Drug intelligence / Profile preview

carboplatin + cisplatin + docetaxel + pemetrexed

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of four cytotoxic agents: carboplatin, cisplatin, docetaxel, and pemetrexed. Each drug has a distinct mechanism of action targeting cancer cell proliferation: - Carboplatin and cisplatin are platinum-based compounds that form DNA crosslinks, inhibiting DNA replication and transcription, ultimately leading to apoptosis. - Docetaxel is a taxane that stabilizes microtubules and prevents their depolymerization during cell division, resulting in mitotic arrest. - Pemetrexed is an antifolate agent that inhibits multiple enzymes involved in folate metabolism (thymidylate synthase, dihydrofolate reductase, glycinamide ribonucleotide formyl transferase), thereby blocking the synthesis of purine and pyrimidine nucleotides required for DNA and RNA synthesis[1][2]. This combination has been studied primarily in advanced or metastatic non-small cell lung cancer (NSCLC) as well as other solid tumors. The rationale for combining these agents is to exploit their complementary mechanisms for enhanced antitumor efficacy.

02

Targets

DNADHFR (Dihydrofolate reductase)GART (GAR transformylase)TS (Thymidylate synthase)TUBB (Tubulin (alpha and beta subunits))

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