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Characterization of SPR994, an Orally Available Carbapenem, with Activity Comparable to Intravenously Administered Carbapenems
ACS Infectious Diseases ( IF 4.0 ) Pub Date : 2018-08-17 00:00:00 , DOI: 10.1021/acsinfecdis.8b00188
Aileen Rubio 1 , Michael J. Pucci 1 , Akash Jain 1
Affiliation  

Carbapenems are potent antibacterials with broad-spectrum activity. However, poor oral absorption generally confines this important drug class to in-hospital use by intravenous (IV) administration. The continued rise in drug resistant pathogens creates a need for alternative oral therapies with broad-spectrum activity. SPR994 is a novel formulation of the orally bioavailable pivoxil prodrug of SPR859 (tebipenem) and is being developed as the first oral carbapenem for treatment of complicated urinary tract infections (cUTIs) in adults. Herein, we describe characteristics beneficial to oral administration and compare the in vitro and in vivo activity of SPR859 or SPR994 with IV carbapenems.

中文翻译:

口服可得的碳青霉烯SPR994的表征,其活性与静脉内给药的碳青霉烯类相当

碳青霉烯类是具有广谱活性的强效抗菌剂。然而,不良的口服吸收通常通过静脉内(IV)给药将这种重要的药物限于医院内使用。耐药病原体的持续增长导致需要具有广谱活性的替代口服疗法。SPR994是SPR859(tebipenem)口服可生物利用的匹伏西尔前药的新型制剂,并且正在开发为治疗成人复杂尿路感染(cUTI)的首个口服碳青霉烯前体。在本文中,我们描述了有利于口服给药的特征,并比较了具有IV碳青霉烯类的SPR859或SPR994的体外体内活性。
更新日期:2018-08-17
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