Drug intelligence / Profile preview

ethinyl estradiol + norgestimate + efavirenz

Development stage
Phase 1
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral
01

Overview

Ethinyl estradiol and norgestimate is a combination oral contraceptive containing a synthetic estrogen (ethinyl estradiol) and a progestin (norgestimate), used primarily to prevent pregnancy and also indicated for the treatment of moderate acne in females who desire contraception. The mechanism of action involves suppression of ovulation by inhibiting gonadotropins, thickening cervical mucus to impede sperm penetration, and altering the endometrial lining to reduce the likelihood of implantation. Efavirenz is an antiretroviral drug (non-nucleoside reverse transcriptase inhibitor) used in HIV therapy. When coadministered with ethinyl estradiol/norgestimate, efavirenz significantly reduces plasma concentrations of the progestin component (norgestimate metabolites), potentially decreasing contraceptive efficacy; it does not significantly affect ethinyl estradiol levels. This combination is not recommended for reliable contraception due to this interaction[1][6][8].

Brand names
TriNessa 28TriNessa28TriNessa-28
02

Targets

ER (Estrogen receptor)Human immunodeficiency virus type 1 reverse transcriptasePR (Progesterone receptor)

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