[Development of a novel aromatase inhibitor, anastrozole (Arimidex)--its basic and clinical studies].

TL;DRAbstract

Anastrozole (JAN), developed by Zeneca UK (presently AstraZeneca UK), is a new aromatase inhibitor which belongs to triazole. Anastrozole shows selective aromatase inhibition and negligible effects on other steroid hormone biosyntheses. The daily dose of 3 mg/kg anastrozole inhibited the growth of DMBA mammary tumours significantly. Anastrozole inhibited the tumor growth at 5 micrograms/mouse/day (s.c.) in androstenedione-treated ovariectomized nude mice inoculated with MCF-7CA cells transfected with aromatase gene. In the Japanese Phase IIa study, the response rate was 27.8% (10/36) in the 0.5 mg group, and 38.2% (13/34) in the 1 mg group. The most common adverse drug reactions were leucopenia in the 0.5 mg group, and LDH increased and leucopenia in the 1 mg group. There were no early deaths, other serious adverse events, or adverse drug reactions of grade 3 or above in this trial; anastrozole was well tolerated. In the Japanese Phase IIb study, the response rates were 33.3% (117/351

Chat with Paper

AI Agents for this Paper