Drug intelligence / Profile preview

trastuzumab rezetecan + fluorouracil

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

Overview

SHR-A1811 + fluorouracil is an investigational combination therapy pairing the anti-HER2 antibody-drug conjugate (ADC) SHR-A1811 (trastuzumab rezetecan) with the antimetabolite chemotherapy agent fluorouracil (5-FU). SHR-A1811 is composed of a humanized anti-HER2 IgG1 monoclonal antibody (trastuzumab) conjugated to a topoisomerase I inhibitor payload (SHR9265, an exatecan derivative) via a cleavable tetrapeptide-based linker, with a drug-to-antibody ratio (DAR) of approximately 5.7. Fluorouracil is a small molecule that acts as a thymidylate synthase inhibitor, disrupting DNA synthesis and repair. This combination is being developed by Suzhou Suncadia Biopharmaceuticals (a subsidiary of Hengrui Pharma) and is currently in Phase Ib/II clinical trials for the treatment of HER2-expressing advanced or metastatic gastric adenocarcinoma and gastroesophageal junction (GEJ) adenocarcinoma.

Other names
SHR-A1811 plus fluorouracilSHR-A-1811 plus fluorouracilSHR-A 1811 plus fluorouracil
02

Targets

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

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