Sundar Shyam, Jha T K, Thakur C P, Bhattacharya S K, Rai M
Kala-azar Medical Research Center, Banaras Hindu University, Varanasi, India.
Trans R Soc Trop Med Hyg. 2006 Dec;100 Suppl 1:S26-33. doi: 10.1016/j.trstmh.2006.02.011. Epub 2006 May 26.
Large-scale antimony resistance in the treatment of visceral leishmaniasis (VL) in north Bihar, India, has led to the development of miltefosine as an alternative therapy. In a pilot study and later in three Phase II studies involving 249 patients, oral miltefosine, 100-150 mg/day for 28 days, was shown to cure approximately 90% patients with reasonable safety. In the pivotal Phase III trial, 299 patients were treated at three centres with amphotericin B as the comparator drug (99 patients). In this trial 38% and 20% patients had mild to moderate vomiting and diarrhoea respectively, similar to previous studies. Asymptomatic transient elevation of hepatic transaminases and mild renal dysfunction were observed in 15% and 10% patients respectively. The final cure rate was 94% with miltefosine and 97% with amphotericin B; based on these results, the drug was approved in India. Subsequently in two paediatric studies involving 119 patients in the age group of 2-11 years, the safety and efficacy of miltefosine (2.5 mg/kg daily for 28 days) was established with a cure rate (94%) similar to that seen in adults. Miltefosine is the first oral antileishmanial drug with a high degree of safety and efficacy for the treatment of VL.
在印度比哈尔邦北部,大规模锑耐药性致使内脏利什曼病(VL)治疗中出现了米替福新这种替代疗法。在一项试点研究以及随后涉及249名患者的三项II期研究中,口服米替福新,每日100 - 150毫克,持续28天,显示能治愈约90%的患者,且安全性良好。在关键的III期试验中,三个中心对299名患者进行了治疗,以两性霉素B作为对照药物(99名患者)。在该试验中,分别有38%和20%的患者出现轻度至中度呕吐和腹泻,与先前研究相似。分别有15%和10%的患者出现无症状性肝转氨酶短暂升高和轻度肾功能不全。米替福新的最终治愈率为94%,两性霉素B为97%;基于这些结果,该药物在印度获批。随后在两项涉及119名2至11岁儿童的儿科研究中,确定了米替福新(每日2.5毫克/千克,持续28天)的安全性和有效性,治愈率(94%)与成人相似。米替福新是首个用于治疗VL的安全性和有效性都很高的口服抗利什曼原虫药物。