Drug intelligence / Profile preview

disitamab vedotin + toripalimab + trastuzumab

Development stage
Unknown
Lead developer
RemeGen
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

disitamab vedotin + toripalimab + trastuzumab is a combination regimen consisting of three drugs: - **disitamab vedotin**: an antibody-drug conjugate (ADC) targeting HER2. It uses a humanized anti-HER2 antibody (disitamab; hertuzumab) conjugated via a valine-citrulline linker to the cytotoxic payload monomethyl auristatin E (MMAE), which inhibits microtubule polymerization, leading to cancer cell death[5]. - **toripalimab**: a monoclonal antibody acting as an immune checkpoint inhibitor that binds to PD-1 on T cells, thereby blocking the interaction between PD-1 and its ligands, enhancing immune response against cancer cells[1]. - **trastuzumab**: a monoclonal antibody targeting HER2, leading to inhibition of signaling pathways, antibody-dependent cellular cytotoxicity, and cell cycle arrest in HER2-overexpressing tumors[5]. This triplet regimen is primarily under evaluation as a first-line therapy for patients with locally advanced or metastatic gastric or gastroesophageal junction (G/GEJ) adenocarcinomas expressing HER2, either highly or at median/low levels. The combination offers superior objective response rates and progression-free survival compared to regimens omitting one of the targeted agents or replacing one with chemotherapy[1][2][4].

02

Targets

PDCD1 (Programmed cell death protein 1 receptor)TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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