Fezolinetant, sold under the brand name Veozah, is a medication used for the treatment of hot flashes (vasomotor symptoms) due to menopause.
Routes of administration by mouth.
It is a medication used for the treatment of hot flashes, vasomotor symptoms, due to menopause.
It is a small-molecule, orally active, selective neurokinin-3 (NK3) receptor antagonist for the treatment of sex hormone-related disorders.
Protein binding 51%
Metabolism CYP1A2, CYP2C9, CYP2C19 to lesser extent
Elimination half- life 9.6h
Excretion
Urine 76.9%, feces 14.7%
The most common side effects include abdominal pain, diarrhea, insomnia, back pain, hot flush and elevated hepatic transaminases.
It is the first neurokinin 3 (NK3) receptor antagonist approved by the US Food and Drug Administration (FDA) to treat moderate to severe hot flashes from menopause.
Fezolinetant has high affinity for and potent inhibition of the NK3 receptor.
NK3 receptor antagonists dose-dependently suppress luteinizing hormone (LH) secretion, though not that of follicle-stimulating hormone (FSH), and consequently to dose-dependently decrease estradiol and progesterone levels in women and testosterone levels in men.
They are similar to GnRH modulators, and present as a potential clinical alternative to them for use in the same kinds of indications.
The inhibition of sex hormone production by NK3 receptor inactivation tends to be less complete and non-castrating relative to that of GnRH modulators, and so they may have a reduced incidence of menopausal-like side effects such as loss of bone mineral density.
NK3 receptor antagonists including fezolinetant have been found to alleviate hot flashes in menopausal women, independent of their actions on the hypothalamic–pituitary–gonadal axis and hence on sex hormone production.
NK3 receptor antagonists are a useful clinical alternative to estrogens for management of hot flashes, but with potentially reduced risks and side effects.
Effectiveness of Fezolinetant to treat moderate to severe hot flashes was demonstrated in each of the first 12-week, randomized, placebo-controlled, double-blind portions of two phase III clinical trials.