General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0TKVCB
ADC Name
Loncastuximab tesirine
Brand Name
Zynlonta
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
Drug Status
Approved in 2021
Drug-to-Antibody Ratio
2.3
Structure
Antibody Name
Loncastuximab
 Antibody Info 
Antigen Name
B-lymphocyte antigen CD19 (CD19)
 Antigen Info 
Payload Name
SG3199 (SC-DR002)
 Payload Info 
Therapeutic Target
Human deoxyribonucleic acid (hDNA)
 Target Info 
Linker Name
Mal-PEG8-Val-Ala-PABC
 Linker Info 
Conjugate Type
Random Cysteines
Combination Type
tesirine
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).
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.
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.
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).
Special Approval(s)
Priority review (FDA); Accelerated approval (FDA); Orphan drug (FDA); Orphan drug (EMA)
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
Trial ID
NCT02669264
Chronic lymphocytic leukemia
1 Trials
Trial ID
NCT02669017; EudraCT2016-000952-92
Diffuse large b-cell lymphoma
2 Trials
Trial ID
NCT02669017; EudraCT2016-000952-92
TWCT00003373; NCT05660395; EudraCT2021-005209-29
1 Trials
Trial ID
NCT05658562; jRCT2021220031
6 Trials
Trial ID
NCT05453396
CTR20211724; ChiCTR2300072058
NCT03589469; EudraCT2017-004288-11
NCT05464719
NCT06918912; EudraCT2024-516929-31; EudraCT2022-001147-24; EUCT2024-516929-31-00
NCT05222438
Follicular lymphoma
1 Trials
Trial ID
NCT02669017; EudraCT2016-000952-92
2 Trials
Trial ID
NCT05453396
NCT04699461; EudraCT2020-003695-40
Mantle cell lymphoma
1 Trials
Trial ID
NCT02669017; EudraCT2016-000952-92
1 Trials
Trial ID
NCT05453396
Unspecific non-hodgkin lymphoma
2 Trials
Trial ID
NCT02669017; EudraCT2016-000952-92
TWCT00003373; NCT05660395; EudraCT2021-005209-29
5 Trials
Trial ID
NCT05453396
NCT05190705
NCT05296070
NCT05464719
NCT06918912; EudraCT2024-516929-31; EudraCT2022-001147-24; EUCT2024-516929-31-00
ADC-specific functional property(2027 Update)
Binding Affinity
Click To Hide/Show 1 ADC-specific functional property Data
Dissocation Constant (Kd) Binding Target Description Reference
Undisclosed
CD19
CD19-expressing Ramos cells exposed to ADCT-402 (1 hour at 4°C) showed prominent cell surface binding
[1]
Bystander Killing Effect
Click To Hide/Show 1 ADC-specific functional property Data
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]
General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
Click To Hide/Show 89 Absorption Data Related to This Level
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.
[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]
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,
[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,
[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]
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.
[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.
[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.
[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]
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.
[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.
[3]
Maximum Observed Concentration (Cmax) 2995 ug/L
PK parameters were available to be calculated from 85 patients, cycle 1
[4]
Area Under the Concentration-Time Curve (AUC) 15245 day*ug/L
PK parameters were available to be calculated from 85 patients, cycle 1
[4]
Maximum Observed Concentration (Cmax) 3155 ug/L
PK parameters were available to be calculated from 85 patients, cycle 2
[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]
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
[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
[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
[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]
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
[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
[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
[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
Click To Hide/Show 84 Distribution Data Related to This Level
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
Click To Hide/Show 51 Metabolism Data Related to This Level
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
Click To Hide/Show 110 Excretion Data Related to This Level
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

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[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
[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
[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
[8]
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 5 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Objective Response Rate (ORR)  NCT03589469
Phase 2
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).
Objective Response Rate (ORR)  NCT02669017
Phase 1
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).

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Complete Remission (CR)  NCT02669017
Phase 1
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).

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Complete Remission (CR)  NCT02669264
Phase 1
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).

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Complete Remission (CR)  Undisclosed Undisclosed
This study evaluated the outcomes of 13 DLBCL patients relapsed after CAR-T cells treated with loncastuximab in the LOTIS-2 trial.
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Objective Response Rate (ORR)
48.28%
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.
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.
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.
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%
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.
Administration Dosage
5 to 200 ug/kg; intravenously over 1 hour, once every 3 weeks (one cycle) by a 3+3 dose-escalation design.
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.
Other Endpoint
For loncastuximab tesirine 120 ug/kg,Median Progression-Free Survival (mPFS)=4.80 months.The median PFS OS=11.60 months.
Experiment 3 Reporting the Activity Date of This ADC [11]
Efficacy Data Complete Remission (CR)
26.70%
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.
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).
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%
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.
Administration Dosage
15 to 150 ug/kg once every 3 weeks (Q3W) or 50 ug/kg IV weekly.
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.
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.
Experiment 5 Reporting the Activity Date of This ADC [13]
Efficacy Data Complete Remission (CR)
46.16%
References
Ref 1 ADCT-402, a PBD dimer-containing antibody drug conjugate targeting CD19-expressing malignancies
Ref 2 Loncastuximab Tesirine: First Approval
Ref 3 Loncastuximab tesirine: an effective therapy for relapsed or refractory diffuse large B-cell lymphoma
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