Abaloparatide
PTHrP Analog | Anabolic Bone-Building Agent
Abaloparatide is an FDA-approved anabolic bone-building agent and synthetic analog of parathyroid hormone-related protein (PTHrP). It selectively activates the PTH1 receptor to stimulate new bone formation while minimizing bone resorption. In the phase III ACTIVE trial, abaloparatide showed superior BMD increases at the hip compared to teriparatide, with substantial fracture risk reduction. It was approved in the US in 2017 and EU in 2022 for postmenopausal women and men with osteoporosis at high fracture risk.
Moleküler Gösterim
M.W.: 3,960 Da
PubChem 2D yapı diyagramı
Referans Flakon
Referans illüstrasyonu — ürün listesi değildir
Etki Mekanizması
Abaloparatide works through selective activation of the parathyroid hormone 1 receptor (PTH1R), a G protein-coupled receptor expressed on osteoblasts and osteocytes. It preferentially binds to the RG (relaxed, G-protein-coupled) conformational state of PTH1R, which elicits a transient downstream cyclic AMP signaling response favoring anabolic bone formation over resorption. This selective binding pattern produces more bone-building activity with less hypercalcemic effect compared to native PTH. The result is increased cortical and trabecular bone volume, density, and improved microarchitecture.
Abaloparatide is an FDA-approved anabolic bone-building agent and synthetic analog of parathyroid hormone-related protein (PTHrP). It selectively activates the PTH1 receptor to stimulate new bone formation while minimizing bone resorption. In the phase III ACTIVE trial, abaloparatide showed superior BMD increases at the hip compared to teriparatide, with substantial fracture risk reduction. It was approved in the US in 2017 and EU in 2022 for postmenopausal women and men with osteoporosis at high fracture risk.
Moleküler Veri
Araştırma Endikasyonları
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Doz Protokolleri
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| Hedef | Doz | Sıklık | Yol |
|---|---|---|---|
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Etkileşimler
Bisphosphonates (Alendronate)
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Teriparatide
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Kaynaklar
- Effect of Abaloparatide vs Placebo on New Vertebral Fractures in Postmenopausal Women With Osteoporosis (ACTIVE Trial) — Miller PD, Hattersley G, Riis BJ, et al.
- ACTIVExtend Trial: Abaloparatide Followed by Alendronate — Cosman F, Miller PD, Williams GC, et al.
- Phase 2 Dose-finding Study of BA058 in Postmenopausal Women — Leder BZ, O'Dea LS, Zanchetta JR, et al.
- Profile of Abaloparatide and Its Potential in Postmenopausal Osteoporosis — Tella SH, Kommalapati A, Correa R