Drug intelligence / Profile preview

asunaprevir + ethinyl estradiol + norgestimate

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

**Asunaprevir + ethinyl estradiol + norgestimate** is a combination of three drugs: asunaprevir, a direct-acting antiviral typically used in hepatitis C virus (HCV) treatment as an NS3 protease inhibitor, and ethinyl estradiol + norgestimate, which together form a hormonal contraceptive commonly used as birth control and for treating moderate acne in women. - **Mechanism of Action:** - **Asunaprevir** inhibits HCV replication by blocking the NS3/4A protease involved in viral polyprotein processing. - **Ethinyl estradiol + norgestimate** act as contraceptives by suppressing ovulation via negative feedback on the hypothalamic-pituitary-ovarian axis, modifying cervical mucus to prevent sperm penetration, and changing the endometrium to hinder implantation[1][2][5]. - **Drug interaction:** Co-administration may decrease serum concentrations of the active metabolites of norgestimate, reducing the contraceptive’s effectiveness; higher estrogen contraceptive regimens may be recommended due to this interaction[1][3].

02

Targets

NS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)PR (Progesterone receptor)ER (Estrogen receptor)

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