Currow David C, Abernethy Amy P
Discipline of Palliative & Supportive Services, Flinders University, GPO Box 2100, Adelaide, SA 5001, Australia.
Future Oncol. 2014 Apr;10(5):789-802. doi: 10.2217/fon.14.14. Epub 2014 Jan 28.
Anamorelin hydrochloride is an orally active ghrelin receptor agonist in development by Helsinn, for the treatment of non-small-cell lung cancer (NSCLC) cachexia. In preclinical and clinical studies, the potent affinity of anamorelin for the ghrelin receptor is associated with significant appetite-enhancing activity and resultant improvements in body weight, lean body mass, and handgrip strength compared with placebo. The accompanying stimulatory effects on growth hormone and IGF-1 are not associated with tumor growth, and overall survival in patients with cancer is not compromised. Anamorelin is well tolerated with no dose-limiting toxicities identified to date. The findings of ongoing Phase III studies are needed to confirm the significant potential of anamorelin to treat NSCLC cachexia.
盐酸阿那莫林是 Helsinn 公司正在研发的一种口服活性胃饥饿素受体激动剂,用于治疗非小细胞肺癌(NSCLC)恶病质。在临床前和临床研究中,与安慰剂相比,阿那莫林对胃饥饿素受体的强效亲和力与显著的食欲增强活性以及体重、瘦体重和握力的改善有关。其对生长激素和胰岛素样生长因子-1的伴随刺激作用与肿瘤生长无关,且不会损害癌症患者的总生存期。阿那莫林耐受性良好,迄今未发现剂量限制性毒性。需要正在进行的 III 期研究结果来证实阿那莫林治疗 NSCLC 恶病质的巨大潜力。