Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0SHGPV
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|---|---|---|---|---|---|---|
| ADC Name |
PF-06647263
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| Synonyms |
PF-06647263
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| Organization |
Stemcentrx (Top20 MNC) (Originator);Pfizer (Top20 MNC)
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| Drug Status |
Phase 1 (discontinued)
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| Drug-to-Antibody Ratio |
4.6
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| Structure |
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| Antibody Name |
HuE22
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Antibody Info | ||||
| Antigen Name |
Ephrin-A4 (EFNA4)
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Antigen Info | ||||
| Payload Name |
N-acetyl-gamma-calicheamicin
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Payload Info | ||||
| Therapeutic Target |
Human deoxyribonucleic acid (hDNA)
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Target Info | ||||
| Linker Name |
AcButDMH
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Linker Info | ||||
| Conjugate Type |
Random Lysines
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| Combination Type |
ozogamicin
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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 | ||
|---|---|---|---|---|---|---|---|---|---|
| Breast cancer |
1 Trials
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| Unspecific solid tumor |
1 Trials
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General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 1410 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1360 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1360 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 21.8 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W.
|
[1] |
| Time to Maximum Concentration (Tmax) | 2.52 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1277 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1249 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1246 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 25.41 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W.
|
[1] |
| Time to Maximum Concentration (Tmax) | 1 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3686 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3483 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3475 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 58.25 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W.
|
[1] |
| Time to Maximum Concentration (Tmax) | 1 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6350 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6057 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6023 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 84.4 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W.
|
[1] |
| Time to Maximum Concentration (Tmax) | 3.97 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 7227 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6667 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6363 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 101.6 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W.
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[1] |
| Time to Maximum Concentration (Tmax) | 1.05 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 14200 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13600 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13400 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 154 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W.
|
[1] |
| Time to Maximum Concentration (Tmax) | 1.03 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 594.1 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 12.64 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 1 (single dose).
|
[1] |
| Time to Maximum Concentration (Tmax) | 1 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 1 (single dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 927.8 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 11.86 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Time to Maximum Concentration (Tmax) | 1 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 544.8 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 11.96 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 1 (single dose).
|
[1] |
| Time to Maximum Concentration (Tmax) | 1 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 1 (single dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1166 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 13.73 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Time to Maximum Concentration (Tmax) | 1 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1056 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 22.63 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 1 (single dose).
|
[1] |
| Time to Maximum Concentration (Tmax) | ` | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 1 (single dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | `570 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 27.45 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Time to Maximum Concentration (Tmax) | 1 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 669.9 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 16.86 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 1 (single dose).
|
[1] |
| Time to Maximum Concentration (Tmax) | 1 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 1 (single dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1274 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Maximum Observed Concentration (Cmax) | 17.84 | ng/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Time to Maximum Concentration (Tmax) | 1 | h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 1410 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1360 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1360 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUCt.
|
[1] |
| Volume of Distribution (Vd) | 116 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1277 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1249 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1246 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUCt.
|
[1] |
| Volume of Distribution (Vd) | 162.7 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3686 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3483 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3475 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUCt.
|
[1] |
| Volume of Distribution (Vd) | 114.8 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6350 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6057 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6023 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUCt.
|
[1] |
| Volume of Distribution (Vd) | 134 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 7227 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6667 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6363 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUCt.
|
[1] |
| Volume of Distribution (Vd) | 116.5 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 14200 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13600 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13400 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUCt.
|
[1] |
| Volume of Distribution (Vd) | 159 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 594.1 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 927.8 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Volume of Distribution (Vd) | 84.01 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 544.8 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1166 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Volume of Distribution (Vd) | 102.3 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1056 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | `570 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Volume of Distribution (Vd) | 96.1 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 669.9 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1274 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Volume of Distribution (Vd) | 72.31 | L |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 1410 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1360 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1360 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1277 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1249 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1246 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3686 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3483 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3475 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6350 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6057 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6023 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 7227 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6667 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6363 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 14200 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13600 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13400 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 594.1 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 927.8 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 544.8 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1166 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1056 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | `570 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 669.9 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1274 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 1410 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1360 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1360 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W, AUCt.
|
[1] |
| Clearance (CL) | 0.938 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W.
|
[1] |
| Elimination Half-Life (t1/2) | 4.76 | day |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.015 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1277 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1249 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1246 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W, AUCt.
|
[1] |
| Clearance (CL) | 1.547 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W.
|
[1] |
| Elimination Half-Life (t1/2) | 4.403 | day |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.03 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3686 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3483 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 3475 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W, AUCt.
|
[1] |
| Clearance (CL) | 1.108 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W.
|
[1] |
| Elimination Half-Life (t1/2) | 3.541 | day |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.05 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6350 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6057 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6023 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W, AUCt.
