Payload Information

General Information of This Payload
Payload ID
PAY0AKDAM
Name
SGD-1882
Synonyms
SGD-1882
   Click to Show/Hide
Target(s) Human Deoxyribonucleic acid (hDNA)
 Target Info 
Structure
Formula
C42H39N5O7
Isosmiles
COc1ccc(C2=CN3C(=O)c4cc(OC)c(OCCCOc5cc6c(cc5OC)C(=O)N5C=C(c7ccc(N)cc7)CC5C=N6)cc4N=CC3C2)cc1
InChI
InChI=1S/C42H39N5O7/c1-50-32-11-7-26(8-12-32)28-16-31-22-45-36-20-40(38(52-3)18-34(36)42(49)47(31)24-28)54-14-4-13-53-39-19-35-33(17-37(39)51-2)41(48)46-23-27(15-30(46)21-44-35)25-5-9-29(43)10-6-25/h5-12,17-24,30-31H,4,13-16,43H2,1-3H3
InChIKey
OMRPLUKQNWNZAV-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
725.802
Polar area
137.51
Complexity
54
xlogp Value
7.0855
Heavy Count
54
Rot Bonds
11
Hbond acc
10
Hbond Donor
1
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
Serclutamab talirine [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)
4.17%
High EGFR expression (EGFR+++)
Patients Enrolled
Advanced, histologically confirmed solid tumors associated with EGFR overexpression (centralized testing).
Administration Dosage
Ser-T intravenously once every 4 weeks (Q4W; 5-50 ug/kg) in the dose-escalation phase.
Related Clinical Trial
NCT Number NCT03234712  Phase Status Phase 1
Clinical Description
A phase 1 study evaluating the safety, pharmacokinetics, and anti-tumor activity of ABBV-321 in subjects with advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR).
Primary Endpoint
One patient was PR (N=1/24, 4.17%), 6 patients was SD (N=6/24,25.00%). Median DOR (CR + PR + SD)=6.40 months (95% CI 3.0not reached). The median PFS=1.8 months (95% CI 1.3-5.8), median OS=7.10 months (95% CI: 4.1-12.3).
Other Endpoint
Ser-T RP2D regimen=25 ug/kg Q4W.
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Partial Response (PR)
4.20%
High EGFR expression (EGFR+++)
Patients Enrolled
Advanced, histologically confirmed solid tumors associated with EGFR overexpression (centralized testing).
Administration Dosage
Ser-T intravenously once every 4 weeks (Q4W; 5-50 ug/kg) in the dose-escalation phase.
Related Clinical Trial
NCT Number NCT03234712  Phase Status Phase 1
Clinical Description
A phase 1 study evaluating the safety, pharmacokinetics, and anti-tumor activity of ABBV-321 in subjects with advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR).
Primary Endpoint
Responses included 1 partial response (PR), 6 stable disease (SD), 14 progressive disease (PD); 3 patients were not evaluable for response. Median duration of clinical benefit (complete response + PR + SD) was 6.40 months (95% CI: 3.00-not reached).
Other Endpoint
The median PFS was 1.80 months (95% CI: 1.30-5.80) and the median OS was 7.10 months (95% CI: 4.10-12.30).
Experiment 3 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT03234712  Phase Status Phase 1
Clinical Description
A phase 1 study evaluating the safety, pharmacokinetics, and anti-tumor activity of ABBV-321 in subjects with advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR).
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 34.00% (Day 66) High EGFR expression (EGFR+++)
Method Description
ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model Glioblastoma PDX model (PDX: SNO199)
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 40.00% (Day 66) Low EGFR expression (EGFR+)
Method Description
ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model Glioblastoma PDX model (PDX: SNO199)
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 76.00% (Day 24) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,demonstrated with ABBV-321 dosed at 0.15 mg/kg 2 every seven days 3.
