Drug intelligence / Profile preview

carboplatin + cisplatin + pemetrexed

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of three cytotoxic agents: carboplatin, cisplatin, and pemetrexed. All three are small molecule chemotherapeutic drugs used primarily in the treatment of non-squamous non-small cell lung cancer (NSCLC) and malignant pleural mesothelioma. Pemetrexed is a multitargeted antifolate that inhibits enzymes involved in folate metabolism (thymidylate synthase, dihydrofolate reductase, glycinamide ribonucleotide formyl transferase), thereby blocking DNA and RNA synthesis[1][6]. Cisplatin and carboplatin are platinum-based agents that cause DNA crosslinking and inhibit DNA replication and transcription, leading to apoptosis[1][4]. This triple combination is not standard; most clinical protocols use either cisplatin or carboplatin with pemetrexed rather than both platinum agents together. However, all three have been studied individually or as doublets for advanced NSCLC or mesothelioma[1][4][5].

02

Targets

DNAGART (GAR transformylase)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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