Drug intelligence / Profile preview

cyclophosphamide + dofequidar + doxorubicin + fluorouracil

Development stage
Preclinical
Lead developer
Takeda
Modality
Small Molecules
Administration
Intravenous
01

Overview

A combination chemotherapy regimen consisting of cyclophosphamide, dofequidar, doxorubicin, and fluorouracil. This combination builds upon the established FAC/CAF regimen (fluorouracil, doxorubicin, cyclophosphamide) with the addition of dofequidar, a multidrug resistance-reversing agent. Dofequidar (MS-209) works by inhibiting P-glycoprotein and other drug efflux pumps, potentially enhancing the effectiveness of the chemotherapy drugs by preventing cancer cells from developing resistance. The standard components work through different mechanisms: cyclophosphamide is an alkylating agent that damages DNA, doxorubicin is an anthracycline that intercalates DNA and inhibits topoisomerase II, and fluorouracil is an antimetabolite that interferes with DNA and RNA synthesis.

02

Targets

ABCB1 (P-glycoprotein)TS (Thymidylate synthase)DNAMRP (Multidrug resistance-associated protein family)TOP2A (DNA topoisomerase II)

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