Antibody Information

General Information of This Antibody
Antibody ID
ANI0FUQLW
Antibody Name
Cofetuzumab
Organization
Pfizer Inc.
Indication
Solid tumors
Synonyms
hu6M024; PF-06523435; hu24
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Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Humanized IgG1-kappa
Antigen Name
Inactive tyrosine-protein kinase 7 (PTK7)
  Antigen Info 
ChEMBI ID
CHEMBL3989981
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence
Q1VQLVQSGPEVKKPGASVKVSCKASGYTFTDYAVHWVRQAPGKRLEWIGVISTYNDYTY
NNQDFKGRVTMTRDTSASTAYMELSRLRSDTAVYYCARGNSYFYALDYWGQGTSVTVSSA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP
SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDEL
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPG
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Heavy Chain Varible Domain
QVQLVQSGPEVKKPGASVKVSCKASGYTFTDYAVHWVRQAPGKRLEWIGVISTYNDYTYN
NQDFKGRVTMTRDTSASTAYMELSRLRSEDTAVYYCARGNSYFYALDYWGQGTSVTVSS
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Heavy Chain Constant Domain 1
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKV
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Heavy Chain Constant Domain 2
APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK
PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK
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Heavy Chain Constant Domain 3
GQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS
DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG
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Heavy Chain Hinge Region
EPKSCDKTHTCPPCP
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Heavy Chain CDR 1
GYTFTDYA
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Heavy Chain CDR 2
ISTYNDYT
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Heavy Chain CDR 3
ARGNSYFYALDY
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Light Chain Sequence
EIVLTQSPATLSLSPGERATLSCRASESVDSYGKSFMHWYQQKPGQAPRLLIYRASNLES
GIPARFSGSGSGTDFTLTISSLEPEDFAVYYCQQSNEDPWTFGGGTKLEIKRTVAAPSVF
IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS
STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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Light Chain Varible Domain
EIVLTQSPATLSLSPGERATLSCRASESVDSYGKSFMHWYQQKPGQAPRLLIYRASNLES
GIPARFSGSGSGTDFTLTISSLEPEDFAVYYCQQSNEDPWTFGGGTKLEIK
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Light Chain Constant Domain
RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD
SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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Light Chain CDR 1
ESVDSYGKSF
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Light Chain CDR 2
RAS
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Light Chain CDR 3
QQSNEDPWT
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Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
Cofetuzumab pelidotin [Phase 1]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Partial Response (PR)
16.67%
Patients Enrolled
Metastatic TNBC or ER low (ER and PgR <5%, HER2 negative) breast cancer, and had received at least one prior chemotherapy for metastatic disease.
Administration Dosage
Gedatolisib 110 mg weekly + cofetuzumab pelidotin 1.4 mg/kg every 3 weeks, 180 mg + 1.4 mg/kg, and 180 mg + 2.8 mg/kg.
Related Clinical Trial
NCT Number NCT03243331  Clinical Status Phase 1
Clinical Description
An initial safety study of gedatolisib plus PTK7-ADC for metastatic triple-negative breast cancer.
Primary Endpoint
A total of 18 pts were enrolled in three dose cohorts: gedatolisib 110 mg weekly cofetuzumab pelidotin 1.40 mg/kg every 3 weeks (n=4), 180 mg, 1.40 mg/kg (n=3), and 180 mg, 2.80 mg/kg (n=11). Nausea, anorexia, fatigue, and mucositis were common but rarely reached grade 3 severity. Myelosuppression was uncommon. ORR was 16.67% (3/18). An additional 3 pts had stable disease (of these 2 had stable disease for>18 weeks); CB18 was 27.80%. Median PFS was 2.00 months (95% confidence interval for PFS: 1.20-6.20). Pts with clinical benefit were enriched with genomic alterations in the PI3K and PTK7 pathways.

