ABALOPARATIDE

Description: Abaloparatide (Trade name Tymlos; formerly known as BA058) is a 34 amino acid synthetic analog of parathyroid hormone-related protein (PTHrP) that is used to treat osteoporosis. Like the related drug teriparatide, and unlike bisphosphonates, it is an anabolic (i.e., bone growing) agent. A subcutaneous injection formulation of the drug has completed a Phase III trial for osteoporosis. This single study found a decrease in fractures. On 28 April 2017, it was approved by Food and drug administration (FDA) to treat postmenopausal osteoporosis. Abaloparatide has 41% homology to parathyroid hormone (PTH) (1-34) and 76% homology to parathyroid hormone-related protein (PTHrP) (1-34). It works as an anabolic agent for the bone, through selective activation of the parathyroid hormone 1 receptor (PTH1R), a G protein-coupled receptor (GPCR) expressed in the osteoblasts and osteocytes. Abaloparatide preferentially binds the RG conformational state of the PTH1R, which in turn elicits a transient downstream cyclic AMP signaling response towards to a more anabolic signaling pathway.

References: Bone. 2017, 95: 143–150.