Drug intelligence / Profile preview

5-fluorouracil + mitoxantrone + prednimustine

Development stage
Unknown
Lead developer
Merck
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous (mitoxantrone, Fluorouracil), Oral (prednimustine)
01

Overview

This is a combination chemotherapy regimen consisting of three agents: - **5-fluorouracil** (a pyrimidine analog antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis), - **Mitoxantrone** (a synthetic anthracenedione that intercalates into DNA and inhibits topoisomerase II, leading to DNA strand breaks and apoptosis), - **Prednimustine** (an alkylating agent combining prednisolone and chlorambucil, exerting cytotoxic effects through DNA cross-linking as well as glucocorticoid activity). The combination has been studied primarily for the treatment of advanced breast cancer. In clinical trials, this regimen demonstrated a response rate of approximately 45% in patients with advanced breast cancer, including those who had failed prior chemotherapy. The main dose-limiting toxicities were leukopenia and thrombocytopenia; other common side effects included nausea, vomiting, and alopecia[1]. The PMF regimen is considered an active but relatively toxic option for advanced breast cancer.

Other names
PMF regimen
02

Targets

TOP2A (DNA topoisomerase II)TS (Thymidylate synthase)DNAGR (Glucocorticoid receptor)

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