Drug intelligence / Profile preview

levonorgestrel + ethinylestradiol

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Loette Diario is a low-dose combined oral contraceptive (COC) containing the synthetic progestin levonorgestrel (100 mcg) and the synthetic estrogen ethinylestradiol (20 mcg). Marketed by Pfizer, it is provided in a 28-day 'Diario' (daily) format consisting of 21 active pink film-coated tablets and 7 white placebo tablets to ensure continuous daily administration. The drug's primary mechanism involves the suppression of ovulation by inhibiting the release of gonadotropins (LH and FSH) from the pituitary gland. Additionally, it increases the viscosity of cervical mucus to impede sperm transport and alters the endometrial lining to prevent implantation. While primarily indicated for contraception, Loette Diario is also used to manage conditions such as polycystic ovary syndrome (PCOS), acne, and dysmenorrhea. It has been utilized in Phase III clinical trials as a comparator arm to evaluate cardiometabolic health markers in adolescent girls with hyperinsulinemic ovarian androgen excess.

Brand names
Loette DiarioLoette
Other names
Levonorgestrel/Ethinylestradiol 100/20Combined oral contraceptive
02

Targets

RB1 (Retinoblastoma-associated Protein)PR-A (Progesterone Receptor A)ESR1 (ERα)AR (Adrenergic receptors)ESR2 (ERβ)

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