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leflutrozole + levonorgestrel + ethinyl estradiol
- Development stage
- Unknown
- Lead developer
- Mereo BioPharma
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
leflutrozole + levonorgestrel + ethinyl estradiol is a drug combination consisting of the aromatase inhibitor leflutrozole (BGS649) and a combined oral contraceptive (COC) containing the progestin levonorgestrel and the estrogen ethinyl estradiol. Leflutrozole, originally developed by Novartis and later licensed to Mereo BioPharma, is a potent, non-steroidal aromatase inhibitor that blocks the conversion of testosterone to estradiol; it has been primarily investigated for the treatment of male obese subjects with hypogonadotropic hypogonadism to restore testosterone levels. The specific combination with levonorgestrel and ethinyl estradiol was evaluated in Phase 1 clinical trials to assess the potential for drug-drug interactions, specifically to determine if leflutrozole alters the pharmacokinetics of the contraceptive components in healthy female subjects.
- Other names
- BGS649 + levonorgestrel + ethinyl estradiol
02
Targets
ESR2 (ERβ)ESR1 (ERα)PR (Progesterone receptor)CYP19A1 (Aromatase)
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