Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0OUXWT
ADC Name
Rolinsatamab talirine
Synonyms
ABBV 176; ABBV-176; DC-1630993; h16f; ABV176
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Organization
AbbVie, Inc.
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
Rolinsatamab
  Antibody Info 
Antigen Name
Prolactin receptor (PRLR)
  Antigen Info 
Payload Name
SGD-1882
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
Mc-Val-Ala
  Linker Info 
Conjugate Type
Site-specific conjugation through the engineered cysteine S328C.
Combination Type
Talirine
Puchem SID
472419795 , 381128267
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Objective Response Rate (ORR)  NCT03145909
Phase 1
A phase 1 study evaluating the safety, pharmacokinetics and anti-tumor activity of ABBV-176 in subjects with advanced solid tumors likely to express prolactin receptor (PRLR).
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 90.5
%
BT-474 cells
Invasive breast carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
BT-474 cells
Invasive breast carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
BT-474 cells
Invasive breast carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 14 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
5.5
pM
T-47D cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.01
nM
CAMA-1 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.01
nM
22RV1 cells
Prostate carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.11
nM
SW403 cells
Colon adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.16
nM
SMOV-2 cells
Ovarian clear cell adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.24
nM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.26
nM
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.32
nM
MCF-7 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.6
nM
AN3-CA cells
Endometrial adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.77
nM
MDA-MB-231 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
5.2
nM
Huh-7 cells
Adult hepatocellular carcinoma
Half Maximal Inhibitory Concentration (IC50) 
8.6
nM
Hep-G2 cells
Hepatoblastoma
Half Maximal Inhibitory Concentration (IC50) 
> 22
nM
UACC-812 cells
Invasive breast carcinoma of no special type
Half Maximal Inhibitory Concentration (IC50) 
> 22
nM
MDA-MB-231 cells
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Objective Response Rate (ORR)
0.00%
Patients Enrolled
Locally advanced or metastatic solid tumor types associated with PRLR expression, including breast cancer, colorectal cancer, and adrenocortical carcinoma. Patients had progressed on prior treatment, were not amenable to treatment with curative intent, and had no other therapy options known to provide clinical benefit, or were ineligible for such therapies. Patients had an Eastern Cooperative Oncology Group performance status of 0 or 1, and adequate bone marrow, renal, and hepatic function.

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Administration Dosage
Initial dose was 2.70 ug/kg, dose increment was capped at a 100% increase, or at a 50% increase if a grade2 drug-related toxicity had been observed, intravenously every 21 days.
Related Clinical Trial
NCT Number NCT03145909  Clinical Status Phase 1
Clinical Description A phase 1 study evaluating the safety, pharmacokinetics and anti-tumor activity of ABBV-176 in subjects with advanced solid tumors likely to express prolactin receptor (PRLR).
Primary Endpoint
MtD was not formally determined, as identification of a tolerable dose was confounded by late-onset toxicities. ABBV-176 was associated with significant toxicity in this phase 1, dose-escalation study.
Other Endpoint
No patient had an objective response.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.50%
Method Description
Mice implanted with BT-474 breast cancer model and dosed with a single dose of ABBV-176 at 0.5 mg/kg.
In Vivo Model BT-474 CDX
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00%
Method Description
Mice implanted with BT-474 breast cancer model and dosed with a single dose of ABBV-176 at 0.1 mg/kg.
In Vivo Model BT-474 CDX
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00%
Method Description
Mice implanted with BT-474 breast cancer model and dosed with a single dose of ABBV-176 at 0.3 mg/kg.
In Vivo Model BT-474 CDX
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Revealed Based on the Cell Line Data
Click To Hide/Show 14 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.50 pM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.01 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Breast adenocarcinoma CAMA-1 cells CVCL_1115
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.01 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Prostate carcinoma 22RV1 cells CVCL_1045
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Colon adenocarcinoma SW403 cells CVCL_0545
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.16 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Ovarian clear cell adenocarcinoma SMOV-2 cells CVCL_S920
Experiment 6 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.24 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 7 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.26 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 8 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.32 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.60 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Endometrial adenocarcinoma AN3-CA cells CVCL_0028
Experiment 10 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.77 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 11 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.20 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Adult hepatocellular carcinoma Huh-7 cells CVCL_0336
Experiment 12 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.60 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Hepatoblastoma Hep-G2 cells CVCL_0027
Experiment 13 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 22.00 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Invasive breast carcinoma of no special type UACC-812 cells CVCL_1781
Experiment 14 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 22.00 nM
Method Description
The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 A first-in-human, phase 1, dose-escalation study of ABBV-176, an antibody-drug conjugate targeting the prolactin receptor, in patients with advanced solid tumors. Invest New Drugs. 2020 Dec;38(6):1815-1825.
Ref 2 ABBV-176, a PRLR antibody drug conjugate with a potent DNA-damaging PBD cytotoxin and enhanced activity with PARP inhibition. BMC Cancer. 2021 Jun 9;21(1):681.

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