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奥替康唑:首次获批。

Oteseconazole: First Approval.

作者信息

Hoy Sheridan M

机构信息

Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.

出版信息

Drugs. 2022 Jun;82(9):1017-1023. doi: 10.1007/s40265-022-01734-y.

DOI:10.1007/s40265-022-01734-y
PMID:35713845
Abstract

Oteseconazole (VIVJOA™) is an orally administered azole antifungal agent developed by Mycovia Pharmaceuticals for the treatment of fungal infections. It inhibits cytochrome P450 (CYP) 51, thereby affecting the formation and integrity of the fungal cell membrane, but has a low affinity for human CYP enzymes due to its tetrazole metal-binding group. Oteseconazole is the first agent to be approved (in April 2022) for recurrent vulvovaginal candidiasis (RVVC) in the USA, where it is indicated to reduce the incidence of RVVC in females with a history of RVVC who are NOT of reproductive potential. Clinical development for the treatment of onychomycosis, and invasive and opportunistic infections is ongoing. This article summarizes the milestones in the development of oteseconazole leading to this first approval for reducing the incidence of RVVC in females with a history of RVVC who are NOT of reproductive potential.

摘要

奥替康唑(VIVJOA™)是Mycovia制药公司研发的一种口服唑类抗真菌药物,用于治疗真菌感染。它抑制细胞色素P450(CYP)51,从而影响真菌细胞膜的形成和完整性,但由于其四唑金属结合基团,对人CYP酶的亲和力较低。奥替康唑是美国首个获批(2022年4月)用于复发性外阴阴道念珠菌病(RVVC)的药物,适用于有RVVC病史且无生育潜力的女性,以降低RVVC的发病率。治疗甲癣、侵袭性和机会性感染的临床开发正在进行中。本文总结了奥替康唑的研发历程中的里程碑事件,这些事件促成了它首次获批用于降低有RVVC病史且无生育潜力的女性的RVVC发病率。

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本文引用的文献

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Cochrane Database Syst Rev. 2022 Jan 10;1(1):CD009151. doi: 10.1002/14651858.CD009151.pub2.
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In vitro activities of the tetrazole VT-1161 compared with itraconazole and fluconazole against and non- species.唑类药物 VT-1161 与伊曲康唑和氟康唑体外抗 和 非 种的活性比较。
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Impact of the Major Candida glabrata Triazole Resistance Determinants on the Activity of the Novel Investigational Tetrazoles VT-1598 and VT-1161.
探索在甾醇14α-脱甲基酶(CYP51)抗真菌唑类抑制剂设计中的长臂酰胺连接侧链。
J Med Chem. 2025 Jun 12;68(11):10781-10799. doi: 10.1021/acs.jmedchem.4c02922. Epub 2025 May 22.
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Anti- Activity of Cysteine-Modified Amidated Decoralin in the Presence of Engineered Nanomaterials.工程纳米材料存在下,半胱氨酸修饰的酰胺化去甲珊瑚素的抗活性。
Pharmaceutics. 2025 Apr 2;17(4):460. doi: 10.3390/pharmaceutics17040460.
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Exploring medium and long arm extensions of 1,2,4-triazole derivatives as 14α-demethylase (CYP51) inhibitors.探索1,2,4-三唑衍生物作为14α-脱甲基酶(CYP51)抑制剂的中、长臂延伸物。
RSC Med Chem. 2025 Mar 12;16(5):2270-2280. doi: 10.1039/d4md00863d. eCollection 2025 May 22.
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