Approved & therapeutic
Abaloparatide
Tymlos
Abaloparatide is a synthetic analog of parathyroid hormone-related protein (1-34), given by daily subcutaneous injection. In the US it is approved for the treatment of postmenopausal women with osteoporosis at high risk for fracture, and to increase bone density in men with osteoporosis at high risk for fracture — in each case including patients who have failed or are intolerant to other available osteoporosis therapy. Note that the men's indication is worded as a bone density indication, not a fracture reduction one. Like teriparatide, it is an anabolic bone agent.
- Status
- Abaloparatide is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- About 1 hour.
- How it's taken
- Subcutaneous injection
- Mechanism
- Other
- Pathways
- PTH1 receptor
How Abaloparatide works
Abaloparatide is a PTHrP(1-34) analog that acts as an agonist at the PTH1 receptor, activating cAMP signalling and stimulating new bone formation. It is described as favouring the RG conformation of the receptor, producing a shorter signalling episode than teriparatide, which has been proposed to explain differences in bone resorption markers and calcium handling. Whether that translates into a clinical advantage has not been established.
What research has looked at
- In the pivotal 18-month ACTIVE trial (2,463 participants) in postmenopausal women, abaloparatide produced an 86 percent relative reduction in new vertebral fractures versus placebo, which was the primary endpoint.
- Nonvertebral fracture risk reduction of roughly 43 percent versus placebo (2.7 percent versus 4.7 percent, measured over the 18 months of treatment plus a 1-month follow-up period with no drug) was reported as a secondary endpoint, not the primary one.
- Bone mineral density increased at the lumbar spine, total hip and femoral neck versus placebo.
- ACTIVE included an open-label teriparatide arm, but the trial was designed to compare abaloparatide with placebo; superiority over teriparatide for fracture reduction was not established.
- The indication in men was based on bone mineral density change rather than on fracture outcomes.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- Contraindicated in patients with known hypersensitivity to abaloparatide or any component; reported reactions have included anaphylaxis, dyspnea and urticaria.
- Risk of osteosarcoma: the label directs avoiding use in patients at increased baseline risk, including those with open epiphyses, metabolic bone disease such as Paget's disease, bone metastases or a history of skeletal malignancy, prior external beam or implant radiation involving the skeleton, and hereditary disorders predisposing to osteosarcoma. Patients are told to report persistent localized bone pain or a new tender soft tissue mass.
- Orthostatic hypotension, which may occur after a dose; the label directs sitting or lying down if symptoms develop.
- Hypercalcemia: the label directs avoiding use in patients with pre-existing hypercalcemia or an underlying hypercalcemic disorder such as primary hyperparathyroidism.
- Hypercalciuria and urolithiasis.
- Common reactions in postmenopausal women were hypercalciuria (11 percent), dizziness (10 percent), nausea (8 percent), headache (8 percent) and palpitations (5 percent); in men, injection site erythema (13 percent), dizziness (9 percent), arthralgia (7 percent), injection site swelling (7 percent) and injection site pain (6 percent).
- The osteosarcoma Boxed Warning was removed from this label effective December 2021; the current US label has no Boxed Warning section.
Sources
- PubMed research on Abaloparatide · NIH · National Library of Medicine
- DrugBank record for Abaloparatide · DrugBank
- Active clinical trials for Abaloparatide · U.S. National Library of Medicine
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Abaloparatide FAQ
What is Abaloparatide?
Abaloparatide is a synthetic analog of parathyroid hormone-related protein (1-34), given by daily subcutaneous injection. In the US it is approved for the treatment of postmenopausal women with osteoporosis at high risk for fracture, and to increase bone density in men with osteoporosis at high risk for fracture — in each case including patients who have failed or are intolerant to other available osteoporosis therapy. Note that the men's indication is worded as a bone density indication, not a fracture reduction one. Like teriparatide, it is an anabolic bone agent.
How does Abaloparatide work?
Abaloparatide is a PTHrP(1-34) analog that acts as an agonist at the PTH1 receptor, activating cAMP signalling and stimulating new bone formation. It is described as favouring the RG conformation of the receptor, producing a shorter signalling episode than teriparatide, which has been proposed to explain differences in bone resorption markers and calcium handling. Whether that translates into a clinical advantage has not been established.
Is Abaloparatide FDA approved?
Yes. Abaloparatide is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Abaloparatide?
Reported half-life: About 1 hour.
How is Abaloparatide taken?
Subcutaneous injection.
What side effects have been reported with Abaloparatide?
Reported in the sources: Contraindicated in patients with known hypersensitivity to abaloparatide or any component; reported reactions have included anaphylaxis, dyspnea and urticaria; Risk of osteosarcoma: the label directs avoiding use in patients at increased baseline risk, including those with open epiphyses, metabolic bone disease such as Paget's disease, bone metastases or a history of skeletal malignancy, prior external beam or implant radiation involving the skeleton, and hereditary disorders predisposing to osteosarcoma. Patients are told to report persistent localized bone pain or a new tender soft tissue mass; Orthostatic hypotension, which may occur after a dose; the label directs sitting or lying down if symptoms develop; Hypercalcemia: the label directs avoiding use in patients with pre-existing hypercalcemia or an underlying hypercalcemic disorder such as primary hyperparathyroidism; Hypercalciuria and urolithiasis; Common reactions in postmenopausal women were hypercalciuria (11 percent), dizziness (10 percent), nausea (8 percent), headache (8 percent) and palpitations (5 percent); in men, injection site erythema (13 percent), dizziness (9 percent), arthralgia (7 percent), injection site swelling (7 percent) and injection site pain (6 percent); The osteosarcoma Boxed Warning was removed from this label effective December 2021; the current US label has no Boxed Warning section.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.