Drug intelligence / Profile preview

melphalan + trifluridine + tipiracil + bevacizumab

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of four drugs: - **Melphalan** is an alkylating agent used primarily in the treatment of multiple myeloma and ovarian cancer. It works by cross-linking DNA strands, thereby inhibiting DNA and RNA synthesis and leading to cell death. - **Trifluridine** is a thymidine-based nucleoside analogue that incorporates into DNA after phosphorylation, causing dysfunction in DNA replication. - **Tipiracil** is a thymidine phosphorylase inhibitor that prevents the breakdown of trifluridine, increasing its bioavailability. - **Bevacizumab** is a monoclonal antibody targeting vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis (the formation of new blood vessels) required for tumor growth. The combination of trifluridine/tipiracil with bevacizumab has been approved for previously treated metastatic colorectal cancer and has shown improved overall survival compared to trifluridine/tipiracil alone[1][2][5][6]. Melphalan has been studied as part of investigational regimens in liver-dominant metastatic colorectal cancer, sometimes followed by consolidation therapy with trifluridine-tipiracil plus bevacizumab[8].

Brand names
Lonsurf
Other names
melphalantrifluridine and tipiracilTAS-102TAS102TAS 102bevacizumab
02

Targets

TYMP (Thymidine phosphorylase)VEGFA (Vascular endothelial growth factor A)DNATS (Thymidylate synthase)

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