Tella Sri Harsha, Kommalapati Anuhya, Correa Ricardo
Endocrinology, Diabetes and Metabolism, National Institute of Health.
Internal Medicine, Medstar Washington Hospital Center.
Cureus. 2017 May 31;9(5):e1300. doi: 10.7759/cureus.1300.
Abaloparatide (previously known as BA058) is a synthetic 34-amino acid peptide and novel selective activator of parathyroid hormone receptor 1 (PTHR1) currently under development as a new anabolic agent in the management of osteoporosis. This paper reviews the profile and potential of abaloparatide in the treatment of postmenopausal osteoporosis. This paper is based on clinical trials and a PubMed search. Search terms used were "abaloparatide", "BA058", and "PTHrP". This review outlines the effects of this anabolic PTHR1 activator, which increases bone mineral density in patients at high risk for osteoporosis. The potential adverse effects of abaloparatide are also summarized. Abaloparatide has 41% homology to parathyroid hormone (PTH) (1-34) and 76% homology to parathyroid hormone-related protein (PTHrP) (1-34). The molecule was meticulously selected to retain stability and potent bone anabolic activity, and it has a limited effect on bone resorption (hence, a low calcium-mobilizing potential). Abaloparatide has shown promising results in a reduction of new onset vertebral (approximately 86% reduction) and nonvertebral fractures (approximately 43% reduction). In clinical trials to date, abaloparatide appears to have a good safety and tolerability profile with a significantly lower degree of hypercalcemia compared to that of teriparatide. Based on the clinical trials, the optimum dose of abaloparatide is 80 mcg subcutaneous once daily.
阿巴洛帕替德（曾用名BA058）是一种由34个氨基酸组成的合成肽，是甲状旁腺激素受体1（PTHR1）的新型选择性激活剂，目前正作为一种治疗骨质疏松症的新型促合成代谢药物进行研发。本文综述了阿巴洛帕替德在治疗绝经后骨质疏松症方面的概况和潜力。本文基于临床试验和PubMed搜索。使用的搜索词为“阿巴洛帕替德”、“BA058”和“PTHrP”。本综述概述了这种促合成代谢的PTHR1激活剂的作用，它可增加骨质疏松症高危患者的骨矿物质密度。还总结了阿巴洛帕替德可能的不良反应。阿巴洛帕替德与甲状旁腺激素（PTH）（1-34）有41%的同源性，与甲状旁腺激素相关蛋白（PTHrP）（1-34）有76%的同源性。该分子经过精心筛选，以保持稳定性和强大的骨促合成代谢活性，并且对骨吸收的影响有限（因此，钙动员潜力较低）。阿巴洛帕替德在减少新发椎体骨折（约减少86%）和非椎体骨折（约减少43%）方面已显示出有前景的结果。在迄今为止的临床试验中，与特立帕肽相比，阿巴洛帕替德似乎具有良好的安全性和耐受性，高钙血症程度明显更低。基于临床试验，阿巴洛帕替德的最佳剂量为每日一次皮下注射80微克。
