Drug intelligence / Profile preview

KM257 + capecitabine

Development stage
Phase 1
Lead developer
Roche
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

KM257 + capecitabine is a combination therapy comprising a humanized monoclonal antibody and a cytotoxic antimetabolite. **KM257** is a monoclonal antibody designed to target **MUC1** (Mucin-1), a transmembrane glycoprotein that is frequently overexpressed and aberrantly glycosylated in various epithelial cancers, including gastric, colorectal, and breast cancers. By binding to the tandem repeat domain of MUC1, KM257 aims to inhibit tumor growth and potentially induce antibody-dependent cellular cytotoxicity (ADCC). **Capecitabine** is an orally administered prodrug of 5-fluorouracil (5-FU). It undergoes a three-step enzymatic conversion to 5-FU, with the final step occurring primarily in tumor tissues via thymidine phosphorylase. The resulting 5-FU inhibits thymidylate synthase, thereby disrupting DNA synthesis and inducing cell death. The combination is being investigated for its potential to provide synergistic anti-tumor activity in MUC1-positive advanced solid tumors.

Other names
KM-257 + capecitabineanti-MUC1 antibody + capecitabine
02

Targets

CD3 (T-cell surface glycoprotein CD3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)DNAMUC1 (Mucin-1 Antigen)

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