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一种即将上市的治疗甲癣的药物:他氟硼酸盐。

An upcoming drug for onychomycosis: Tavaborole.

作者信息

Sharma Neha, Sharma Dhruva

机构信息

Department of Pharmacology, NIMS Medical College, Jaipur, Rajasthan, India.

Department of General Surgery, Jawaharlal Nehru Medical College, Ajmer, Rajasthan, India.

出版信息

J Pharmacol Pharmacother. 2015 Oct-Dec;6(4):236-9. doi: 10.4103/0976-500X.171870.

DOI:10.4103/0976-500X.171870
PMID:26816482
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4714399/
Abstract

Fungal infection of the nail as well as nail bed is termed as 'onychomycosis'. It is caused by dermatophytes, non-dermatophytic fungal species and yeasts like Candida albicans. It is traditionally treated by topical antifungals, systemic agents like ketoconazole, griseofulvin, itraconazole, fluconazole, etc. Chemical avulsion or surgical removal of nail can also be tried to treat this disease. In spite of all these treatment options available, podiatrists were always in search of an ideal drug molecule with lesser side effects and which may improve the patient compliance. This exhaustive search led to the discovery of a better antifungal agent, known as "Tavaborole." A systematic literature search was carried out using databases such as PubMed, Cochrane Reviews, Google Scholar, etc. Detailed information about onychomycosis and tavaborole was gathered. Tavaborole is the first oxaborole antifungal agent approved by FDA in July 2014. It is marketed under the trade name "Kerydin." It acts by inhibiting protein synthesis in the fungus. It inhibits an enzyme known as cytosolic leucyl-transfer RNA synthetase, or LeuRS, which plays a key role in fungal essential protein synthesis. Dermatitis at the site of topical application, erythema, exfoliation and ingrowing toe nail has been reported in 1% of subjects. Tavaborole may offer a promising role in the treatment of onychomycosis and may compell podiatrists to offer its use in onychomycosis. The present study describes about chemical nature, mechanism of action and two completed phase 3 clinical trial findings of Tavaborole.

摘要

指甲以及甲床的真菌感染被称为“甲癣”。它由皮肤癣菌、非皮肤癣菌真菌种类以及白色念珠菌等酵母菌引起。传统上通过外用抗真菌药、酮康唑、灰黄霉素、伊曲康唑、氟康唑等全身性药物进行治疗。也可以尝试化学脱甲或手术拔甲来治疗这种疾病。尽管有所有这些治疗选择,但足病医生一直在寻找一种副作用较小且能提高患者依从性的理想药物分子。这种详尽的探索导致了一种更好的抗真菌剂“他氟硼酸盐”的发现。使用PubMed、Cochrane综述、谷歌学术等数据库进行了系统的文献检索。收集了有关甲癣和他氟硼酸盐的详细信息。他氟硼酸盐是2014年7月被美国食品药品监督管理局批准的首个氧硼戊环类抗真菌剂。它以“Kerydin”的商品名销售。它通过抑制真菌中的蛋白质合成起作用。它抑制一种名为胞质亮氨酰 - 转移RNA合成酶(LeuRS)的酶,该酶在真菌必需蛋白质合成中起关键作用。1%的受试者报告了局部应用部位的皮炎、红斑、脱屑和嵌甲。他氟硼酸盐可能在甲癣治疗中发挥有前景的作用,并可能促使足病医生在甲癣治疗中使用它。本研究描述了他氟硼酸盐的化学性质、作用机制以及两项完成的3期临床试验结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/9805238b7cce/JPP-6-236-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/2b96263a57d1/JPP-6-236-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/42643a80a85b/JPP-6-236-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/f0b20bcdd40b/JPP-6-236-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/401bae68c517/JPP-6-236-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/9805238b7cce/JPP-6-236-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/2b96263a57d1/JPP-6-236-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/42643a80a85b/JPP-6-236-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/f0b20bcdd40b/JPP-6-236-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/401bae68c517/JPP-6-236-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7845/4714399/9805238b7cce/JPP-6-236-g005.jpg

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Efinaconazole 10% nail solution: a new topical treatment with broad antifungal activity for onychomycosis monotherapy.10% 艾氟康唑甲溶液:一种用于甲真菌病单药治疗的具有广泛抗真菌活性的新型局部治疗药物。
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Ethynyl-substituted benzosiloxaboroles: the role of C(π)⋯B interactions in their crystal packing and use in Cu(i)-catalyzed 1,3-dipolar cycloaddition.乙炔基取代的苯并硅硼杂环戊二烯:C(π)⋯B相互作用在其晶体堆积中的作用及其在铜(I)催化的1,3-偶极环加成反应中的应用
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