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norelgestromin
- Development stage
- Phase 4
- Lead developer
- Johnson & Johnson
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Transdermal
01
Overview
Norelgestromin is a synthetic progestin used primarily as a hormonal contraceptive in combination with ethinyl estradiol. It is the active metabolite of norgestimate and acts as the main progestational component in transdermal contraceptive patches such as Evra and Xulane. Norelgestromin works by suppressing gonadotropins to inhibit ovulation, thickening cervical mucus to impede sperm penetration, and altering the endometrium to reduce the likelihood of implantation. It exhibits high affinity for progesterone receptors with minimal androgenic activity compared to related compounds[3][4][5][8]. The drug may also be used in menopausal hormone therapy and has been investigated for potential use in breast cancer treatment[3].
- Brand names
- EvraOrtho EvraXulaneZafemy
- Other names
- norelgestromine
02
Targets
ESR1 (ERα)PR (Progesterone receptor)
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