Drug intelligence / Profile preview

trastuzumab rezetecan + everolimus

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

SHR-A1811 + eve is a combination therapy comprising trastuzumab rezetecan (SHR-A1811) and everolimus. Trastuzumab rezetecan is a next-generation antibody-drug conjugate (ADC) targeting HER2, developed by Jiangsu Hengrui Pharmaceuticals. It consists of a humanized anti-HER2 monoclonal antibody (trastuzumab) conjugated via a cleavable tetrapeptide linker to a topoisomerase I inhibitor payload (SHR169265), with a drug-to-antibody ratio (DAR) of 6. Everolimus is a small-molecule inhibitor of the mechanistic target of rapamycin (mTOR). This combination is currently being investigated in a Phase III clinical trial sponsored by Fudan University for the treatment of patients with the Luminal Androgen Receptor (LAR) subtype of triple-negative breast cancer (TNBC), a molecularly distinct subtype that may exhibit low HER2 expression.

Other names
trastuzumab rezetecan + everolimus
02

Targets

TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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