Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0KTRKE
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| ADC Name |
PF-06664178
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| Synonyms |
PF-06664178; PF?06664178; RN927C
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| Organization |
Pfizer (Top20 MNC) (Originator)
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| Drug Status |
Phase 1 (discontinued)
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| Drug-to-Antibody Ratio |
2
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| Structure |
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| Antibody Name |
PF-06478924
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Antibody Info | ||||
| Antigen Name |
Tumor-associated calcium signal transducer 2 (TACSTD2)
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Antigen Info | ||||
| Payload Name |
Auristatin 0101 (Aur0101)
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Payload Info | ||||
| Payload Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
AcLys-Val-Cit-PABC
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Linker Info | ||||
| Conjugate Type |
Enzymatic Catalysis
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2027 Update
The indication landscape of This ADC
2027 Update
The clinical trial pipelines of This ADC
| Indication | Phase 1 | Phase 2 | Phase 3 | Approved | ||
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| Unspecific solid tumor |
1 Trials
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| Lung cancer |
1 Trials
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| Breast cancer |
1 Trials
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| Ovarian cancer |
1 Trials
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2027 Update
General Information of The ADMET Data Related to This ADC
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 97.9 | day*ug/mL |
Comprehensive Pharmacokinetic Characterization of Antibody-Drug Conjugates,2.4 mg/kg.
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[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 97.9 | day*ug/mL |
Comprehensive Pharmacokinetic Characterization of Antibody-Drug Conjugates,2.4 mg/kg.
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[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 97.9 | day*ug/mL |
Comprehensive Pharmacokinetic Characterization of Antibody-Drug Conjugates,2.4 mg/kg.
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[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 97.9 | day*ug/mL |
Comprehensive Pharmacokinetic Characterization of Antibody-Drug Conjugates,2.4 mg/kg.
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[1] |
| Clearance (CL) | 32.7 | mL/day/kg |
Comprehensive Pharmacokinetic Characterization of Antibody-Drug Conjugates,2.4 mg/kg.
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[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 | [2] | ||||
| Patients Enrolled |
Eligible patients had advanced/metastatic solid tumors refractory to standard therapy (Part 2 required NSCLC/ovarian/breast cancer with target expression), ECOG 0-1, and adequate organ function, excluding those with active CNS metastases, recent anticancer therapies, or uncontrolled infections.
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| Administration Dosage |
Part 1 - PF-06664178 will be administered intravenously every 21 days in cohorts of 2 or more patients starting at a dose of 0.15 mg/kg. Increases in dose will continue until MTD is determined.Part 2 - patients with select tumor types (Non Small Cell Lung Cancer ovarian cancer, and breast cancer ) will be treated at the MTD selected in Part 1.
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| Related Clinical Trial | |||||
| NCT Number | NCT02122146 | Clinical Status | PHASE1 | ||
| Clinical Description | A Phase 1, Dose Escalation Study Of Pf-06664178 In Patients With Locally Advanced Or Metastatic Solid Tumors | ||||
| Primary Endpoint |
The study assesses first-cycle dose-limiting toxicities (DLTs) to determine MTD, along with treatment-emergent adverse events (TEAEs) and laboratory abnormalities (hematology, chemistry, coagulation, urinalysis) monitored at multiple timepoints during cycles 1-4 and follow-up.
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| Other Endpoint |
Key outcomes include tumor response per RECIST 1.1, immunogenicity (anti-PF-06664178 antibodies), pharmacokinetics (Cmax, AUCtau, CL, Vss, halflife for PF-06664178, total antibody, and unconjugated payload), Trop-2 expression levels, and drug accumulation ratios across all study parts.
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| Experiment 2 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
0%
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| Patients Enrolled |
Advanced solid tumors resistant to standard therapy, or for which no other therapy was available, and at least one measurable lesion defined by Response Evaluation Criteria in Solid Tumors (RECIST version 1.1).
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| Administration Dosage |
Once every 21 days as an intravenous infusion over approximately 60 min, doses starting from 0.15 mg/kg to 6.14 mg/kg.
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| Related Clinical Trial | |||||
| NCT Number | NCT02122146 | Clinical Status | Phase 1 | ||
| Clinical Description | A phase 1, dose escalation study of Pf-06664178 in patients with locally advanced or metastatic solid tumors. | ||||
| Primary Endpoint |
In the 29 response-evaluable patients,the best overall response observed was limited to stable disease (SD) in 11 patients(37.90%) with PR or CR.
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| Other Endpoint |
Doses explored ranged from 0.15 mg/kg to 4.80 mg/kg. Doses of 3.60 mg/kg,4.20 mg/kg and 4.80 mg/kg were considered intolerable due to DLTs. MTD and RP2D were not determined.
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References