In Vivo Model EGFR-expressing malignant mesothelioma PDX model (PDX: 1174)
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 88.57% (Day 68) Moderate EGFR expression (EGFR++)
Method Description
ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model Glioblastoma PDX model (PDX: SNO207)
Experiment 5 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.20% (Day 70) Moderate EGFR expression (EGFR++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.2 mg/kg,every seven days 3.
In Vivo Model EGFR-expressing GBM brain cancer PDX model (PDX: SNO199)
Experiment 6 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.60% (Day 66) Moderate EGFR expression (EGFR++)
Method Description
ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model Glioblastoma PDX model (PDX: SNO207)
Experiment 7 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.70% (Day 74) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.2 mg/kg,every seven days 3.
In Vivo Model EGFR-expressing GBM brain cancer PDX model (PDX: SNO207)
Experiment 8 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.80% (Day 33) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression, administered at 0.5 mg/kg on a Q7D 6 regimen.
In Vivo Model EGFR-expressing colorectal adenocarcinoma PDX model (PDX: LoVo)
Experiment 9 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.40% (Day 74) Moderate EGFR expression (EGFR++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.4 mg/kg,every seven days 3.
In Vivo Model EGFR-expressing GBM brain cancer PDX model (PDX: SNO207)
Experiment 10 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.20% (Day 70) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.4 mg/kg,every seven days 3.
In Vivo Model EGFR-expressing GBM brain cancer PDX model (PDX: SNO199)
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 16 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 52.40% (Day 28) Moderate EGFR expression (EGFR++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.0125 mg/kg.
In Vivo Model EGFR-expressing SW48 CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 55.30% (Day 35) Low EGFR expression (EGFR+)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of lung squamous cell carcinoma cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model EGFR-expressing EBC-1 CDX model
In Vitro Model Lung squamous cell carcinoma EBC-1 cells CVCL_2891
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 70.60% (Day 28) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.025 mg/kg.
In Vivo Model EGFR-expressing SW48 CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 73.80% (Day 38) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model EGFR-expressing A-253 CDX model
In Vitro Model Submandibular gland squamous cell carcinoma A-253 cells CVCL_1060
Experiment 5 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.10% (Day 38) Moderate EGFR expression (EGFR++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.3 mg/kg.
In Vivo Model EGFR-expressing A-253 CDX model
In Vitro Model Submandibular gland squamous cell carcinoma A-253 cells CVCL_1060
Experiment 6 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 82.80% (Day 28) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.05 mg/kg.
In Vivo Model EGFR-expressing SW48 CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 7 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 82.80% (Day 28) Moderate EGFR expression (EGFR++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model EGFR-expressing SW48 CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 8 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.10% (Day 31) Moderate EGFR expression (EGFR++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model EGFR-expressing FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 9 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 89.90% (Day 30) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model EGFR-expressing HCT 116 CDX model
In Vitro Model Colon carcinoma HCT 116 cells CVCL_0291
Experiment 10 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 89.90% (Day 30) Low EGFR expression (EGFR+)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,administered 0.4 mg/kg,at every seven days 3.
In Vivo Model EGFR-expressing HCT 116 CDX model
In Vitro Model Colon carcinoma HCT 116 cells CVCL_0291
Experiment 11 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.80% (Day 31) Negative EGFR expression (EGFR-)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.3 mg/kg.
In Vivo Model EGFR-expressing FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 12 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) Low EGFR expression (EGFR+)
Method Description
ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model Glioblastoma U-87MG CDX model
In Vitro Model Glioblastoma U-87MG ATCC cells CVCL_0022
Experiment 13 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) High EGFR expression (EGFR+++)
Method Description
ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model Glioblastoma U-87MG CDX model
In Vitro Model Glioblastoma U-87MG ATCC cells CVCL_0022
Experiment 14 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 42) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.2 mg/kg,every seven days 3.
In Vivo Model EGFR-expressing U-87MG CDX model
In Vitro Model Glioblastoma U-87MG ATCC cells CVCL_0022
Experiment 15 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 42) High EGFR expression (EGFR+++)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.4 mg/kg,every seven days 3.
