Fritz T A, Unger E C, Sutherland G, Sahn D
ImaRx Pharmaceutical Corp., Tucson, Arizona 85719, USA.
Invest Radiol. 1997 Dec;32(12):735-40. doi: 10.1097/00004424-199712000-00003.
Stabilized microbubbles are under development as contrast agents for medical ultrasound. The authors report the results of Phase I clinical trials of a new ultrasound contrast agent based on lipidencapsulated perfluorocarbon gas microbubbles.
Lipids encapsulating perfluoropropane gas (Aerosomes MRX-115, ImaRx Pharmaceutical Corp., Tucson, AZ) were evaluated in Phase I clinical trials. Two separate studies were performed. The first was a single escalating-dose study (n = 30 subjects), and the second was a multiple-dose study (n = 18 subjects) with rechallenge in several subjects (n = 4) after 21 days. Echocardiographic examinations were performed before and after contrast agent for each test drug administration for both studies, with the exception of the rechallenge group. Doses tested in the single-dose study ranged from 0.005 mL/kg to 0.100 mL/kg body weight. In the multiple-dose study, five doses of 0.005 mL/ kg to 0.030 mL/kg (0.025-0.150 mL/kg total dose) were evaluated. Studies were single-masked, placebo-controlled, and safety assessment and adverse events were monitored.
All doses in both studies were well tolerated with no treatment-related changes in safety measures for either study. Left ventricular cavity and myocardial enhancement were seen with all doses of MRX-115.
MRX-115 is a promising new intravascular ultrasound contrast agent that was safe and well tolerated at the doses evaluated in these studies.
稳定微泡作为医学超声造影剂正在研发中。作者报告了一种基于脂质包裹全氟碳气体微泡的新型超声造影剂的I期临床试验结果。
对包裹全氟丙烷气体的脂质（Aerosomes MRX - 115，ImaRx制药公司，亚利桑那州图森市）进行了I期临床试验。进行了两项独立研究。第一项是单剂量递增研究（n = 30名受试者），第二项是多剂量研究（n = 18名受试者），其中部分受试者（n = 4）在21天后再次接受给药。除再次给药组外，两项研究中每次给予受试药物前后均进行超声心动图检查。单剂量研究中测试的剂量范围为0.005 mL/kg至0.100 mL/kg体重。在多剂量研究中，评估了五剂0.005 mL/kg至0.030 mL/kg（总剂量0.025 - 0.150 mL/kg）。研究为单盲、安慰剂对照，并监测安全性评估和不良事件。
两项研究中的所有剂量耐受性良好，两项研究的安全措施均未出现与治疗相关的变化。所有剂量的MRX - 115均可见左心室腔和心肌增强。
MRX - 115是一种有前景的新型血管内超声造影剂，在这些研究中评估的剂量下安全且耐受性良好。
