Drug intelligence / Profile preview

trastuzumab + fluoropyrimidine + cisplatin

Development stage
Unknown
Lead developer
Genentech
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

A combination drug regimen consisting of **trastuzumab** (a monoclonal antibody targeting HER2), a **fluoropyrimidine** (such as 5-fluorouracil, capecitabine, or S-1, which are small molecule antimetabolites inhibiting DNA synthesis), and **cisplatin** (a platinum-based chemotherapeutic agent causing DNA crosslinking). This regimen is primarily used as a first-line therapy for **HER2-positive advanced gastric and gastroesophageal junction (GEJ) cancers**. Trastuzumab blocks the human epidermal growth factor receptor 2 (HER2/ERBB2), inhibiting proliferation of tumor cells that overexpress this target. Fluoropyrimidines inhibit thymidylate synthase, interfering with DNA replication. Cisplatin forms DNA adducts, promoting apoptosis in rapidly dividing cells. The combination enhances cytotoxic activity and survival outcomes compared to chemotherapy alone in this molecular subgroup[1][3][5].

Other names
trastuzumab + 5-fluorouracil + cisplatintrastuzumab + capecitabine + cisplatintrastuzumab + S-1 + cisplatin
02

Targets

DNATS (Thymidylate synthase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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