Drug intelligence / Profile preview

carmustine + bevacizumab + irinotecan

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

This is a combination regimen of three drugs used primarily in the treatment of recurrent or progressive high-grade gliomas and glioblastoma multiforme. - **Carmustine** is an alkylating agent from the nitrosourea class that cross-links DNA and RNA strands to inhibit replication and transcription. - **Bevacizumab** is a recombinant humanized monoclonal antibody targeting vascular endothelial growth factor A (VEGF-A), thereby inhibiting angiogenesis by preventing VEGF-A from binding to its receptors VEGFR1 and VEGFR2 on endothelial cells[6]. - **Irinotecan** is a small molecule topoisomerase I inhibitor that prevents DNA unwinding necessary for replication and transcription[8]. The combination has been studied in patients with recurrent glioblastoma multiforme (GBM) or other high-grade gliomas who have failed prior therapies. The rationale for this regimen includes targeting tumor cell proliferation through cytotoxic mechanisms (carmustine/irinotecan) while simultaneously inhibiting tumor angiogenesis with bevacizumab[3][6]. This triple-drug therapy has been investigated in retrospective studies for efficacy and safety in these patient populations[3].

Brand names
AvastinGliadel
Other names
BCNUNSC 409962NSC409962NSC-409962rhuMAb-VEGFCPT-11CPT11CPT 11
02

Targets

TOP1 (DNA Topoisomerase I)DNAVEGFA (Vascular endothelial growth factor A)GSR (Glutathione reductase)

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