Department of Neurological Surgery, University of California, San Francisco, Fresno, California.
Edge Therapeutics, Berkeley Heights, New Jersey.
Neurosurgery. 2020 Dec 15;88(1):E13-E26. doi: 10.1093/neuros/nyaa430.
A sustained release microparticle formulation of nimodipine (EG-1962) was developed for treatment of patients with aneurysmal subarachnoid hemorrhage (aSAH).
To assess safety, tolerability, and pharmacokinetics of intracisternal EG-1962 in an open-label, randomized, phase 2 study of up to 12 subjects.
Subjects were World Federation of Neurological Surgeons grades 1 to 2, modified Fisher grades 2 to 4, and underwent aneurysm clipping within 48 h of aSAH. EG-1962, containing 600 mg nimodipine, was administered into the basal cisterns. Outcome on the extended Glasgow Outcome Scale (eGOS), pharmacokinetics, delayed cerebral ischemia and infarction, rescue therapy, and safety were evaluated.
The study was halted when a phase 3 study of intraventricular EG-1962 stopped because that study was unlikely to meet its primary endpoint. Six subjects were randomized (5 EG-1962 and 1 oral nimodipine). After 90-d follow-up, favorable outcome on the eGOS occurred in 1 of 5 EG-1962 and in the single oral nimodipine patient. Four EG-1962 and the oral nimodipine subject had angiographic vasospasm. One EG-1962 subject had delayed cerebral ischemia, and all subjects with angiographic vasospasm received rescue therapy except 1 EG-1962 patient. One subject treated with EG-1962 developed right internal carotid and middle cerebral artery narrowing 5 mo after placement of EG-1962, leading to occlusion and cerebral infarction. Pharmacokinetics showed similar plasma concentrations of nimodipine in both groups.
Angiographic vasospasm and unfavorable clinical outcome still occurred after placement of EG-1962. Internal carotid artery narrowing and occlusion after placement of EG-1962 in the basal cisterns has not been reported.
一种尼莫地平(EG-1962)的缓释微球制剂被开发用于治疗蛛网膜下腔出血(aSAH)患者。
评估颅内 EG-1962 的安全性、耐受性和药代动力学,这是一项开放标签、随机、2 期研究,共纳入 12 名受试者。
受试者为世界神经外科学会联合会 1 至 2 级,改良 Fisher 分级 2 至 4 级,且在 aSAH 后 48 小时内行动脉瘤夹闭术。将含有 600mg 尼莫地平的 EG-1962 注入基底池。评估扩展格拉斯哥预后评分(eGOS)、药代动力学、迟发性脑缺血和梗死、抢救治疗和安全性。
当脑室 EG-1962 的 3 期研究因该研究不太可能达到主要终点而停止时,该研究被停止。6 名受试者被随机分组(5 名 EG-1962 和 1 名口服尼莫地平)。90 天随访后,5 名 EG-1962 中有 1 名和 1 名口服尼莫地平患者的 eGOS 预后良好。4 名 EG-1962 和口服尼莫地平患者有血管痉挛。1 名 EG-1962 患者发生迟发性脑缺血,除 1 名 EG-1962 患者外,所有有血管痉挛的患者均接受了抢救治疗。1 名接受 EG-1962 治疗的患者在放置 EG-1962 后 5 个月出现右侧颈内动脉和大脑中动脉狭窄,导致闭塞和脑梗死。药代动力学显示两组患者的尼莫地平血浆浓度相似。
放置 EG-1962 后仍会发生血管痉挛和临床预后不良。基底池放置 EG-1962 后颈内动脉狭窄和闭塞尚未见报道。