Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute, Lucknow, India.
Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, India.
Drugs Today (Barc). 2022 Jul;58(7):315-326. doi: 10.1358/dot.2022.58.7.3389002.
Contezolid (MRX-I, Youxitai) is an oral oxazolidinone drug being developed by MicuRx Pharmaceutical Co., Ltd., Shanghai, China. It was approved by China's National Medical Products Administration (NMPA) in June 2021, attaining its first approval for the treatment of complicated skin and soft tissue infections (cSSTIs). It is also under clinical development for acute bacterial skin and skin structure infections (ABSSSIs) in the U.S. after receiving qualified infectious disease product (QIDP) classification and fast track status by U.S. Food and Drug Administration (FDA) in September 2018. Contezolid is effective against a broad range of Gram-positive bacteria including activity against methicillin-resistant (MRSA), penicillin-resistant and vancomycin-resistant Enterococci (VRE). It provides a major benefit over the most popular drug of its class, linezolid (Zyvox), by offering an improved safety profile and minimal effects concerning myelosuppression and monoamine oxidase (MAO) inhibition, two independent adverse events limiting linezolid use in the clinic. The recommended dosage regimen of contezolid is 800 mg every 12 hours for 7-14 days with regular food intake and it can be extended if required. At the mentioned dose under fed conditions, satisfactory efficacy against MRSA with a 90%; or higher cumulative fraction of response and probability of target attainment was achieved. Additionally, contezolid also exhibits activity against and .
康替唑胺(MRX-I,佑泽泰)是一种由中国上海 MicuRx 制药有限公司开发的口服噁唑烷酮类药物。它于 2021 年 6 月获得中国国家药品监督管理局(NMPA)批准,首次获准用于治疗复杂性皮肤和软组织感染(cSSTIs)。在美国,它在获得美国食品和药物管理局(FDA)的合格传染病产品(QIDP)分类和快速通道地位后,也在进行治疗急性细菌性皮肤和皮肤结构感染(ABSSSIs)的临床试验。康替唑胺对广泛的革兰氏阳性菌有效,包括对耐甲氧西林金黄色葡萄球菌(MRSA)、青霉素耐药和万古霉素耐药肠球菌(VRE)的活性。与同类药物中最受欢迎的药物利奈唑胺(Zyvox)相比,它提供了一个主要的优势,具有改善的安全性概况和对骨髓抑制和单胺氧化酶(MAO)抑制的最小影响,这两个独立的不良事件限制了利奈唑胺在临床上的应用。康替唑胺的推荐剂量方案为每 12 小时 800mg,持续 7-14 天,与正常饮食一起服用,如果需要,可以延长疗程。在上述剂量下,在进食条件下,对 MRSA 的疗效令人满意,累积反应分数和目标达成率达到 90%或更高。此外,康替唑胺还对 和 具有活性。