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