Drug intelligence / Profile preview

firmonertinib + carboplatin + cisplatin + pemetrexed

Development stage
Unknown
Lead developer
ArriVent BioPharma
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of four drugs: firmonertinib, carboplatin, cisplatin, and pemetrexed. Firmonertinib (AST2818; formerly furmonertinib) is an oral, highly brain-penetrant small molecule inhibitor targeting the epidermal growth factor receptor (EGFR), with broad activity against various EGFR mutations including P-loop and αC-helix compressing (PACC) mutations and exon 20 insertions. It has demonstrated strong antitumor activity in non-small cell lung cancer (NSCLC), particularly in patients with uncommon EGFR mutations[1][2][5]. Carboplatin and cisplatin are platinum-based chemotherapeutic agents that induce DNA crosslinking leading to apoptosis of rapidly dividing cells. Pemetrexed is an antifolate chemotherapy agent that inhibits multiple folate-dependent enzymes involved in nucleotide synthesis, thereby blocking DNA replication and cell division. This combination targets NSCLC through both targeted inhibition of mutant EGFR signaling pathways (firmonertinib) and cytotoxic effects on tumor cells via DNA damage and inhibition of nucleotide synthesis (carboplatin, cisplatin, pemetrexed).

Brand names
Ivesa
Other names
firmonertinibalflutinib
02

Targets

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

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