Drug intelligence / Profile preview

norgestimate

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

Overview

Norgestimate is a **synthetic progestin** (progestogen), mainly used in combination with ethinyl estradiol as an **oral contraceptive** and for the management of **acne vulgaris**. After oral administration, norgestimate is extensively metabolized to its active forms, primarily norelgestromin and norgestrel, which exert effects by binding to progesterone receptors in target tissues. Its main actions are suppression of ovulation, alteration of cervical mucus to inhibit sperm penetration, and modification of the endometrium to reduce implantation potential. Norgestimate was developed to provide effective hormonal contraception with improved tolerability[2][3][5].

Brand names
EstaryllaFemynorMiliMono-LinyahMononessaNymyoOrtho Tri-CyclenOrtho Tri-Cyclen LoPrevifemSprintecTri FemynorTri-LO-EstaryllaTri-LO-MarziaTri-LO-MiliTri-Lo-SprintecTri-EstaryllaTri-LinyahTri-MiliTri-NymyoTri-PrevifemTri-SprintecTri-VylibraTri-Vylibra LoTrinessaTrinessa LoVylibraOrtho-Cyclen
Other names
(+)-13-Ethyl-17-hydroxy-18,19-dinor-17α-pregn-4-en-20-yn-3-one oxime acetate(17α)-17-(Acetyloxy)-13-ethyl-18,19-dinorpregn-4-en-20-yn-3-one 3-oximed-13β-Ethyl-17α-ethynyl-17β-acetoxygon-4-en-3-one oximeDexnorgestrel AcetimeNorgestimatoNorgestimatum
02

Targets

ER (Estrogen receptor)AR (Adrenergic receptors)PR (Progesterone receptor)

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