Drug intelligence / Profile preview

axitinib + lomustine

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Axitinib + lomustine is a combination therapy investigated primarily for the treatment of recurrent glioblastoma (rGB). Axitinib is a small molecule tyrosine kinase inhibitor that selectively targets vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3), thereby inhibiting angiogenesis and tumor growth. Lomustine is an alkylating agent of the nitrosourea class that exerts its cytotoxic effects by causing DNA and RNA cross-linking and alkylation, leading to inhibition of cancer cell replication. The combination has been evaluated in phase II clinical trials for rGB but did not show significant improvement in survival compared to axitinib monotherapy. Both drugs are orally administered small molecules with distinct mechanisms targeting tumor proliferation and survival[1][2][3][4][5][6].

02

Targets

PDGFR (PDGFR family)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)DNA interstrand cross-link

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