Drug intelligence / Profile preview

carboplatin + cisplatin + pemetrexed + zipalertinib

Development stage
Unknown
Lead developer
Taiho Oncology
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination chemotherapy and targeted therapy regimen for the treatment of advanced non-small cell lung cancer (NSCLC), particularly in patients with specific EGFR mutations such as exon 20 insertions. The regimen combines two platinum-based chemotherapies (carboplatin and cisplatin), an antifolate antimetabolite (pemetrexed), and a novel EGFR tyrosine kinase inhibitor (zipalertinib). Carboplatin and cisplatin are both DNA cross-linking agents that induce apoptosis in rapidly dividing cells, while pemetrexed inhibits enzymes involved in folate metabolism, disrupting DNA synthesis. Zipalertinib is an investigational, orally available, irreversible EGFR-TKI designed to target uncommon or resistant EGFR mutations[7][9][10]. This combination aims to maximize antitumor efficacy by leveraging both cytotoxic chemotherapy and targeted inhibition of oncogenic signaling pathways.

02

Targets

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

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