In Vivo Model EGFR-expressing U-87MG CDX model
In Vitro Model Glioblastoma U-87MG ATCC cells CVCL_0022
Experiment 16 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 24) Low EGFR expression (EGFR+)
Method Description
Serclutamab talirine induces efficient tumor cell killing in PDX models of lung squamous cell carcinoma cell with EGFR expression,a single dose of 0.3 mg/kg.
In Vivo Model EGFR-expressing EBC-1 CDX model
In Vitro Model Lung squamous cell carcinoma EBC-1 cells CVCL_2891
Revealed Based on the Cell Line Data
Click To Hide/Show 38 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
15.00 pM
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.23 nM
Negative EGFR expression (EGFR-)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Glioblastoma U-87 MGvIII cells CVCL_0022
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.70 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Astrocytoma U-251MG cells CVCL_0021
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.70 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma LoVo cells CVCL_0399
Experiment 5 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.00 nM
Moderate EGFR expression (EGFR++; IHC 2+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma LS174T cells CVCL_1384
Experiment 6 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.10 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma SK-CO-1 cells CVCL_0626
Experiment 7 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.40 nM
Negative EGFR expression (EGFR-)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Astrocytoma SF268 cells CVCL_1689
Experiment 8 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.50 nM
Low EGFR expression (EGFR+; IHC 1+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Glioblastoma M059K cells CVCL_0401
Experiment 9 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.50 nM
Moderate EGFR expression (EGFR++)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon cancer HT29 cells CVCL_A8EZ
Experiment 10 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.80 nM
Moderate EGFR expression (EGFR++; IHC 2+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma SW403 cells CVCL_0545
Experiment 11 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.90 nM
High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Primitive neuroectodermal tumor PFSK-1 cells CVCL_1642
Experiment 12 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.50 nM
High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Gliosarcoma SF539 cells CVCL_1691
Experiment 13 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.60 nM
Moderate EGFR expression (EGFR++)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma COLO 201 cells CVCL_1987
Experiment 14 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.80 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Glioblastoma M059J cells CVCL_0400
Experiment 15 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.30 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
Experiment 16 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.70 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Astrocytoma SNB-19 cells CVCL_0535
Experiment 17 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.30 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma SW620 cells CVCL_0547
Experiment 18 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.60 nM
Low EGFR expression (EGFR+; IHC 1+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Glioblastoma U-87MG cells CVCL_0022
Experiment 19 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.60 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma SW1116 cells CVCL_0544
Experiment 20 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.70 nM
Low EGFR expression (EGFR+; IHC 1+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon carcinoma RKO cells CVCL_0504
Experiment 21 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.80 nM
Negative EGFR expression (EGFR-)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Anaplastic astrocytoma CHLA-03-AA cells CVCL_U616
Experiment 22 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.80 nM
Moderate EGFR expression (EGFR++)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Rectal adenocarcinoma SW1463 cells CVCL_1718
Experiment 23 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.50 nM
Moderate EGFR expression (EGFR++)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma WiDr cells CVCL_2760
Experiment 24 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.00 nM
Moderate EGFR expression (EGFR++; IHC 2+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma SW480 cells CVCL_0546
Experiment 25 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.40 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Glioblastoma LN-18 cells CVCL_0392
Experiment 26 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9.00 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma DLD-1 cells CVCL_0248
Experiment 27 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9.50 nM
Moderate EGFR expression (EGFR++; IHC 2+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Cecum adenocarcinoma LS1034 cells CVCL_1382
Experiment 28 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.60 nM
Negative EGFR expression (EGFR-)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Glioblastoma SNB-75 cells CVCL_1706
Experiment 29 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.80 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma T84 cells CVCL_0555
Experiment 30 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12.00 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon carcinoma HCT 116 cells CVCL_0291
Experiment 31 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
13.90 nM
Low EGFR expression (EGFR+; IHC 1+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma Caco-2 cells CVCL_0025
Experiment 32 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
14.50 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Glioblastoma T98G cells CVCL_0556
Experiment 33 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
16.10 nM
Low EGFR expression (EGFR+; IHC 1+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Astrocytoma U-138MG cells CVCL_0020
Experiment 34 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
17.60 nM
Low EGFR expression (EGFR+; IHC 1+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma COLO 320DM cells CVCL_0219
Experiment 35 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
18.00 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Anaplastic astrocytoma DBTRG-05MG cells CVCL_1169
Experiment 36 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
23.20 nM
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Glioblastoma A-172 cells CVCL_0131
Experiment 37 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
24.90 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma COLO 320HSR cells CVCL_0220
Experiment 38 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
28.40 nM
High EGFR expression (EGFR+++; IHC 3+)
Method Description
The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model Colon adenocarcinoma HCT 15 cells CVCL_0292
Rolinsatamab talirine [Phase 1]
 ADC Info 
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 [2]
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.

