MK - 0991（默克公司） - Suppr

Groll A H, Walsh T J

Pediatric Oncology Branch, National Cancer Institute, National Institutes of Health, Bethesda, MD 20891, USA.

IDrugs. 1999 Nov;2(11):1201-12.

Merck is developing the echinocandin-type antifungal, MK-0991 (L-743872), a beta-1,3-glucan synthesis inhibitor. It is currently undergoing phase III trials for the potential treatment of systemic fungal infections. The compound entered phase II clinical trials in late 1996. It was administered iv once daily and showed antifungal activity in vitro and in vivo against Candida (including azole-resistant Candida), Aspergillus and certain other fungi. The in vitro activity of MK-0991 has been confirmed by several studies. In November 1998, Morgan Stanley Dean Witter predicted worldwide sales of 40 million USD in 2000, rising to 275 million USD in 2005. In February 1999, Credit Suisse Dean Witter predicted sales of 65 million USD in 2001, rising to 330 million USD in 2002. In February 1999, Lehman Brothers predicted 60% probabilities of US and ex-US market penetrations and launch onto these markets by 2000. Expected sales are predicted to be 15 million USD (in the US) and 10 million USD (ex-US) in 2000, rising to 200 USD million and 175 million USD respectively in 2002. Peak annual sales of 500 million USD (US) and 500 million USD (ex-US) are predicted in 2008.

默克公司正在研发棘白菌素类抗真菌药物MK-0991（L-743872），一种β-1,3-葡聚糖合成抑制剂。它目前正在进行III期试验，用于潜在治疗系统性真菌感染。该化合物于1996年末进入II期临床试验。它通过静脉注射给药，每日一次，在体外和体内对念珠菌（包括耐唑类念珠菌）、曲霉菌和某些其他真菌均显示出抗真菌活性。MK-0991的体外活性已得到多项研究的证实。1998年11月，摩根士丹利添惠预测其2000年全球销售额为4000万美元，到2005年将增至2.75亿美元。1999年2月，瑞士信贷第一波士顿预测其2001年销售额为6500万美元，到2002年将增至3.3亿美元。1999年2月，雷曼兄弟预测其在美国和美国以外市场渗透并于2000年进入这些市场的概率为60%。预计2000年销售额为1500万美元（美国）和1000万美元（美国以外），到2002年将分别增至2亿美元和1.75亿美元。预计2008年的年销售额峰值为5亿美元（美国）和5亿美元（美国以外）。