Drug intelligence / Profile preview

itraconazole + pemetrexed

Development stage
Phase 2
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Itraconazole + pemetrexed is a combination of two pharmaceutical agents used in investigational settings for cancer therapy, particularly in advanced or recurrent non-small cell lung cancer (NSCLC). Itraconazole is an oral antifungal agent that has demonstrated antiangiogenic and potential anticancer properties by inhibiting endothelial cell proliferation, migration, and tube formation. It also inhibits the Hedgehog signaling pathway and can reverse multidrug resistance by blocking efflux pumps such as P-glycoprotein. Pemetrexed is a cytotoxic antifolate chemotherapy agent that inhibits several folate-dependent enzymes involved in nucleotide synthesis, leading to inhibition of DNA replication and cell death. The combination aims to enhance the efficacy of chemotherapy through both direct cytotoxic effects (pemetrexed) and modulation of tumor microenvironment/angiogenesis (itraconazole), as well as overcoming drug resistance mechanisms[1][2][3][5].

02

Targets

ABCB1 (P-glycoprotein)DHFR (Dihydrofolate reductase)GART (GAR transformylase)NPC1 (Niemann-Pick C1 protein binding inhibition)TS (Thymidylate synthase)

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