Drug intelligence / Profile preview

trastuzumab deruxtecan + pembrolizumab + capecitabine

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

Overview

This is a **combination regimen** consisting of trastuzumab deruxtecan (an antibody-drug conjugate targeting HER2), pembrolizumab (a PD-1 immune checkpoint inhibitor), and capecitabine (an oral prodrug of 5-fluorouracil, an antimetabolite chemotherapy). - **Trastuzumab deruxtecan** is an antibody-drug conjugate wherein a humanized anti-HER2 monoclonal antibody is linked to a topoisomerase I inhibitor (deruxtecan). It binds to HER2-overexpressing cells, delivers the payload inside the cancer cell, and induces cytotoxic DNA damage. - **Pembrolizumab** is a monoclonal antibody inhibitor of programmed death-1 (PD-1), releasing the immune system inhibition on cytotoxic T cells, thereby enabling immune-mediated tumor destruction. - **Capecitabine** is a prodrug converted to 5-fluorouracil in vivo, which inhibits DNA synthesis in rapidly dividing tumor cells. This triplet regimen is being developed and explored as a first-line therapy in advanced or metastatic HER2-positive gastric, gastroesophageal junction, or esophageal adenocarcinoma, and is being studied for efficacy and safety in clinical trials, particularly the DESTINY-Gastric03 trial[1][3][5]. Developers are evaluating the combination due to potential synergistic antitumor effects and manageable toxicity when using adjusted doses.

Other names
trastuzumab deruxtecan + pembrolizumab + capecitabine
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)PDCD1 (Programmed cell death protein 1 receptor)TOP1 (DNA Topoisomerase I)DNA

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