Drug intelligence / Profile preview

icotinib + pemetrexed + cisplatin

Development stage
Unknown
Lead developer
Betta Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of three drugs—icotinib, pemetrexed, and cisplatin—used primarily in the treatment of non-small cell lung cancer (NSCLC), particularly in patients with EGFR mutations. - **Icotinib** is an oral small molecule tyrosine kinase inhibitor that selectively targets the epidermal growth factor receptor (EGFR), blocking its phosphorylation and downstream signaling pathways involved in tumor cell proliferation and survival. - **Pemetrexed** is a multi-targeted antifolate chemotherapy agent that inhibits several folate-dependent enzymes essential for DNA synthesis and cell replication, including thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase. - **Cisplatin** is a platinum-based chemotherapeutic agent that forms DNA crosslinks, leading to apoptosis of rapidly dividing cells. The combination leverages targeted therapy (icotinib) with cytotoxic chemotherapy (pemetrexed plus cisplatin) to improve clinical outcomes such as progression-free survival in advanced NSCLC patients[1][3][4]. This regimen may be used as first-line or adjuvant therapy depending on disease stage and molecular profile.

02

Targets

GART (GAR transformylase)DHFR (Dihydrofolate reductase)DNAEGFR T790M (Epidermal growth factor receptor T790M mutant)TS (Thymidylate synthase)

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