   Click to Show/Hide
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  Phase 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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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 [5]
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
Vadastuximab talirine [Terminated in phase 3]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Incomplete Count Recovery (CRi)
26.00% (Placebo + HMA)
Patients Enrolled
Older patients with newly diagnosed acute myeloid leukemia (AML).
Administration Dosage
33A, iv, 10 mcg/kg, every 4 weeks plus azacitidine 75 mg/m2, SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m2, iv x 5 days, every 4 weeks; placebo plus plus azacitidine 75 mg/m2, SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m2, iv x 5 days, every 4 weeks.
Related Clinical Trial
NCT Number NCT02326584  Phase Status Phase 1
Clinical Description
A phase 1b dose-escalation study of SGN-CD33A in combination with standard-of-care for patients with newly diagnosed acute myeloid leukemia.
Experiment 2 Reporting the Activity Date of This ADC [7]
Efficacy Data Complete Remission (CR)
66.70% (Pre-allo Before Stem Cell Transplant)
Patients Enrolled
Patients With Relapsed or Refractory AmL.
Administration Dosage
Post-allo after stem cell transplant in Day 1 of each cycle; Pre-allo in Day 1 of each cycle plus melphalan 30 mg/m2/day iv and fludarabine 140 mg/m2 iv before stem cell transplant.
Related Clinical Trial
NCT Number NCT02785900  Phase Status Phase 3
Clinical Description
A randomized, double-blind phase 3 study of vadastuximab talirine (SGN-CD33A) versus placebo in combination with azacitidine or decitabine in the treatment of older patients with newly diagnosed acute myeloid leukemia (AML).
Experiment 3 Reporting the Activity Date of This ADC [8]
Efficacy Data Complete Remission (CR)
11.00% (all treated, dose escalation/expansion 40 ug/kg)
12.00% (efficacy evaluable, dose escalation/expansion 40 ug/kg)
22.00% (all treated
treatment naive 40 ug/kg)
23.00% (efficacy evaluable, treatment naive 40 ug/kg)
Patients Enrolled
CD33-positive AmL (any level of CD33 expression as detected by local flow cytometric assessment) and had either newly diagnosed AmL (declining intensive induction/consolidation chemotherapy) or AmL relapsed after a minimum remission duration of 12 weeks after intensive induction/consolidation.
Administration Dosage
Slow IV push on day 1 (5-60 ug/kg) or on days 1 and 4 (20 ug/kg) of 21-day cycles.
Related Clinical Trial
NCT Number NCT01902329  Phase Status Phase 1
Clinical Description
A phase 1 trial of SGN-CD33A in patients with CD33-positive acute myeloid leukemia.
Primary Endpoint
The recommended monotherapy dose is 4.00 mg/kg.
Other Endpoint
The complete remission rate (CRc) among the 69 patients in the dose-finding cohorts, was 19.00% (6.00% CR + 13.00% CRi, 95% confidence interval [CI], 10.40-30.10).
