Drugs R D. 2006;7(6):384-8. doi: 10.2165/00126839-200607060-00008.
Telavancin [TD-6424, ARBELIC] is an injectable, bactericidal lipoglycopeptide antibacterial that is in clinical development with Theravance (formerly Advanced Medicine) in the US. Telavancin, which was discovered by Theravance through the application of multivalent drug design, has a broad spectrum of activity against Gram-positive pathogens. Telavancin is currently in phase III development for complicated skin and soft tissue infections (including those caused by methicilin-resistant Staphylococcus aureus [MRSA]), nosocomial pneumonia, as well as other Gram-positive pathogens. The antibacterial effects of telavancin are mediated through multiple mechanisms, including inhibition of cell wall (peptidoglycan) synthesis. The drug also produces changes in bacterial cell membrane permeability. The multiple mechanisms of action may be responsible for the low frequency of spontaneous resistance to telavancin. Theravance and Astellas Pharma entered into a licensing agreement for telavancin in November 2005. The two companies will collaborate for the development and commercialisation of the antibacterial agent worldwide, except Japan. Under the terms of the agreement, Astellas will make a 65 million US dollars up-front payment and royalties on global sales to Theravance; in addition, Theravance is eligible to receive 156 million US dollars in clinical and regulatory milestones payments, including 136 million US dollars for completing enrollment, filling and approval of ongoing phase III programmes, and 20 million US dollars if phase III data indicate telavancin's superiority over vancomycin for the treatment of MRSA. Theravance will continue to explore partnering opportunities in the Japanese market. Telavancin was granted fast-track status by the US FDA in March 2005 for the treatment of complicated skin and skin structure infections (cSSSIs), as well as hospital-acquired pneumonia (nosocomial pneumonia). The compound is currently in phase III trials for these indications in the US. Theravance has also conducted two randomised, double-blind phase II trials (FAST and FAST 2) of telavancin in patients with cSSSIs caused by Gram-positive bacteria, in which telavancin (7 or 10 mg/kg) was compared with standard vancomycin therapy. Results showed that while telavancin was comparable to standard therapy overall, telavancin was associated with superior MRSA eradication rates.
特拉万星[TD - 6424，ARBELIC]是一种注射用的杀菌性脂糖肽类抗菌药物，目前正在美国与先灵葆雅公司（原先进医药公司）进行临床开发。特拉万星由先灵葆雅公司通过多价药物设计发现，对革兰氏阳性病原体具有广泛的活性。目前，特拉万星正处于治疗复杂性皮肤和软组织感染（包括耐甲氧西林金黄色葡萄球菌[MRSA]引起的感染）、医院获得性肺炎以及其他革兰氏阳性病原体感染的III期临床开发阶段。特拉万星的抗菌作用是通过多种机制介导的，包括抑制细胞壁（肽聚糖）合成。该药物还会引起细菌细胞膜通透性的改变。多种作用机制可能是导致对特拉万星自发耐药频率较低的原因。2005年11月，先灵葆雅公司与安斯泰来制药公司就特拉万星达成了许可协议。两家公司将在全球（日本除外）合作进行该抗菌药物的开发和商业化。根据协议条款，安斯泰来将预先支付6500万美元，并就全球销售额向先灵葆雅支付特许权使用费；此外，先灵葆雅有资格获得1.56亿美元的临床和监管里程碑付款，包括完成正在进行的III期项目的入组、申报和批准可获得1.36亿美元，如果III期数据表明特拉万星在治疗MRSA方面优于万古霉素，则可额外获得2000万美元。先灵葆雅将继续探索在日本市场的合作机会。2005年3月，特拉万星被美国食品药品监督管理局授予快速通道地位，用于治疗复杂性皮肤和皮肤结构感染（cSSSIs）以及医院获得性肺炎（医院感染性肺炎）。该化合物目前正在美国针对这些适应症进行III期试验。先灵葆雅还对特拉万星在革兰氏阳性菌引起的cSSSIs患者中进行了两项随机、双盲II期试验（FAST和FAST 2），将特拉万星（7或10mg/kg）与标准万古霉素疗法进行了比较。结果表明，虽然特拉万星总体上与标准疗法相当，但特拉万星的MRSA根除率更高。