|
[1] |
| Clearance (CL) | 0.9244 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W.
|
[1] |
| Elimination Half-Life (t1/2) | 5.353 | day |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.075 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 7227 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6667 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 6363 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W, AUCt.
|
[1] |
| Clearance (CL) | 0.9219 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W.
|
[1] |
| Elimination Half-Life (t1/2) | 4.336 | day |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.1 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 14200 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUCinf.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13600 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUClast.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13400 | ug*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W, AUCt.
|
[1] |
| Clearance (CL) | 1.06 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W.
|
[1] |
| Elimination Half-Life (t1/2) | 5.28 | day |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, 0.134 mg/kg Q3W.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 594.1 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 927.8 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Clearance (CL) | 0.7932 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.01 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 544.8 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1166 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Clearance (CL) | 0.9454 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1056 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | `570 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Clearance (CL) | 0.868 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 1, 0.02 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 669.9 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 1 (single dose), AUCt.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1274 | ng*h/mL |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose), AUCt.
|
[1] |
| Clearance (CL) | 0.8451 | L/h |
Summary of serum PF-06647263 (ADC) pharmacokinetic parameters, Part 2, 0.015 mg/kg QW, cycle 1 day 15 (multiple dose).
|
[1] |
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 | [1] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
10.4
8.3 % |
|||
| Patients Enrolled |
Eligibility criteria include advanced/metastatic solid tumors refractory to standard therapy (Part 2 focuses on triple-negative breast cancer), ECOG PS 0-1, and adequate organ function. Exclusions involve active brain metastases, recent major surgery/radiotherapy/systemic therapy, or uncontrolled infections.
|
||||
| Administration Dosage |
Part 1- PF-06647263 will be administered intravenously in either a 21 day cycle or weekly in cohorts of 2 or more patients starting at a dose of 0.015 mg/kg. Increases in dose will continue until MTD is determined.Part 2- Patients with triple negative breast cancer will be treated at the MTD or Recommended Phase 2 dose selected in Part 1.
|
||||
| Related Clinical Trial | |||||
| NCT Number | NCT02078752 | Clinical Status | PHASE1 | ||
| Clinical Description | A FIRST-IN-HUMAN PHASE 1, DOSE ESCALATION, SAFETY AND PHARMACOKINETIC STUDY OF PF-06647263 IN ADULT PATIENTS WITH ADVANCED SOLID TUMORS | ||||
| Primary Endpoint |
The primary outcomes include dose-limiting toxicities (DLTs) in Part 1, defined as hematologic (e.g., grade 4 neutropenia, febrile neutropenia) or non-hematologic (e.g., bilirubin increase ≥2×ULN, grade ≥3 toxicities) adverse events during the first treatment cycle, and objective response rate (ORR) in Part 2, assessed per RECIST v1.1 criteria for complete or partial response in target and non-target lesions.
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|
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| Other Endpoint |
Secondary outcomes encompass treatment-emergent adverse events (AEs), serious AEs (SAEs), vital sign abnormalities, pharmacokinetic parameters (AUC, Cmax, Tmax, CL, Vss, t½) for PF-06647263, total antibody, and unconjugated payload, laboratory test abnormalities, immunogenicity (anti-drug antibodies), clinical benefit response (CBR), progression-free survival (PFS), and overall survival (OS) stratified by EFNA4 expression.
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|
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| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
10.40
9.10 % |
|||
| Patients Enrolled |
Advanced solid tumors resistant to standard therapy or for which no standard therapy.
|
||||
| Administration Dosage |
Every 3 weeks (Q3W) or every week (QW), following a modified toxicity probability interval (mTPI) method (initial dosing: 0.015 mg/kg Q3W).
|
||||
| Related Clinical Trial | |||||
| NCT Number | NCT02078752 | Clinical Status | Phase 1 | ||
| Clinical Description | A first-in-human phase 1, dose escalation, safety and pharmacokinetic study of PF-06647263 in adult patients with advanced solid tumors. | ||||
| Primary Endpoint |
Six (10.00%) patients achieved a confirmed partial response and 22 (36.70%) patients had stable disease. No correlations were observed between tumor responses and EFNA4 expression levels. Study findings showed manageable safety and favorable PK for PF-06647263 administered QW at the RP2D,with preliminary evidence of limited antitumor activity in patients with TNBC and ovarian cancer.
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| Other Endpoint |
The RP2D was determined to be 0.015 mg/kg QW.
|
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| Experiment 3 Reporting the Activity Date of This ADC | [3] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT02078752 | Clinical Status | Phase 1 | ||
| Clinical Description | A first-in-human phase 1, dose escalation, safety and pharmacokinetic study of PF-06647263 in adult patients with advanced solid tumors. | ||||
References