Drug intelligence / Profile preview

mitoxantrone + tegafur

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Mitoxantrone + tegafur is a combination regimen used in oncology, particularly investigated for the treatment of metastatic breast cancer. Mitoxantrone is an anthracenedione antineoplastic agent that intercalates into DNA and inhibits topoisomerase II, leading to DNA strand breaks and inhibition of cell replication. Tegafur is an oral prodrug of 5-fluorouracil (5-FU), which acts as an antimetabolite by inhibiting thymidylate synthase, thereby disrupting DNA synthesis in rapidly dividing cells. The combination has been studied with folinic acid (leucovorin) as a biochemical modulator to enhance the efficacy of tegafur. Clinical trials have shown this regimen can achieve significant response rates in patients with metastatic breast cancer, though toxicity such as gastrointestinal side effects may occur[1][2][3].

02

Targets

H3 (Histone H3.2)TOP2A (DNA topoisomerase II)TS (Thymidylate synthase)DNA

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