Drug intelligence / Profile preview

bortezomib + fluorouracil + leucovorin + oxaliplatin

Development stage
Unknown
Lead developer
Millennium Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

This is a combination chemotherapy regimen consisting of four agents: bortezomib, fluorouracil (5-FU), leucovorin (folinic acid), and oxaliplatin. Bortezomib is a reversible inhibitor of the 26S proteasome, leading to disruption of protein degradation and induction of apoptosis in cancer cells. Fluorouracil is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis. Leucovorin enhances the binding of fluorouracil to thymidylate synthase, increasing its cytotoxicity. Oxaliplatin is a platinum-based chemotherapeutic that forms DNA crosslinks and induces apoptosis. This combination has been investigated primarily for advanced or metastatic colorectal cancer, with early-phase studies showing partial responses and stable disease in some patients[1][2][8]. The regimen leverages synergistic mechanisms to enhance anti-tumor activity.

02

Targets

TS (Thymidylate synthase)DNAPSMB5 (Proteasome subunit beta Type-5)

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