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Fezolinetant

Chemical compound From Wikipedia, the free encyclopedia

Fezolinetant
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Fezolinetant, sold under the brand name Veozah, among others, is a medication used for the treatment of hot flashes (vasomotor symptoms) due to menopause.[5][11] It is a small-molecule, selective neurokinin-3 (NK3) receptor antagonist taken by mouth.[5] It was developed by Astellas Pharma, which acquired it from Ogeda (formerly Euroscreen) in April 2017.[12][13][14]

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The most common side effects of fezolinetant include abdominal pain, diarrhea, insomnia, back pain, hot flush, and elevated hepatic transaminases.[11]

Fezolinetant was approved for medical use in the United States in May 2023,[11] and it was approved in the European Union in December 2023.[6][7] Fezolinetant is the first NK3 receptor antagonist approved by the US Food and Drug Administration (FDA) to treat moderate to severe hot flashes from menopause.[11] The FDA considers it to be a first-in-class medication.[15]

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Medical uses

Fezolinetant is indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.[5][6]

Adverse effects

In September 2024, the US FDA added a warning to the prescribing label that fezolinetant can cause rare but serious liver injury.[16]

History

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In May 2017, fezolinetant had completed phase I and phase IIa clinical trials for hot flashes in postmenopausal females.[14] Phase IIa trials in polycystic ovary syndrome patients are ongoing.[14]

In March 2023, results from SKYLIGHT 1, a Phase III clinical study of the treatment of moderate to severe hot flashes due to menopause, were published in The Lancet.[17][18]

Fezolinetant shows high affinity for and potent inhibition of the NK3 receptor in vitro (Ki = 25 nM, IC50Tooltip half-maximal inhibitory concentration = 20 nM).[13] Loss-of-function mutations in TACR and TACR3, the genes respectively encoding neurokinin B and its receptor, the NK3 receptor, have been found in patients with idiopathic hypogonadotropic hypogonadism.[13] In accordance, NK3 receptor antagonists like fezolinetant have been found to 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 females and testosterone levels in males.[19] As such, they are similar to GnRH modulators, and present as a potential clinical alternative to them for use in the same kinds of indications.[20] However, 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.[19][20]

Unlike GnRH modulators, but similarly to estrogens, NK3 receptor antagonists including fezolinetant and MLE-4901 (also known as AZD-4901, formerly AZD-2624) have been found to alleviate hot flashes in menopausal females.[21][22] This would seem to be independent of their actions on the hypothalamic–pituitary–gonadal axis and hence on sex hormone production.[21][22] NK3 receptor antagonists are anticipated as a useful clinical alternative to estrogens for management of hot flashes, but with potentially reduced risks and side effects.[21][22]

The effectiveness of Veozah 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.[11] In both trials, after the first 12 weeks, the females on placebo were then re-randomized to Veozah for a 40-week extension study to evaluate safety.[11] Each trial ran a total of 52 weeks.[11] The average age of the trial participants was 54 years old.[11]

The FDA granted the application for fezolinetant priority review designation.[11] The approval of Veozah was granted to Astellas Pharma US, Inc.[11]

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Society and culture

In October 2023, the Committee for Medicinal Products for Human Use of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Veoza, intended for the treatment of hot flushes (vasomotor symptoms) associated with menopause.[6] The applicant for this medicinal product is Astellas Pharma Europe B.V.[6]

Fezolinetant was approved for medical use in the United States in May 2023,[11] and in the European Union in December 2023.[6][7]

Brand names

Fezolinetant is the international nonproprietary name.[23]

Fezolinetant is sold under the brand names Veozah and Veoza.[5][6]

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References

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