Drug intelligence / Profile preview

disitamab vedotin + tislelizumab + capecitabine

Development stage
Phase 2
Lead developer
RemeGen
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination therapy consisting of three agents: - **Disitamab vedotin** is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). It consists of a humanized anti-HER2 monoclonal antibody linked to the cytotoxic agent monomethyl auristatin E (MMAE) via a cleavable peptide linker. Disitamab vedotin binds to HER2-expressing tumor cells, is internalized, and releases MMAE intracellularly, leading to microtubule disruption and cell death[8][10]. - **Tislelizumab** is a monoclonal antibody that targets programmed cell death protein 1 (PD-1), acting as an immune checkpoint inhibitor. By blocking PD-1, it enhances T-cell mediated immune responses against tumor cells. - **Capecitabine** is an oral prodrug that is enzymatically converted to 5-fluorouracil (5-FU) in the body. 5-FU inhibits thymidylate synthase, disrupting DNA synthesis and exerting antitumor effects. The combination aims to leverage targeted cytotoxicity from disitamab vedotin, immune activation from tislelizumab, and chemotherapeutic effects from capecitabine for synergistic antitumor activity. This regimen has been studied in advanced gastric cancer with HER2 overexpression or low expression[1][7].

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)

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