Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0RYBMQ
ADC Name	SHR-A1201
Synonyms	SHR A1201; SHRA1201 Click to Show/Hide
Organization	Jiangsu Hengrui Pharmaceuticals Co., Ltd.; Shanghai Hengrui Pharmaceutical Co., Ltd.
Drug Status	Phase 1
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Phase 1
Drug-to-Antibody Ratio	3.6
Structure
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		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

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	Undisclosed	Phase 1	This phase 1 study investigated the safety, tolerability and pharmacokinetics of SHR-A1201 in patients with human epidermal growth factor receptor 2-positive advanced breast cancer. This phase 1 study enrolled patients in a traditional 3 + 3 dose-escalation design to receive a single dose of SHR-A1201 (1.20 mg/kg, 2.40 mg/kg, 3.60 mg/kg or 4.8 mg/kg). The observation period of dose-limiting toxicity (DLT) was 21 days. A total of 12 patients were enrolled and received SHR-A1201. Click to Show/Hide

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]
Patients Enrolled	HER2-positive locally advanced or metastatic breast cancer (positivity for HER2 was defined as a score of 2+ in immunohistochemical analysis and a positive result in fluorescence in situ hybridization or a score of 3+ in immunohistochemical analysis), the standard treatment was invalid or there was no effective standard treatment plan, the Eastern Cooperative Oncology Group performance status score was 0-1. Click to Show/Hide
Administration Dosage	4 dose-escalation sequences, 1.20 mg/kg, 2.40 mg/kg, 3.60 mg/kg and 4.80 mg/kg, once every 21days, as a 90-min intravenous infusion.

References

Ref 1	Safety, tolerability, pharmacokinetics and immunogenicity of an antibody-drug conjugate (SHR-A1201) in patients with HER2-positive advanced breast cancer: an open, phase I dose-escalation study. Anticancer Drugs. 2023 Jul 1;34(6):763-774.