Drug intelligence / Profile preview

ethinylestradiol + norethisterone

Development stage
Phase 3
Lead developer
Zeria Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

ZO-Y49 is an orally administered low-dose estrogen/progestin (LEP) combination therapy being developed by Zeria Pharmaceutical for the treatment of dysmenorrhea. It consists of the synthetic estrogen ethinylestradiol and the progestin norethisterone. The drug's mechanism of action involves the suppression of the hypothalamic-pituitary-ovarian axis, which inhibits ovulation and reduces the proliferation of the endometrial lining. This reduction in endometrial tissue leads to a decrease in the synthesis of prostaglandins, the primary mediators of uterine contractions and pain associated with dysmenorrhea. As of 2024, ZO-Y49 is in Phase 3 clinical development in Japan, where it is being evaluated for efficacy and safety in female outpatients with dysmenorrhea.

Other names
norethisterone / ethinylestradiolethinylestradiol / norethisterone
02

Targets

AR (Adrenergic receptors)ESR1 (ERα)ESR2 (ERβ)GPER1 (G protein-coupled estrogen receptor 1)GR (Glucocorticoid receptor)mPR (Membrane progesterone receptors)MR (Mineralocorticoid receptor)PR-A (Progesterone Receptor A)RB1 (Retinoblastoma-associated Protein)SHBG (Sex hormone-binding globulin)PR (Progesterone receptor)

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