Experiment 4 Reporting the Activity Date of This ADC [6]
Efficacy Data Complete Remission (CR)
30.00% (33A + HMA)
26.00% (Placebo + HMA)
Patients Enrolled
Older patients with newly diagnosed acute myeloid leukemia (AML).
Administration Dosage
33A, iv, 10 mcg/kg, every 4 weeks plus azacitidine 75 mg/m2, SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m2, iv x 5 days, every 4 weeks; placebo plus plus azacitidine 75 mg/m2, SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m2, iv x 5 days, every 4 weeks.
Related Clinical Trial
NCT Number NCT02326584  Phase Status Phase 1
Clinical Description
A phase 1b dose-escalation study of SGN-CD33A in combination with standard-of-care for patients with newly diagnosed acute myeloid leukemia.
Experiment 5 Reporting the Activity Date of This ADC [9]
Efficacy Data Complete Remission (CR)
43.00% (all treated)
42.00% (secondary AmL)
34.00% (75 y old)
80.00% (FLT3/ITD+)
50.00% (MRC adv)
39.00% (Und. Myelo)
Patients Enrolled
New diagnosis of CD33-expressing AmL, they could not have received prior therapy with HMAs; however, prior low-intensity treatment, such as hydroxyurea for cytoreduction or other low-intensity therapies for preceding myelodysplastic syndrome (MDS), an Eastern Cooperative Oncology Group (ECOG) performance status 0 or 1, with adequate baseline renal, hepatic, and pulmonary function.

   Click to Show/Hide
Administration Dosage
Azacitidine (75 mg/m2 subcutaneous/intravenous 7 days) or decitabine (20 mg/m2 intravenous 5 days) was administered per institutional standard. On the final day of HMA administration (day 7 of azacitidine treatment and day 5 of decitabine treatment), vadastuximab talirine (10 ug/kg) was administered via slow intravenous push (1-2 mL/min), after infusion of the HMA, as 28-day cycles for up to 4 cycles of treatment.

   Click to Show/Hide
Related Clinical Trial
NCT Number NCT01902329  Phase Status Phase 1
Clinical Description
A phase 1 trial of SGN-CD33A in patients with CD33-positive acute myeloid leukemia.
Primary Endpoint
The 30- and 60-day mortality rates were 2% and 8%, respectively. No DLTs or infusion-related reactions were observed in the combination cohort of this study.
Other Endpoint
CR and CRi, was 70.00% (43% CR + 26% CRi, 95% CI, 55.70-81.70). Median RFS was 7.70 months (95% CI, 4.90-15.40) with 11.30 months (95% CI, 8.80-13.20) median OS.
Experiment 6 Reporting the Activity Date of This ADC [10]
Patients Enrolled
Patients with operable HER2-positive primary breast cancer.
Administration Dosage
Anthracycline then Trastuzumab Emtansine and Pertuzumab ; Anthracycline then Trastuzumab, Pertuzumab, and Taxane.
Related Clinical Trial
NCT Number NCT02614560  Phase Status Phase 1/2
Clinical Description
A phase 1/2 study of vadastuximab talirine administered in sequence with allogeneic hematopoietic stem cell transplant in patients with relapsed or refractory acute myeloid leukemia (AML).
Experiment 7 Reporting the Activity Date of This ADC [11]
Patients Enrolled
Patients With acute myeloid leukemia (AML).
Administration Dosage
SGN-CD33A iv in Day 1 or Days 1 and 4 of each cycle; High dose cytarabine + SGN-CD33A (28-day cycles); Standard dose cytarabine and daunorubicin + SGN-CD33A; standard dose cytarabine and daunorubicin + SGN-CD33A and High dose cytarabine + SGN-CD33A.
Related Clinical Trial
NCT Number NCT01902329  Phase Status Phase 1
Clinical Description
A phase 1 trial of SGN-CD33A in patients with CD33-positive acute myeloid leukemia.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [12]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00% (Day 36) High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 100mcg/kg.
In Vitro Model Erythroleukemia HEL 92.1.7 cells (Multidrug resistance) CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC [12]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 29.44% (Day 30) High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 30mcg/kg.
