Английская Википедия:Fezolinetant
Шаблон:Short description Шаблон:Use American English Шаблон:Use dmy dates Шаблон:Cs1 config Шаблон:Infobox drug
Fezolinetant, sold under the brand name Veozah among others, is a medication used for the treatment of hot flashes (vasomotor symptoms) due to menopause.[1][2] It is a small-molecule, orally active, selective neurokinin-3 (NK3) receptor antagonist which is under development by for the treatment of sex hormone-related disorders.Шаблон:Medcn It is taken by mouth.[1] It is developed by Astellas Pharma which acquired it from Ogeda (formerly Euroscreen) in April 2017.[3][4][5]
The most common side effects include abdominal pain, diarrhea, insomnia, back pain, hot flush and elevated hepatic transaminases.[2]
Fezolinetant was approved for medical use in the United States in May 2023,[2] and in the European Union in December 2023.[6][7] Fezolinetant 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.[2] The FDA considers it to be a first-in-class medication.[8]
Medical uses
Fezolinetant is indicated for the treatment of moderate to severe vasomotor symptoms due to menopause.[1][6]
History
In May 2017, fezolinetant had completed phase I and phase IIa clinical trials for hot flashes in postmenopausal females.[5] Phase IIa trials in polycystic ovary syndrome patients are ongoing.[5]
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.[9][10]
Fezolinetant shows high affinity for and potent inhibition of the NK3 receptor in vitro (Ki = 25 nM, Шаблон:Abbrlink = 20 nM).[4] 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.[4] 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.[11] 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.[12] 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.[11][12]
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.[13][14] This would seem to be independent of their actions on the hypothalamic–pituitary–gonadal axis and hence on sex hormone production.[13][14] 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.[13][14]
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.[2] 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.[2] Each trial ran a total of 52 weeks.[2] The average age of the trial participants was 54 years old.[2]
The FDA granted the application for fezolinetant priority review designation.[2] The approval of Veozah was granted to Astellas Pharma US, Inc.[2]
Society and culture
Legal status
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,[2] and in the European Union in December 2023.[6][7]
Brand names
Fezolinetant is the international nonproprietary name.[15]
Fezolinetant is sold under the brand names Veozah and Veoza.[1][6]
References
Шаблон:Neurokinin receptor modulators Шаблон:Portal bar Шаблон:Authority control
- ↑ 1,0 1,1 1,2 1,3 Ошибка цитирования Неверный тег
<ref>
; для сносокVeozah FDA label
не указан текст - ↑ 2,00 2,01 2,02 2,03 2,04 2,05 2,06 2,07 2,08 2,09 2,10 Шаблон:Cite press release Шаблон:PD-notice
- ↑ Шаблон:Cite press release
- ↑ 4,0 4,1 4,2 Шаблон:Cite journal
- ↑ 5,0 5,1 5,2 Шаблон:Cite web
- ↑ 6,0 6,1 6,2 6,3 6,4 6,5 Ошибка цитирования Неверный тег
<ref>
; для сносокVeoza EPAR
не указан текст - ↑ 7,0 7,1 Ошибка цитирования Неверный тег
<ref>
; для сносокVeoza PI
не указан текст - ↑ Шаблон:Cite report
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ 11,0 11,1 Шаблон:Cite journal
- ↑ 12,0 12,1 Шаблон:Cite journal
- ↑ 13,0 13,1 13,2 Шаблон:Cite web
- ↑ 14,0 14,1 14,2 Шаблон:Cite web
- ↑ Шаблон:Cite journal
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