Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0TZZNJ
ADC Name
Mipasetamab uzoptirine
Synonyms
ADCT-601; ADCT601; BGB 601; BGB-601; BGB601; ADCT 601
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Organization
ADC Therapeutics SA; Overland Pharmaceutical (Shanghai) Co., Ltd
Drug Status
Phase 1
Indication
In total 1 Indication(s)
Solid tumors [ICD11:2A00-2A0Z|2B50-2F9Z]
Phase 1
Drug-to-Antibody Ratio
2
Structure
Antibody Name
Mipasetamab
  Antibody Info 
Antigen Name
Tyrosine-protein kinase receptor UFO (AXL)
  Antigen Info 
Payload Name
SG3199
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
BCN-HydraSpace-Val-Ala-PABC
  Linker Info 
Conjugate Type
Site specifically conjugated using GlycoConnect technology (Synaffix) to PL1601.
Combination Type
PL1601
Puchem SID
472419526 , 433770677 , 476001017 , 481988020 , 480403157
ChEBI ID
CHEMBL5095300
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 8 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 35
%
BRCA1-mutated ovarian cancer PDX model (PDX: CTG-0703)
Tumor Growth Inhibition value (TGI) 
≈ 57.4
%
Pancreatic cancer PDX model (PDX: PAXF1657)
Tumor Growth Inhibition value (TGI) 
≈ 65.8
%
BRCA1-mutated ovarian cancer PDX model (PDX: CTG-0703)
Tumor Growth Inhibition value (TGI) 
≈ 68.7
%
MMAE-resistant non-small cell lung cancer PDX model (PDX: NCI-H1299)
Tumor Growth Inhibition value (TGI) 
≈ 72.1
%
MMAE-resistant non-small cell lung cancer PDX model (PDX: NCI-H1299)
Tumor Growth Inhibition value (TGI) 
≈ 84.9
%
Pancreatic cancer PDX model (PDX: PAXF1657)
Tumor Growth Inhibition value (TGI) 
≈ 96.9
%
Pancreatic cancer PDX model (PDX: PAXF1657)
Tumor Growth Inhibition value (TGI) 
≈ 98.5
%
Esophageal caner PDX model (PDX: ES0195)
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 69.4
%
SN12C cells
Renal cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 86.2
%
SN12C cells
Renal cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97.6
%
MDA-MB-231 cells
Breast adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 98.5
%
SN12C cells
Renal cell carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.02
nM
SK-LU-1 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.11
nM
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.35
nM
MDA-MB-231 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.47
nM
PANC-1 cells
Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.59
nM
A-172 cells
Glioblastoma
Half Maximal Inhibitory Concentration (IC50) 
0.83
nM
SN12C cells
Renal cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
2.2
nM
NCI-H1299 cells
Lung large cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
9.29
nM
MDA-MB-361 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
14.62
nM
Karpas-299 cells
ALK-positive anaplastic large cell lymphoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 35.00% (Day 65) Positive AXL expression (AXL+++/++)
Method Description
In vivo antitumor activity of ADCT-601 in BRCA1-mutated ovarian cancer PDX model. Single-dose (0.15 mg/kg,q.d.) ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model BRCA1-mutated ovarian cancer PDX model (PDX: CTG-0703)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 57.40% (Day 21) Positive AXL expression (AXL+++/++)
Method Description
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.075 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 65.80% (Day 65) Negative AXL expression (AXL-)
Method Description
In vivo antitumor activity of ADCT-601 in BRCA1-mutated ovarian cancer PDX model. Single-dose (0.15 mg/kg,q.d.) ADCT-601 in combination with olaparib (50 mg/kg) and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model BRCA1-mutated ovarian cancer PDX model (PDX: CTG-0703)
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 68.70% (Day 30) Negative AXL expression (AXL-)
Method Description
In vivo antitumor activity of ADCT-601 in a MMAE-resistant NCI-H1299 NSCLC model. Single-dose (0.50 mg/kg,q.d.) ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model MMAE-resistant non-small cell lung cancer PDX model (PDX: NCI-H1299)
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 72.10% (Day 30) Positive AXL expression (AXL+++/++; 88,000 copy number)
Method Description
In vivo antitumor activity of ADCT-601 in a MMAE-resistant NCI-H1299 NSCLC model. Single-dose (1.00 mg/kg,q.d.) ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model MMAE-resistant non-small cell lung cancer PDX model (PDX: NCI-H1299)
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.90% (Day 21) Positive AXL expression (AXL+++/++; 88,000 copy number)
Method Description
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.15 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.90% (Day 21) Positive AXL expression (AXL+++/++; 88,000 copy number)
Method Description
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.30 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.50% (Day 51) Positive AXL expression (AXL+++/++; 36,000 copy number)
Method Description
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (1 mg/kg,q.d.) 0.ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model Esophageal caner PDX model (PDX: ES0195)
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.40% (Day 60) Positive AXL expression (AXL+++/++)
Method Description
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.30 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model kidney cancer CDX model
In Vitro Model Renal cell carcinoma SN12C cells CVCL_1705
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.20% (Day 60) Positive AXL expression (AXL+++/++)
Method Description
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.60 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model kidney cancer CDX model
In Vitro Model Renal cell carcinoma SN12C cells CVCL_1705
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.60% (Day 23) Positive AXL expression (AXL+++/++)
Method Description
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (1.00 mg/kg,q.d.). ADCT-601 and isotype-control ADC were administered intravenously (day 1) to treatment groups of 10 mice.
In Vivo Model Triple-negative breast cancer CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.50% (Day 60) Positive AXL expression (AXL+++/++)
Method Description
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (1.00 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model Kidney cancer CDX model
In Vitro Model Renal cell carcinoma SN12C cells CVCL_1705
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.02 nM Positive AXL expression (AXL+++/++; 46,000 copy number)
Method Description
In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.

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In Vitro Model Lung adenocarcinoma SK-LU-1 cells CVCL_0629
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.11 nM Positive AXL expression (AXL+++/++; 88,000 copy number)
Method Description
In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.

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In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.35 nM Positive AXL expression (AXL+++/++; 79,000 copy number)
Method Description
In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.

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In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.47 nM Positive AXL expression (AXL+++/++; 24,000 copy number)
Method Description
In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.

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In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.59 nM Positive AXL expression (AXL+++/++; 23,000 copy number)
Method Description
In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.

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In Vitro Model Glioblastoma A-172 cells CVCL_0131
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.83 nM Positive AXL expression (AXL+++/++; 79,000 copy number)
Method Description
In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.

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In Vitro Model Renal cell carcinoma SN12C cells CVCL_1705
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 2.20 nM Positive AXL expression (AXL+++/++; 20,000 copy number)
Method Description
In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.

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In Vitro Model Lung large cell carcinoma NCI-H1299 cells CVCL_0060
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 9.29 nM Positive AXL expression (AXL+++/++; 79,000 copy number)
Method Description
In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.

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In Vitro Model Breast adenocarcinoma MDA-MB-361 cells CVCL_0620
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 14.62 nM Positive AXL expression (AXL+++/++; 36,000 copy number)
Method Description
In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.

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In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
References
Ref 1 Preclinical Development of ADCT-601, a Novel Pyrrolobenzodiazepine Dimer-based Antibody-drug Conjugate Targeting AXL-expressing Cancers. Mol Cancer Ther. 2022 Apr 1;21(4):582-593.

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