Kyriakakis Nikolaos, Chau Vincent, Lynch Julie, Orme Steve M, Murray Robert D
St James's University Hospital, Leeds Teaching Hospitals NHS Trust, Leeds Centre for Diabetes and Endocrinology, Department of Endocrinology , Beckett Street, Leeds LS9 7TF , UK +44 0 113 206 4578 ; +44 0 113 206 5065 ;
Expert Opin Pharmacother. 2014 Dec;15(18):2681-92. doi: 10.1517/14656566.2014.970173. Epub 2014 Oct 11.
The novel formulation of lanreotide, lanreotide (LAN) autogel (ATG), has been available in Europe since 2001 and USA from 2006 for the treatment of acromegaly. It is one of only two clinically available somatostatin analogs available for use in acromegaly. Data relating to the use of ATG in acromegaly, specifically relating to comparison to octreotide (OCT) LAR and patient acceptability and preference, have been slow to accumulate.
We performed a comprehensive review of the original literature relating to development, pharmacokinetics, acceptability and clinical efficacy of ATG.
LAN ATG is a novel formulation of LAN consequent on self-assembly of nanotubules in water. Diffusion between molecules within the nanotubules and surrounding tissue fluid in vivo leads to pseudo first-order pharmacokinetics. Efficacy is equivalent to the alternate long-acting somatostatin analog, OCT LAR, normalizing growth hormone and IGF-I levels in around 60 and 50% respectively. Control of tumor growth is observed in over 95% of patients, with 64% seeing a clinically significant reduction in tumor size. ATG is provided in a prefilled syringe for deep subcutaneous injection, allowing self-injection, and may be administered up to 8 weeks greatly improving convenience for the patient. The data strongly support consideration of ATG as the medical therapy of choice for patients with acromegaly.
兰瑞肽的新型制剂兰瑞肽(LAN)自凝胶(ATG)自2001年起在欧洲上市,2006年起在美国上市,用于治疗肢端肥大症。它是临床上仅有的两种可用于肢端肥大症的生长抑素类似物之一。关于ATG在肢端肥大症中的应用数据,特别是与奥曲肽(OCT)长效释放制剂(LAR)的比较以及患者的可接受性和偏好方面的数据积累缓慢。
我们对有关ATG的研发、药代动力学、可接受性和临床疗效的原始文献进行了全面综述。
LAN ATG是LAN在水中自组装形成纳米管后的新型制剂。纳米管内分子与体内周围组织液之间的扩散导致伪一级药代动力学。其疗效与另一种长效生长抑素类似物OCT LAR相当,分别使约60%和50%的患者生长激素和胰岛素样生长因子-I水平恢复正常。超过95%的患者肿瘤生长得到控制,64%的患者肿瘤大小出现临床显著缩小。ATG采用预填充注射器进行深部皮下注射,可自行注射,给药间隔可达8周,极大地提高了患者的便利性。这些数据有力地支持将ATG视为肢端肥大症患者的首选药物治疗方法。