Drug intelligence / Profile preview

5-fluorouracil + folinic acid + mitoxantrone + prednisone

Development stage
Preclinical
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination chemotherapy regimen consisting of four drugs: - **5-fluorouracil** (5-FU): an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and leading to cell death, primarily in rapidly dividing cancer cells. - **Folinic acid** (leucovorin): a reduced form of folic acid that enhances the binding of 5-FU to thymidylate synthase, increasing its cytotoxic effect. Folinic acid itself is not cytotoxic but potentiates the action of 5-FU[2][3]. - **Mitoxantrone**: an anthracenedione antineoplastic agent that intercalates into DNA and inhibits topoisomerase II, resulting in inhibition of DNA replication and repair. It also has immunosuppressive properties[8]. - **Prednisone**: a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressive effects; it is commonly used as part of palliative regimens for hormone-refractory prostate cancer when combined with mitoxantrone[8]. This specific four-drug combination does not have a widely recognized brand or protocol name but represents an intensive multi-agent chemotherapy approach potentially used for advanced cancers such as metastatic prostate cancer or other solid tumors where each component has demonstrated efficacy either alone or in smaller combinations.

02

Targets

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

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