一種新型注射抗生素的體外試驗(yàn)和人體臨床試驗(yàn)結(jié)果顯示：用于治療革蘭氏陽性細(xì)菌導(dǎo)致的嚴(yán)重感染，藥物抵抗性較小而體外活性極其強(qiáng)大。在2005年4月荷蘭哥本哈根舉行的歐洲臨床微生物學(xué)和感染疾病學(xué)會年會上報道了這項(xiàng)結(jié)果。

一項(xiàng)臨床試驗(yàn)設(shè)計用于評估這種新型Telavancin抗生素的耐藥性發(fā)展情況，在金黃色葡萄球菌中的綜合研究資料顯示，Telavacin對突變耐藥菌株有較低活性。這種藥物顯示出對革蘭氏細(xì)菌有強(qiáng)大的光譜活性，包括萬古霉素中度抗藥性金黃色葡萄球菌和萬古霉素耐藥金黃色葡萄球菌菌株。另外一項(xiàng)試驗(yàn)顯示：這種藥物在血漿、皮膚大水皰中有著很好的穿透性，能夠達(dá)到殺滅S aureus包括甲氧苯青霉素耐藥菌株的有效濃度。在血透患者中進(jìn)行的臨床試驗(yàn)結(jié)果顯示：對中度～中度腎功能損害患者建議降低用藥劑量。

在一項(xiàng)計劃研究對S aureus以及其它革蘭氏陽性細(xì)菌有效的多價藥物研究方案中，Theravance公司發(fā)現(xiàn)了這種新型脂甘油肽，Televancin。Televancin具有獨(dú)特的多功能作用機(jī)制，該公司相信能夠加速殺滅細(xì)菌減少耐藥細(xì)菌生成的危險。該藥正在進(jìn)行III期臨床試驗(yàn)，治療復(fù)雜的皮膚以及皮膚結(jié)構(gòu)的感染、以及醫(yī)院內(nèi)獲得性肺炎。在臨床使用中所能達(dá)到的較大濃度，觀察到對細(xì)菌胞膜功能，例如膜去極化以及通透性，都有直接作用。
 
Injectible Antibiotic Shows Potent Activity
 
The results of in vitro studies and human clinical studies of a new injectable antibiotic showed low potential for drug resistance as well as potent in vitro activity for serious infections caused by Gram-positive bacteria. These results were presented at the annual European Congress of Clinical Microbiology and Infectious Diseases (ECCMID), held in Copenhagen (Denmark) in April 2005.

A study designed to evaluate the potential of the antibiotic for development of resistance to the new drug, called telavancin, among a collection of Staphylocaccus aureus revealed that telavancin has a low potential for resistant mutant selection. The compound exhibited potent in vitro activity across a broad spectrum of Gram-positive organisms, including vancomycin-intermediate S aureus and vancomycin-resistant S aureus strains. Another study showed excellent penetration of the drug in plasma and skin blister fluid, achieving concentrations well above those shown to be bactericidal against S aureus, including methicillin-resistant strains. Still another study of the drug used in hemodialysis subjects concluded that a dosage reduction is recommended for patients with moderate-to-severe renal impairment.

Televancin is a novel lipoglycopeptide discovered by Theravance (So. San Francisco, CA, USA) through the application of multivalent drug design in a program dedicated to finding new antibiotics for serious infections due to S aureus and other Gram-positive pathogens. Televance has a unique multifunctional mechanism of action that the company believes speeds bacterial killing and reduces the risks of inducing resistance. The compound is currently in phase III study for the treatment of complicated skin and skin structure infections and hospital-acquired pneumonia. At higher, clinically achievable concentrations, direct effects on bacterial plasma membrane function, such as membrane potential depolarization and increased permeability, were observed.