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Description

Abaloparatide (brand name Tymlos) is a human parathyroid hormone related peptide [PTHrP(1-34)] analog indicated for the treatment of postmenopausal women with osteoporosis at high risk for fracture. Abaloparatide is a PTHrP(1-34) analog which acts as an agonist at the PTH1 receptor (PTH1R). This results in activation of the cAMP signaling pathway in target cells. In rats and monkeys, abaloparatide had an anabolic effect on bone, demonstrated by increases in BMD and bone mineral content (BMC) that correlated with increases in bone strength at vertebral and/or nonvertebral sites. Abaloparatide was approved in April 28, 2017 by the FDA (as Tymlos) for the treatment of postmenopausal women with osteoporosis at high risk for fracture.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
0.087 nM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TYMLOS

PubMed

Sample Use Guides

In Vivo Use Guide
Recommended dose is 80 ug subcutaneously once daily; patients should receive supplemental calcium and vitamin D if dietary intake is inadequate. Administer as a subcutaneous injection into periumbilical region of abdomen. Administer initially where the patient can sit or lie down in case symptoms of orthostatic hypotension occur.
Route of Administration: Other
In Vitro Use Guide
cAMP signaling potency of Abaloparatide in PTHR1-expressing cells was found to be approximately 5-fold greater than that of PTH (1–34) (EC50 = ∼0.087 vs ∼0.44nM; P = .0009).
Substance Class Protein
Protein Type HORMONE
Protein Sub Type
Sequence Type COMPLETE
Record UNII
AVK0I6HY2U
Record Status Validated (UNII)
Record Version
Subunit 0