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Abaloparatide

Abaloparatide (brand name Tymlos).

Abaloparatide is a parathyroid hormone-related protein (PTHrP) analog drug used to treat osteoporosis. 

 

 

It is approved to treat postmenopausal osteoporosis.

Indication: to treat postmenopausal women with osteoporosis who are at high risk of bone fractures.

 

 

It an anabolic bone agent.

 

It is 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. 

It  preferentially binds the PTH1R, which  elicits a transient downstream cyclic AMP signaling response towards to a more anabolic signaling pathway.

Studies show increased cortical and trabecular bone volume and density, and trabecular microarchitecture improvement in vertebral and nonvertebral bones after short-term and long-term daily subcutaneous injection compared to controls. 

There is a dose-dependent increased in bone mass and strength in long-term treatment but also found that prolonged abalorapatide-SC treatment leads to increased incidence of osteosarcoma.

No present evidence for increased risk of bone tumors due to prolonged systemic administration.

Use is not advised the use for more than 2 years, or in patients with history of Paget disease and/or other conditions that exacerbates the risk of developing osteosarcoma.

 

 

Pregnancy category US: N (Not classified yet)

Like the related drug teriparatide, and unlike bisphosphonates, it is an anabolic agent.

A subcutaneous injection formulation.

Approved by Food and drug administration (FDA) to treat postmenopausal osteoporosis.

Abaloparatide is indicated to treat postmenopausal women with osteoporosis who are more susceptible to bone fractures.

The dose recommended is 80mcg subcutaneous injection once a day, administered in the periumbilical area using a prefilled pen device containing 30 doses.

Preclinical studies revealed that abaloparatide systemic daily administration leads to a dose- and time-dependent increase in the incidence of osteosarcoma in rodents.

Whether abaloparatide-SC will cause osteosarcoma in humans is unknown.

Use of abaloparatide is not recommended for individuals at increased risk of osteosarcoma, and it is not advised for more than 2 years during a patient’s lifetime.

The most common side effects reported by more than 2% of clinical trials subjects are hypercalciuria, dizziness, nausea, headache, palpitations, fatigue, upper abdominal pain and vertigo.

A 34 amino acid synthetic analog of PTHrP. 

It has 41% homology to parathyroid hormone (PTH) (1-34) and 76% homology to parathyroid hormone-related protein (PTHrP).

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.

Studies indicate a dose-dependent increased in bone mass and strength in long-term abalorapatide treatment.

Abaloparatide showed superior anabolic effects on the hips compared to teriparatide.

In the phase III Abaloparatide Comparator Trial in Vertebral Endpoints (ACTIVE) trial, a 18-months randomized, multicenter, double-blinded, placebo-controlled study evaluated the long-term efficacy of abaloparatide compared to placebo and teriparatide in 2,463 postmenopausal women.

In the aboove study Women who received daily injections of abaloparatide experienced substantial reduction in the incidence of fractures compared to placebo, and a greater BMD increase at 6, 12 and 18 months in spinal, hips and femoral bones was observed in abaloparatide compared to placebo and teriparatide-treated subjects.

Combined abaloparatide and alendronate therapy reduce significantly the incidence of vertebral and nonvertebral fractures.

Phase II trials initiated in a 24-week randomized trial  in postmenopausal women with osteoporosis assessing bone mass density (BMD): changes as the increase at doses of 40 and 80 mcg were found in the lumbar spine, femur and hips of abaloparatide-treated participants compared to placebo. 

 

 

It showed superior anabolic effects on the hips compared to teriparatide.

 

 

Combined abaloparatide and alendronate therapy reduce significantly the incidence of vertebral and nonvertebral fractures.

 

One reply on “Abaloparatide”

Thanks for pointing out that Abaloparatide is a parathyroid hormone-related protein analog drug used to treat osteoporosis. My mother has been suffering from osteoporosis. I guess I should look for a clinic on Monday that can provide Abaloparatide injection to treat osteoporosis at high risk for fracture.

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