Drug intelligence / Profile preview

anastrozole + tegafur-uracil

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Anastrozole + tegafur-uracil is a combination therapy consisting of anastrozole, a non-steroidal aromatase inhibitor, and tegafur-uracil (UFT), an oral prodrug formulation that delivers 5-fluorouracil (5-FU) via metabolic conversion. Anastrozole inhibits the enzyme aromatase, thereby reducing estrogen synthesis and limiting the growth stimulus for estrogen receptor-positive breast cancer cells. Tegafur is converted in vivo to 5-FU; uracil inhibits dihydropyrimidine dehydrogenase to increase 5-FU bioavailability and prolong its antitumor effect. The combination has been studied as neoadjuvant therapy for postmenopausal women with ER-positive, HER2-negative breast cancer. Clinical trials showed greater tumor shrinkage compared to anastrozole alone but also increased risk of liver dysfunction[1][2][4].

Other names
anastrozole/UFTanastrozole plus UFTanastrozole plus tegafur/uracil
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)CYP19A1 (Aromatase)

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