Drug intelligence / Profile preview

idarubicin + levo-folinate + tegafur

Development stage
Unknown
Lead developer
Pfizer
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

The combination of idarubicin, levo-folinate, and tegafur is an oral chemotherapy regimen that has been studied for the treatment of advanced breast cancer, particularly in patients who had been previously treated. A Phase I-II study involving 30 pretreated advanced breast cancer patients evaluated this combination. Patients received oral idarubicin (12 mg/m²/day for 3 days every 4 weeks) along with tegafur and levo-folinate. The maximum tolerated doses were established at 200 mg/m² (days 1-30) for tegafur and 50 mg (days 1-30) for levo-folinate. ## Efficacy and Safety * Among 27 evaluable patients, 2 partial remissions (7%) and 12 stable disease cases (45%) were observed. * Median time to progression was 4 months (range 2-14 months). * Median survival was 10 months (range 3-30 months). * Patients received a median of 4 treatment cycles (range 1-13). * Toxicity primarily included gastrointestinal side effects, with minimal hematologic toxicity. ## Components * **Idarubicin**: An antineoplastic medication belonging to the anthracycline class. * **Tegafur**: An oral fluoropyrimidine that acts as a prodrug of 5-fluorouracil (5-FU), an antimetabolite. * **Levo-folinate**: A folate analog that enhances the efficacy of fluoropyrimidines like tegafur by stabilizing the binding of 5-FU to its target enzyme.

02

Targets

TOP2A (DNA topoisomerase II)TS (Thymidylate synthase)

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