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Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Objective Response Rate (ORR)
27.00% (Ovarian cancer, every 3 weeks)
16.00% (NSCLC, every 3 weeks)
21.00% (TNBC, every 3 weeks)
26.00% (Ovarian cancer, every 2 weeks)
33.00% (NSCLC, every 2 weeks)
Patients Enrolled
Locally advanced or metastatic solid tumors resistant to standard therapy or with no available standard therapy, and Eastern Cooperative Oncology Group (ECOG) performance status 0 or 1.
Administration Dosage
Intravenously every 3 weeks at 0.20-3.70 mg/kg or every 2 weeks at 2.10-3.20 mg/kg.
Related Clinical Trial
NCT Number NCT02222922  Clinical Status Phase 1
Clinical Description
A first-in-human phase 1, dose escalation, safety and pharmacokinetic study of PF-06647020 in adult patients with advanced solid tumors.
Primary Endpoint
The most common, treatment-related adverse events for PF-06647020 administered every 3 weeks were nausea, alopecia,fatigue, headache, neutropenia, and vomiting (45%); 25% of patients had grade 3 neutropenia. Two patients experienced doselimiting toxicities (grade 3 headache and fatigue) at the highest every 3 weeks dose evaluated. The recommended phase II dose was 2.80 mg/kg every 3 weeks. The overall safety profile observed with PF-06647020 administered every 2 weeks was similar to that of the every 3 weeks regimen. Systemic exposure for the ADC and total antibody generally increased in a dose-proportional manner. Antitumor activity was observed in treated patients with overall objective response rates of 27.00% in ovarian cancer (n=63), 19% in NSCLC (n=31), and 21% in TNBC (n=29).

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Experiment 3 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT04189614  Clinical Status Phase 1
Clinical Description
A phase 1b efficacy and safety study of cofetuzumab pelidotin (ABBV-647, a PTK7-targeting antibody drug conjugate) in subjects with PTK7-expressing, recurrent non-small cell lung cancer.
ADC1-12 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE)
5.76%
Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE)
86.04%
High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
39.39 nM
High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50) > 200 nM Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
ADC1-4 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE)
20.12%
Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE)
93.45%
High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.32 nM
High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50) > 200 nM Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
ADC1-11 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE)
26.44%
Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE) ≈ 100.00% High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.10 nM
High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50) > 200 nM Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
ADC1-2 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE)
34.22%
Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE)
93.47%
High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.23 nM
High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50) > 200 nM Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
ADC1-1 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE)
38.87%
Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Maximum inhibition efficiency (MIE)
95.76%
High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.31 nM
High PTK7 expression (PTK7 +++)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50) > 200 nM Low PTK7 expression (PTK7 +)
Method Description
Cells were then treated with a 10-points titration of compounds, including ADC1-1, ADC1-11,ADC1-4,ADC1-2 and ADC1-12. The plates were incubated for 7 days at 37°C, 5% CO2. Next, 50 uL of Cell-Titer- Glo reagent was added to each well. The mixture was mixed on an orbitalshaker for 10 mins to allow cell lysis.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
References
Ref 1 Initial Phase I Safety Study of Gedatolisib plus Cofetuzumab Pelidotin for Patients with Metastatic Triple-Negative Breast Cancer. Clin Cancer Res. 2022 Aug 2;28(15):3235-3241.
Ref 2 First-in-Human Study of PF-06647020 (Cofetuzumab Pelidotin), an Antibody-Drug Conjugate Targeting Protein Tyrosine Kinase 7, in Advanced Solid Tumors. Clin Cancer Res. 2021 Aug 15;27(16):4511-4520.
Ref 3 A Phase 1b Efficacy and Safety Study of Cofetuzumab Pelidotin (ABBV-647, a PTK7-Targeting Antibody Drug Conjugate) in Subjects With PTK7-Expressing, Recurrent Non-Small Cell Lung Cancer, NCT04189614
Ref 4 Antibody drug conjugates; 2023-07-06.

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