Drug intelligence / Profile preview

S-1 + carboplatin + gefitinib

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Combination chemotherapy regimen consisting of three drugs used primarily as a first-line treatment for advanced non-small cell lung cancer (NSCLC) patients harboring activating epidermal growth factor receptor (EGFR) mutations. - **S-1** is an oral fluoropyrimidine derivative combining tegafur with two modulators, gimeracil and oteracil, which inhibits DNA synthesis in cancer cells by interfering with thymidylate synthase. - **Carboplatin** is a platinum-based chemotherapeutic agent that causes DNA crosslinking and damage leading to apoptosis of cancer cells. - **Gefitinib** is an orally active small molecule epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), blocking EGFR signaling pathways involved in tumor cell proliferation and survival. This triplet combination has shown efficacy and tolerability in phase II clinical trials, demonstrating improved progression-free survival and response rates compared to monotherapy or doublet regimens in EGFR-mutated NSCLC patients[1][2]. The regimen typically involves carboplatin administered intravenously on day 1, S-1 given orally days 1–14, and daily oral gefitinib continuously during cycles.

Other names
tegafur/gimeracil/oteracil (S-1)CBDCA (carboplatin)Iressa (gefitinib)
02

Targets

DNAEGFR (Epidermal growth factor receptor)TS (Thymidylate synthase)

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