Sarecycline hydrochloride for the treatment of acne vulgaris.
Sarecycline hydrochloride for the treatment of acne vulgaris.
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盐酸沙雷环素用于治疗寻常痤疮。
DOI：
10.1358/dot.2019.55.10.3045040
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发表时间：
2019
期刊：
影响因子：
1.8
通讯作者：
S. Chopra
中科院分区：
文献类型：
--
作者：
G. Kaul;D. Saxena;A. Dasgupta;S. Chopra
盐酸沙林克林（Seysara）是一种新型、窄谱四环素衍生物，于2018年10月获得美国食品和药物管理局（FDA）批准，用于治疗炎症性非结节性中重度寻常痤疮。它最初由Paratek Pharmaceuticals，Inc.开发。（美国）和Allergan plc（美国），后来被Almirall S.A.收购。（西班牙巴塞罗那）。Almirall S.A.以商品名Seysara获得美国FDA批准的口服sarecycline片剂。Sarecycline对重要的皮肤/软组织病原体具有抗菌活性，对痤疮皮肤杆菌（一种与痤疮病变相关的厌氧革兰氏阳性细菌）具有靶向活性，并且还与用于治疗寻常痤疮的其他四环素一样发挥抗炎作用。有趣的是，与广谱四环素类不同，鼠尾草素对需氧革兰氏阴性杆菌和与内源性肠道微生物植物群相关的厌氧菌的效力较低。这为它提供了更特异的抗菌谱，具有更低的不良脱靶抗菌作用的机会，从而使其成为同类产品中有希望的治疗选择。与其他四环素类药物相比，它的耐药倾向较低，对耐四环素金黄色葡萄球菌以及耐红霉素和克林霉素的念珠菌也有活性。痤疮菌株。Sarecycline已成功地进行了多项I期、II期和三项III期研究，确定其为耐受性良好的每日一次口服药物，可作为片剂用于治疗9岁或以上的患者。
Sarecycline hydrochloride (Seysara) is a novel, narrow-spectrum tetracycline derivative approved by the U.S. Food and Drug Administration (FDA) in October 2018 for the treatment of inflammatory non-nodular moderate to severe acne vulgaris. It was initially developed by Paratek Pharmaceuticals, Inc. (U.S.) and Allergan plc (U.S.), which later was acquired by Almirall S.A. (Barcelona, Spain). Almirall S.A. obtained U.S. FDA approval of oral sarecycline tablets under the trade name Seysara. Sarecycline exhibits antibacterial activity against important skin/soft tissue pathogens with targeted activity against Cutibacterium acnes--an anaerobic Gram-positive bacterium linked with acne lesions--and also exerts anti-inflammatory effects as do other tetracyclines used in the treatment of acne vulgaris. Interestingly, unlike the broad-spectrum tetracyclines, sarecycline is less potent against aerobic Gram-negative bacilli and anaerobic bacteria associated with endogenous intestinal microbial flora. This provides it with a more specific antibacterial spectra with lower chances of adverse off-target antibacterial effects, thus making it a promising choice of treatment over others in its class. It has also demonstrated low propensity to resistance as compared with other tetracyclines and is also active against tetracycline-resistant Staphylococcus aureus as well as erythromycin- and clindamycin-resistant C. acnes strains. Sarecycline has successfully undergone numerous phase I, phase II and three phase III studies establishing it as a well-tolerated once-daily oral drug available as a tablet for the treatment of patients 9 years of age or above.