General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0KTRKE
ADC Name
PF-06664178
Synonyms
PF-06664178; PF?06664178; RN927C
   Click to Show/Hide
Organization
Pfizer (Top20 MNC) (Originator)
Drug Status
Phase 1 (discontinued)
Drug-to-Antibody Ratio
2
Structure
Antibody Name
PF-06478924
 Antibody Info 
Antigen Name
Tumor-associated calcium signal transducer 2 (TACSTD2)
 Antigen Info 
Payload Name
Auristatin 0101 (Aur0101)
 Payload Info 
Payload Target
Microtubule (MT)
 Target Info 
Linker Name
AcLys-Val-Cit-PABC
 Linker Info 
Conjugate Type
Enzymatic Catalysis
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
Unspecific solid tumor
1 Trials
Trial ID
NCT02122146; EudraCT2015-002704-84
Lung cancer
1 Trials
Trial ID
NCT02122146; EudraCT2015-002704-84
Breast cancer
1 Trials
Trial ID
NCT02122146; EudraCT2015-002704-84
Ovarian cancer
1 Trials
Trial ID
NCT02122146; EudraCT2015-002704-84
2027 Update
General Information of The ADMET Data Related to This ADC
Absorption
Click To Hide/Show 1 Absorption Data Related to This Level
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.
[1]
Distribution
Click To Hide/Show 1 Distribution Data Related to This Level
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.
[1]
Metabolism
Click To Hide/Show 1 Metabolism Data Related to This Level
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.
[1]
Excretion
Click To Hide/Show 2 Excretion Data Related to This Level
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.
[1]
Clearance (CL) 32.7 mL/day/kg
Comprehensive Pharmacokinetic Characterization of Antibody-Drug Conjugates,2.4 mg/kg.
[1]
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Undisclosed  NCT02122146
PHASE1
A Phase 1, Dose Escalation Study Of Pf-06664178 In Patients With Locally Advanced Or Metastatic Solid Tumors
Objective Response Rate (ORR)  NCT02122146
Phase 1
A phase 1, dose escalation study of Pf-06664178 in patients with locally advanced or metastatic solid tumors.
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
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.
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.
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.
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.
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Objective Response Rate (ORR)
0%
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).
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.
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.
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.
References
Ref 1 Joint Disposition Properties and Comprehensive Pharmacokinetic Characterization of Antibody-Drug Conjugates
Ref 2 A Study Of PF-06664178 In Patients With Advanced Solid Tumors
Ref 3 A phase 1, dose-escalation study of PF-06664178, an anti-Trop-2/Aur0101 antibody-drug conjugate in patients with advanced or metastatic solid tumors. Invest New Drugs. 2018 Oct;36(5):836-847.