Drug intelligence / Profile preview

dulanermin + leucovorin + fluorouracil + irinotecan + bevacizumab

Development stage
Unknown
Lead developer
Genentech
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Recombinant Proteins and Enzymes, Small Molecules
Administration
Intravenous
01

Overview

**dulanermin + leucovorin + fluorouracil + irinotecan + bevacizumab** is a multi-agent chemotherapy regimen combining an investigational pro-apoptotic agent (dulanermin) with established colorectal cancer chemotherapy drugs (leucovorin, fluorouracil, irinotecan) and the VEGF-targeting monoclonal antibody bevacizumab. - **Dulanermin** is a recombinant human TRAIL (TNF-related apoptosis-inducing ligand) that induces apoptosis in cancer cells via death receptors. - **Leucovorin** (folinic acid) enhances the efficacy of fluorouracil by stabilizing its binding to thymidylate synthase. - **Fluorouracil** (5-FU) is a pyrimidine analog that inhibits thymidylate synthase, impairing DNA synthesis. - **Irinotecan** inhibits topoisomerase I, causing DNA strand breaks during replication. - **Bevacizumab** is a humanized monoclonal antibody that inhibits angiogenesis by binding vascular endothelial growth factor A (VEGF-A), preventing tumor vascularization[1][2][3][4][5][6]. This regimen is investigated primarily for advanced or metastatic colorectal cancer, leveraging multiple mechanisms: promotion of cancer cell apoptosis, inhibition of DNA synthesis and repair, and blockade of tumor angiogenesis.

02

Targets

TS (Thymidylate synthase)TNFRSF10B (DR5)TOP1 (DNA Topoisomerase I)VEGFA (Vascular endothelial growth factor A)TNFRSF10A (Death receptor 4)

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