Experiment 4 Reporting the Activity Date of This ADC | [12] | ||||
| Efficacy Data | Complete Remission (CR) |
40.20%
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| Patients Enrolled |
R/R B-acute lymphocytic leukemia (ALL) for standard therapies had failed, intolerant to standard therapies, or no other treatment options were available, in the opinion of the investigator, were eligible for the study, other key inclusion criteria included Eastern Cooperative Oncology Group (ECOG) performance status of 0 to 2.
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| Administration Dosage |
15 to 150 ug/kg once every 3 weeks (Q3W) or 50 ug/kg IV weekly.
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| Related Clinical Trial | |||||
| NCT Number | NCT02669264 | Clinical Status | Phase 1 | ||
| Clinical Description | A phase 1, open-label, adaptive dose-escalation, multicenter study to evaluate the tolerability, safety, pharmacokinetics, and anti-tumor activity of ADCT-402 in patients with relapsed or refractory B-cell lineage acute lymphoblastic leukemia (B-ALL). | ||||
| Primary Endpoint |
Part II (dose expansion portion) utilized the doses of 120 and 150 ug/kg, selected based on antitumor activity and tolerability seen during part I. The overall response rate (ORR) in patients with DLBCL, mantle cell lymphoma, and follicular lymphoma was 42.30%, 46.70%, and 78.60%, respectively.
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| Other Endpoint |
The median progression-free survival (PFS) was 3.10 months in all patients with B-NHL and 2.80 months in patients with DLBCL, whereas the median OS was 8.30 months in all patients and 7.50 months in patients with DLBCL.
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| Experiment 5 Reporting the Activity Date of This ADC | [13] | ||||
| Efficacy Data | Complete Remission (CR) |
46.16%
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References
