Drug intelligence / Profile preview

erlotinib + pemetrexed

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

Overview

Erlotinib + pemetrexed is a combination therapy consisting of two small molecule drugs used primarily in the treatment of advanced non-small cell lung cancer (NSCLC). Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR-mediated signaling pathways, thereby inhibiting tumor cell proliferation and survival. Pemetrexed is a multitargeted antifolate chemotherapy agent that disrupts folate-dependent metabolic processes essential for DNA synthesis by inhibiting enzymes such as thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT). The combination has demonstrated synergistic antitumor activity in preclinical models and clinical trials, improving progression-free survival compared to either agent alone in NSCLC patients. However, the combination also increases the risk of adverse effects such as rash, diarrhea, fatigue, myelosuppression, and anemia[1][3][4][5].

Other names
erlotinib and pemetrexedpemetrexed and erlotinib
02

Targets

DHFR (Dihydrofolate reductase)GART (GAR transformylase)TS (Thymidylate synthase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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