Drug intelligence / Profile preview

gemcitabine + mitoxantrone

Development stage
Phase 2
Lead developer
Eli Lilly
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Gemcitabine + mitoxantrone is a combination chemotherapy regimen consisting of two small molecule antineoplastic agents. Gemcitabine is a nucleoside analog that inhibits DNA synthesis by incorporation into DNA and inhibition of ribonucleotide reductase, leading to cell cycle arrest and apoptosis. Mitoxantrone is an anthracenedione that intercalates into DNA, causing crosslinks and strand breaks, and inhibits topoisomerase II, resulting in cytotoxicity. This combination has been studied as a treatment for metastatic breast cancer (as second- or third-line therapy) and for relapsed or refractory acute leukemia. The regimen has demonstrated objective response rates in these settings with manageable toxicity profiles[1][4].

Other names
gemcitabine/mitoxantronegemcitabine and mitoxantronegemcitabine hydrochloride + mitoxantrone hydrochloride
02

Targets

DNADNA polymerase familyRNR (Ribonucleotide reductase)TOP2A (DNA topoisomerase II)

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