Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ATULB
ADC Name
Laprituximab emtansine
Synonyms
J2898A-SMCC-DM1; IMGN-289; IMGN 289; IMGN289
   Click to Show/Hide
Organization
ImmunoGen, Inc.
Drug Status
Terminated in phase 1
Indication
In total 1 Indication(s)
Solid tumors [ICD11:2A00-2A0Z|2B50-2F9Z]
Terminated in phase 1
Drug-to-Antibody Ratio
3.5
Structure
Antibody Name
Laprituximab
  Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
  Antigen Info 
Payload Name
Mertansine DM1
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
  Linker Info 
Conjugate Type
Random conjugation through nucleophilic lysines.
Combination Type
Emtansine
Puchem SID
472407943 , 381127774
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
Undisclosed  NCT01963715
Phase 1
A phase 1, multi-center, open-label study of IMGN289 administered intravenously in adult patients with EGFR-positive solid tumors.
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) 
58.3
%
FaDu cells
Hypopharyngeal squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
83.3
%
HSC-2 cells
Oral cavity squamous cell carcinoma
Minimal Effective Dose (MED) 
1
mg/kg
FaDu cells
Hypopharyngeal squamous cell carcinoma
Minimal Effective Dose (MED) 
2.5
mg/kg
HSC-2 cells
Oral cavity squamous cell carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.25
nM
HNSCC cells
Head and neck squamous cell carcinoma
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]
Related Clinical Trial
NCT Number NCT01963715  Clinical Status Phase 1
Clinical Description A phase 1, multi-center, open-label study of IMGN289 administered intravenously in adult patients with EGFR-positive solid tumors.
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 [2]
Efficacy Data Tumor Growth Inhibition value (TGI) 58.30% High EGFR expression (EGFR+++/++)
Method Description
The cytotoxic activity of IMGN289 was evaluated against a panel of SCCHN cell lines in vitro. Immunodeficient mice bearing established subcutaneous xenograft tumors were treated with a single intravenous injection of IMGN289 at 1,2.5 or 5.0 mg/kg (based on antibody concentration). IMGN289 dose was 5 mg/kg administered as a single injection.
In Vivo Model Head and neck squamous cell carcinomas CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) 83.30% High EGFR expression (EGFR+++/++)
Method Description
The cytotoxic activity of IMGN289 was evaluated against a panel of SCCHN cell lines in vitro. Immunodeficient mice bearing established subcutaneous xenograft tumors were treated with a single intravenous injection of IMGN289 at 1,2.5 or 5.0 mg/kg (based on antibody concentration). IMGN289 dose was 5 mg/kg administered as a single injection.
In Vivo Model Head and neck squamous cell carcinomas CDX model
In Vitro Model Oral cavity squamous cell carcinoma HSC-2 cells CVCL_1287
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Minimal Effective Dose (MED) 1.00 mg/kg High EGFR expression (EGFR+++/++)
Method Description
The cytotoxic activity of IMGN289 was evaluated against a panel of SCCHN cell lines in vitro. Immunodeficient mice bearing established subcutaneous xenograft tumors were treated with a single intravenous injection of IMGN289 at 1,2.5 or 5.0 mg/kg (based on antibody concentration).
In Vivo Model Head and neck squamous cell carcinomas CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Minimal Effective Dose (MED) 2.50 mg/kg High EGFR expression (EGFR+++/++)
Method Description
The cytotoxic activity of IMGN289 was evaluated against a panel of SCCHN cell lines in vitro. Immunodeficient mice bearing established subcutaneous xenograft tumors were treated with a single intravenous injection of IMGN289 at 1,2.5 or 5.0 mg/kg (based on antibody concentration).
In Vivo Model Head and neck squamous cell carcinomas CDX model
In Vitro Model Oral cavity squamous cell carcinoma HSC-2 cells CVCL_1287
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.25 nM High EGFR expression (EGFR+++/++)
Method Description
Effects of IMGN289 on clonogenicity and proliferation were tested in HNSCC cell lines with varying cetuximab and gefitinib sensitivities.
In Vitro Model Head and neck squamous cell carcinoma HNSCC cells Homo sapiens
References
Ref 1 A Phase 1, Multi-center, Open-label Study of IMGN289 Administered Intravenously in Adult Patients With EGFR-positive Solid Tumors
Ref 2 Preclinical evaluation of IMGN289, an anti-EGFR antibody-maytansinoid conjugate for the treatment of squamous cell carcinoma of the head and neck.
Ref 3 Antitumor effect of IMGN289, an anti-EGFR antibody-drug conjugate (ADC), in preclinical models of head and neck squamous cell carcinomas (HNSCC). Journal of Clinical Oncology 32, no. 15_suppl.

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