In Vitro Model Adult acute myeloid leukemia HL-60 cells CVCL_0002
Experiment 3 Reporting the Activity Date of This ADC [12]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 47.77% (Day 36) High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 300mcg/kg.
In Vitro Model Erythroleukemia HEL 92.1.7 cells (Multidrug resistance) CVCL_2481
Experiment 4 Reporting the Activity Date of This ADC [12]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 78.95% (Day 38) Negative CD33 expression (CD33-)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 100mcg/kg.
In Vitro Model Anaplastic thyroid cancer TF1-alpha cells (Multidrug resistance) Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC [12]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.41% (Day 36) High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 1000mcg/kg.
In Vitro Model Erythroleukemia HEL 92.1.7 cells (Multidrug resistance) CVCL_2481
Experiment 6 Reporting the Activity Date of This ADC [12]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.53% (Day 38) Negative CD33 expression (CD33-)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 300mcg/kg.
In Vitro Model Anaplastic thyroid cancer TF1-alpha cells (Multidrug resistance) Homo sapiens
Experiment 7 Reporting the Activity Date of This ADC [12]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.99% (Day 30) High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 100mcg/kg.
In Vitro Model Adult acute myeloid leukemia HL-60 cells CVCL_0002
Experiment 8 Reporting the Activity Date of This ADC [12]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.99% (Day 40) Negative CD33 expression (CD33-)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 300mcg/kg.
In Vitro Model Anaplastic thyroid cancer TF1-alpha cells (Multidrug resistance) Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 33 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 ng/mL
Moderate CD33 expression (CD33++; CD33 MFI=3,919)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG019 Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 ng/mL
Moderate CD33 expression (CD33++; 6,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Childhood acute monocytic leukemia MV4-11 cells CVCL_0064
Experiment 3 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.20 ng/mL
High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG022 Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.20 ng/mL
Moderate CD33 expression (CD33++; CD33 MFI=1,355)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG014 Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.20 ng/mL
High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG023 Homo sapiens
Experiment 6 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.20 ng/mL
High CD33 expression (CD33+++; CD33 MFI=10,762)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG018 Homo sapiens
Experiment 7 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.20 ng/mL
High CD33 expression (CD33+++; CD33 MFI=11,850)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG015 Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.40 ng/mL
Low CD33 expression (CD33+; CD33 MFI=107)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG003 Homo sapiens
Experiment 9 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.90 ng/mL
Moderate CD33 expression (CD33++; CD33 MFI=5,817)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG002 Homo sapiens
Experiment 10 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.00 ng/mL
High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Adult acute myeloid leukemia HL-60 cells CVCL_0002
Experiment 11 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.00 ng/mL
High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Adult acute myeloid leukemia KG-1 cells CVCL_0374
Experiment 12 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.00 ng/mL
Negative CD33 expression (CD33-; CD33 MFI=20)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG017 Homo sapiens
Experiment 13 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.00 ng/mL
Negative CD33 expression (CD33-; CD33 MFI=49)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG001 Homo sapiens
Experiment 14 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.00 ng/mL
High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Acute myeloid leukemia SH-1 cells CVCL_2191
Experiment 15 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.00 ng/mL
High CD33 expression (CD33+++; CD33 MFI=23,223)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Erythroleukemia HEL 92.1.7 cells CVCL_2481
Experiment 16 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.00 ng/mL
High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Childhood acute monocytic leukemia THP-1 cells CVCL_0006
Experiment 17 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 7.50 ng/mL High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Acute myeloid leukemia SIG-M5 cells CVCL_1694
Experiment 18 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.00 ng/mL
