Drug intelligence / Profile preview

EGFR-TKI + pemetrexed + carboplatin

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

Overview

This is a combination regimen consisting of an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) with the chemotherapeutic agents pemetrexed and carboplatin. The EGFR-TKIs used in this context include first-generation (e.g., gefitinib), second-generation (e.g., afatinib), or third-generation (e.g., osimertinib) inhibitors. This combination is primarily used for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC) harboring activating EGFR mutations such as exon 19 deletions or L858R substitutions. The rationale for combining an EGFR-TKI with chemotherapy is to improve progression-free survival and overall survival compared to monotherapy by targeting both the driver mutation and rapidly dividing tumor cells[1][2][3]. Pemetrexed is an antifolate antimetabolite that inhibits folate-dependent enzymes involved in nucleotide synthesis, while carboplatin is a platinum-based agent that induces DNA crosslinking and apoptosis in cancer cells.

Other names
EGFR tyrosine kinase inhibitor plus pemetrexed and carboplatinEGFR-TKI plus PCgefitinib + pemetrexed + carboplatinafatinib + pemetrexed + carboplatinosimertinib + pemetrexed + carboplatin
02

Targets

DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)EGFR (Epidermal growth factor receptor)DNA

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