Drug intelligence / Profile preview

afatinib + pemetrexed

Development stage
Phase 1
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral (afatinib), Intravenous (pemetrexed)
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Overview

Afatinib + pemetrexed is a **combination regimen** used for the treatment of **EGFR mutation-positive non-small cell lung cancer (NSCLC)**, primarily after failure of first-line osimertinib therapy. **Afatinib** is an irreversible small-molecule inhibitor of the ErbB receptor family, targeting **EGFR (ErbB1)**, **HER2 (ErbB2)**, and **HER4 (ErbB4)**. It blocks downstream signaling pathways responsible for cell proliferation and survival. **Pemetrexed** is a multi-targeted antifolate chemotherapy agent that inhibits several enzymes involved in folate metabolism and DNA synthesis. The combination aims to overcome acquired resistance to osimertinib, and studies have shown that this regimen yields promising disease control and response rates with a manageable safety profile in EGFR-mutant NSCLC patients refractory to osimertinib[1][2][4][7].

02

Targets

ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)DHFR (Dihydrofolate reductase)EGFR (Epidermal growth factor receptor)GART (GAR transformylase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)TS (Thymidylate synthase)

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