Abaloparatide

Abaloparatide Uses, Dosage, Side Effects, Food Interaction and all others data.

Abaloparatide is an analog of PTHrP (parathyroid hormone-related protein). It was approved in April 28, 2017 by the FDA (as Tymlos) for the treatment of postmenopausal women with osteoporosis at high risk for fracture. Abaloparatide is a synthetic peptide that is related to hPTHrP and has demonstrated in preclinical testing the potential to widen the anabolic window for bone therapeutics, stimulating bone formation with a limited effect on bone resorption and mineral mobilization. This could enable improved convenience over currently available anabolic therapies, resulting in greater compliance and, ultimately, greater benefit to patients.

Abaloparatide (BA058), a proprietary analog of human parathyroid hormone-related protein (hPTHrP), is currently undergoing clinical trials by the company for the treatment of osteoporosis in postmenopausal women. PTHrP is a critical peptide for promoting new bone formation, with a distinct role from parathyroid hormone, or PTH, which primarily regulates calcium homeostasis and bone resorption. Clinical studies show increased bone mineral density (BMD) and levels of bone formation markers in a dose-response relationship.

Abaloparatide
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Abaloparatide
Availability	Prescription only
Generic	Abaloparatide
Abaloparatide Other Names	Abaloparatide
Related Drugs	Prolia, hydrochlorothiazide, alendronate, calcitonin, Fosamax, Tymlos
Weight	3120mcg/1.56ml,
Type	Subcutaneous Solution, Subcutaneous
Formula	C₁₇₄H₃₀₀N₅₆O₄₉
Weight	3961.0 Da
Protein binding	In vitro plasma protein binding is approximately 70%.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Abaloparatide is a parathyroid hormone-related protein (PTHrP) analog used for the treatment of osteoporosis in postmenopausal women with a high risk of fracture.

Investigated for use/treatment in postmenopausal osteoporosis to reduce vertebral and/or non-vertebral fractures.

Abaloparatide is also used to associated treatment for these conditions: High risk of fracture Osteoporosis

How Abaloparatide works

In target cells, abaloparatide acts as an agonist on PTH type 1 receptor (PTH1R) and activates both G protein–mediated cAMP signaling and β-arrestin-mediated ERK-1/2 signaling pathways with similar potency [A19105]. Abaloparatide binds to RG conformation of PTH1R with greater selectivity that results in more transient cell signalling responses.

Toxicity

Abaloparatide has shown to induce higher incidences of osteosarcoma in a dose-dependent manner in a 2 year carcinogenicity study with female and male rats. This correlation is not known to be reflected in humans, however patients with increased risk of osteosarcoma including Paget's disease, open epiphyses, and skeletal malignancies should avoid this treatment. Abaloparatide may also cause hypercalcemia so should be avoided in patients with pre-existing conditions of primary hyperthyroidism or hypercalcemia. Overdose is commonly associated with hypercalcemia, nausea, vomiting, dizziness, tachycardia, orthostatic hypotension and headache. There is no known antidote for abaloparatide.

Food Interaction

Administer vitamin supplements. If dietary intake is inadequate, patients should receive supplemental calcium and vitamin D.
Take at the same time every day.
Take with or without food.

Abaloparatide Disease Interaction

Major: hyperparathyroidism, malignancyModerate: urolithiasis

Volume of Distribution

Vd is approximately 50L.

Elimination Route

The time it takes to reach peak concentration following subcutaneous administration of 80 mcg abaloparatide ranges from 0.25 to 0.52 hr, with the median time of 0.51hr. The bioavailability in healthy women is 36% following administration.

Half Life

The mean (SD) half-life if 1.7 (0.7) hrs.

Elimination Route

Metabolized products are mainly eliminated via renal excretion. Patients with severe renal impairment should be monitored with increased risk of adverse effects however there are no recommended dosage adjustments in patients with mild, moderate or severe renal impairment.