The macrolide class of antibiotics, including the early generation macrolides erythromycin, clarithromycin and azithromycin, have been used broadly for treatment of respiratory tract infections. An increase of treatment failures of early generation macrolides is due to the upturn in bacterial macrolide resistance to 48% in the US and over 80% in Asian countries and has led to the use of alternate therapies, such as fluoroquinolones. The safety of the fluoroquinolones is now in question and alternate antibiotics for the outpatient treatment of community acquired bacterial pneumonia are needed. Telithromycin, approved in 2003, is no longer used owing to serious adverse events, collectively called the ‘Ketek effects’. Telithromycin has a side chain pyridine moiety that blocks nicotinic acetylcholine receptors. Blockade of these receptors is known experimentally to cause the side effects seen with telithromycin in patients use. Solithromycin is a new macrolide, the first fluoroketolide, which has been tested successfully in two Phase 3 trials and is undergoing regulatory review at the FDA. Solithromycin is differentiated from telithromycin chemically and biologically in that its side chain is chemically different and does not significantly block nicotinic acetylcholine receptors. Solithromycin was well tolerated and effective in clinical trials.

中文翻译：

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索霉素的旅程-一切都在化学过程中

大环内酯类抗生素，包括较早的大环内酯类红霉素，克拉霉素和阿奇霉素，已广泛用于治疗呼吸道感染。早期大环内酯类药物治疗失败的增加是由于细菌大环内酯类药物的耐药性在美国上升到48％，在亚洲国家超过80％，并导致了替代疗法的使用，例如氟喹诺酮类药物。现在，人们对氟喹诺酮类药物的安全性提出了疑问，需要替代抗生素对社区获得性细菌性肺炎进行门诊治疗。由于严重的不良事件（统称为“ Ketek效应”），2003年获批的Telithromycin不再使用。Telithromycin具有可阻断烟碱乙酰胆碱受体的侧链吡啶部分。从实验上已知这些受体的阻断会导致替利霉素在患者使用中产生的副作用。索霉素是一种新的大环内酯，第一个氟代酮内酯，已在两项三期临床试验中成功进行了测试，目前正在FDA进行监管审查。Solithromycin在化学和生物学上与Telithromycin有所不同，因为其侧链在化学上是不同的，并且不会显着阻断烟碱乙酰胆碱受体。索霉素在临床试验中被很好地耐受和有效。Solithromycin在化学和生物学上与Telithromycin有所不同，因为其侧链在化学上是不同的，并且不会显着阻断烟碱乙酰胆碱受体。索霉素在临床试验中被很好地耐受和有效。Solithromycin在化学和生物学上与Telithromycin有所不同，因为其侧链在化学上是不同的，并且不会显着阻断烟碱乙酰胆碱受体。索霉素在临床试验中被很好地耐受和有效。