Abaloparatide

Abaloparatide (Tymlos) — PTHrP-Based Anabolic Peptide

Evidence & Status

  • FDA Approved
  • Strong Human Evidence
  • Strong

FDA Approval Scope

TYMLOS is approved for postmenopausal women and men with osteoporosis at high fracture risk or with appropriate treatment-failure/intolerance context; cumulative use beyond 2 years during a patient's lifetime is not recommended because safety and efficacy beyond 2 years have not been evaluated.

At a Glance

An FDA-approved synthetic 34-amino-acid PTHrP analogue used as TYMLOS for osteoporosis in eligible postmenopausal women and men. Strong evidence is specific to labeled osteoporosis use, not anti-aging.

Plain English

Abaloparatide is a prescription osteoporosis medicine designed to stimulate bone formation through the PTH1 receptor. The TYMLOS label covers eligible postmenopausal women and men with osteoporosis. Research and labeling for this osteoporosis use should not be generalized to longevity or healthy-person bone enhancement.

Overview

Abaloparatide is a synthetic 34-amino-acid analogue of human PTHrP(1-34) that activates the PTH1 receptor. TYMLOS is the specific U.S. product context: an anabolic osteoporosis treatment for postmenopausal women and men at high fracture risk or with appropriate treatment-failure/intolerance context. This record does not represent abaloparatide as an anti-aging or healthy-person bone-enhancement treatment.

Research Summary

The ACTIVE randomized trial included 2,463 postmenopausal women with osteoporosis and found lower vertebral and nonvertebral fracture incidence with abaloparatide than placebo. Those findings apply to the studied postmenopausal osteoporosis population; total trial enrollment must not be read as the abaloparatide treatment-arm size. Current TYMLOS labeling separately includes treatment to increase bone density in men with osteoporosis at high fracture risk or with appropriate treatment-failure/intolerance context. The strong evidence rating reflects established osteoporosis evidence and labeled use, not anti-aging.

Research Areas

  • Osteoporosis
  • Bone mineral density
  • Fracture prevention
  • PTH1R biased agonism
  • Anabolic bone therapy
  • Hypercalcemia risk reduction

Safety & Risks

Serious Risks

  • Abaloparatide caused a dose-dependent increase in osteosarcoma in rat studies; it is unknown whether TYMLOS causes osteosarcoma in humans, and observational studies with PTH analogues have not shown an increased human risk
  • Avoid use in patients at increased baseline risk of osteosarcoma, including patients with open epiphyses, metabolic bone diseases such as Paget’s disease, bone metastases or skeletal malignancies, prior skeletal radiation, or hereditary disorders predisposing to osteosarcoma
  • Orthostatic hypotension can occur, particularly with early doses
  • TYMLOS can cause hypercalcemia and is not recommended in patients with pre-existing hypercalcemia or underlying hypercalcemic disorders
  • Hypercalciuria and urolithiasis can occur; monitoring may be appropriate in patients with suspected hypercalciuria or active urolithiasis
  • TYMLOS is contraindicated in patients with a history of systemic hypersensitivity to abaloparatide or product components

Reported Side Effects

  • Hypercalciuria
  • Dizziness
  • Nausea
  • Headache
  • Palpitations
  • Fatigue
  • Upper abdominal pain
  • Vertigo
  • Injection site reactions
United States
FDA-approved as TYMLOS for postmenopausal women with osteoporosis at high fracture risk or who have failed or are intolerant to other available osteoporosis therapy, and to increase bone density in men with osteoporosis at high fracture risk or who have failed or are intolerant to other available osteoporosis therapy. Use for more than 2 years during a patient’s lifetime is not recommended because safety and efficacy beyond 2 years have not been evaluated.
United Kingdom
International regulatory status is not represented by the selected sources in this record.
Australia
International regulatory status is not represented by the selected sources in this record.
Canada
International regulatory status is not represented by the selected sources in this record.

Citations & Sources