Moderate CD33 expression (CD33++; CD33 MFI=1,035)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG008 Homo sapiens
Experiment 19 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.00 ng/mL
Low CD33 expression (CD33+; CD33 MFI=216)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG013 Homo sapiens
Experiment 20 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
22.00 ng/mL
High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Adult acute monocytic leukemia U-937 cells CVCL_0007
Experiment 21 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
23.00 ng/mL
Low CD33 expression (CD33+; CD33 MFI=299)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG010 Homo sapiens
Experiment 22 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
26.00 ng/mL
High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Acute myeloid leukemia HNT-34 cells CVCL_2071
Experiment 23 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
32.00 ng/mL
Moderate CD33 expression (CD33++; CD33 MFI=1,184)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG004 Homo sapiens
Experiment 24 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
33.00 ng/mL
Moderate CD33 expression (CD33++; CD33 MFI=6,598)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG011 Homo sapiens
Experiment 25 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
49.00 ng/mL
Moderate CD33 expression (CD33++; CD33 MFI=2,278)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Anaplastic thyroid cancer TF1-alpha cells (Multidrug resistance) Homo sapiens
Experiment 26 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
61.00 ng/mL
Moderate CD33 expression (CD33++; 7,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Esophageal squamous cell carcinoma TF-1 cells CVCL_1759
Experiment 27 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
68.00 ng/mL
High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Adult acute myeloid leukemia SH-2 cells CVCL_2190
Experiment 28 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 110.00 ng/mL Negative CD33 expression (CD33-; CD33 MFI=0)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG009 Homo sapiens
Experiment 29 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 110.00 ng/mL High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG020 Homo sapiens
Experiment 30 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 110.00 ng/mL Low CD33 expression (CD33+; CD33 MFI=353)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model Acute myeloid leukemia Acute myeloid leukemia cells #SG012 Homo sapiens
Experiment 31 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000.00 ng/mL High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 32 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000.00 ng/mL Low CD33 expression (CD33+; CD33 MFI=318)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Ovarian clear cell adenocarcinoma ES-2 cells CVCL_3509
Experiment 33 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 5000.00 ng/mL High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description
The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
References
Ref 1 Phase I study of anti-epidermal growth factor receptor antibody-drug conjugate serclutamab talirine: Safety, pharmacokinetics, and antitumor activity in advanced glioblastoma. Neurooncol Adv. 2022 Dec 21;5(1):vdac183.
Ref 2 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 3 A Phase 1 Study Evaluating the Safety, Pharmacokinetics, and Anti-tumor Activity of ABBV-321 in Subjects With Advanced Solid Tumors Associated With Overexpression of the Epidermal Growth Factor Receptor (EGFR)
Ref 4 Targeting Multiple EGFR-expressing Tumors with a Highly Potent Tumor-selective Antibody-Drug Conjugate. Mol Cancer Ther. 2020 Oct;19(10):2117-2125.
Ref 5 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.
Ref 6 A Phase 1b Dose-escalation Study of SGN-CD33A in Combination With Standard-of-care for Patients With Newly Diagnosed Acute Myeloid Leukemia, NCT02326584
Ref 7 A Randomized, Double-blind Phase 3 Study of Vadastuximab Talirine (SGN-CD33A) Versus Placebo in Combination With Azacitidine or Decitabine in the Treatment of Older Patients With Newly Diagnosed Acute Myeloid Leukemia (AML), NCT02785900
Ref 8 A phase 1 trial of vadastuximab talirine as monotherapy in patients with CD33-positive acute myeloid leukemia. Blood. 2018 Jan 25;131(4):387-396.
Ref 9 A phase 1 trial of vadastuximab talirine combined with hypomethylating agents in patients with CD33-positive AML. Blood. 2018 Sep 13;132(11):1125-1133.
Ref 10 A Phase 1/2 Study of Vadastuximab Talirine Administered in Sequence With Allogeneic Hematopoietic Stem Cell Transplant in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML), NCT02614560
Ref 11 A Phase 1 Trial of SGN-CD33A in Patients With CD33-positive Acute Myeloid Leukemia, NCT01902329
Ref 12 SGN-CD33A: a novel CD33-targeting antibody-drug conjugate using a pyrrolobenzodiazepine dimer is active in models of drug-resistant AML. Blood. 2013 Aug 22;122(8):1455-63.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.