Class: Parathyroid Agents
Warning: Risk Of Osteosarcoma1
See full prescribing information for complete boxed warning.1
Abaloparatide caused a dose-dependent increase in the incidence of osteosarcoma, a malignant bone tumor, in male and female rats. It is unknown whether abaloparatide will cause osteosarcoma in humans.1
Use of abaloparatide is not recommended in patients at increased risk for osteosarcoma.1
Cumulative use of abaloparatide and parathyroid hormone analogs (e.g., teriparatide) for more than 2 years during a patient’s lifetime is not recommended.1
Abaloparatide is a human parathyroid hormone related peptide [PTHrP(1-34)] analog.1
Uses for Abaloparatide
Abaloparatide has the following uses:
Abaloparatide is a PTHrP(1-34) analog indicated for the treatment of postmenopausal women with osteoporosis at high risk for fracture.1
Abaloparatide Dosage and Administration
Abaloparatide is available in the following dosage form(s) and strength(s):
Injection: 3120 mcg/1.56 mL (2000 mcg/mL) in a single-patient-use prefilled pen. The prefilled pen delivers 30 daily doses of 80 mcg abaloparatide in 40 mcL of sterile, clear, colorless solution.1
It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:
Recommended dose is 80 mcg subcutaneously once daily; patients should receive supplemental calcium and vitamin D if dietary intake is inadequate.1
Administer as a subcutaneous injection into periumbilical region of abdomen.1
Administer initially where the patient can sit or lie down in case symptoms of orthostatic hypotension occur.1
Cautions for Abaloparatide
Risk of Osteosarcoma
Abaloparatide caused a dose-dependent increase in the incidence of osteosarcoma in male and female rats after subcutaneous administration at exposures 4–28 times the human exposure at the clinical dose of 80 mcg. It is unknown whether abaloparatide will cause osteosarcoma in humans.1
The use of abaloparatide is not recommended in patients at increased risk of osteosarcoma including those with Paget's disease of bone or unexplained elevations of alkaline phosphatase, open epiphyses, bone metastases or skeletal malignancies, hereditary disorders predisposing to osteosarcoma, or prior external beam or implant radiation therapy involving the skeleton.1
Cumulative use of abaloparatide and parathyroid hormone analogs (e.g., teriparatide) for more than 2 years during a patient’s lifetime is not recommended. 1
Orthostatic hypotension may occur with abaloparatide, typically within 4 hours of injection. Associated symptoms may include dizziness, palpitations, tachycardia, or nausea, and may resolve by having the patient lie down. For the first several doses, abaloparatide should be administered where the patient can sit or lie down if necessary.1
Abaloparatide may cause hypercalcemia. Abaloparatide is not recommended in patients with pre-existing hypercalcemia or in patients who have an underlying hypercalcemic disorder, such as primary hyperparathyroidism, because of the possibility of exacerbating hypercalcemia.1
Hypercalciuria and Urolithiasis
Abaloparatide may cause hypercalciuria. It is unknown whether abaloparatide may exacerbate urolithiasis in patients with active or a history of urolithiasis. If active urolithiasis or pre-existing hypercalciuria is suspected, measurement of urinary calcium excretion should be considered.1
Abaloparatide is not indicated for use in females of reproductive potential. There are no human data with abaloparatide use in pregnant women to inform any drug-associated risks. Animal reproduction studies with abaloparatide have not been conducted.
Abaloparatide is not indicated for use in females of reproductive potential. There is no information on the presence of abaloparatide in human milk, the effects on the breastfed infant, or the effects on milk production.
Safety and effectiveness of abaloparatide have not been established in pediatric patients. Abaloparatide is not recommended for use in pediatric patients with open epiphyses or hereditary disorders predisposing to osteosarcoma because of an increased baseline risk of osteosarcoma.1
Of the total number of patients in the postmenopausal osteoporosis clinical studies of abaloparatide, 82% were age 65 years and over, and 19% were age 75 years and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, but greater sensitivity of some older individuals cannot be ruled out.1
No dosage adjustment is required for patients with mild, moderate, or severe renal impairment. A study of a single dose of abaloparatide 80 mcg given subcutaneously was conducted in subjects with normal renal function or mild, moderate, or severe renal impairment. The maximal concentration (Cmax) and area under the concentration-time curve (AUC) of abaloparatide increased 1.4- and 2.1-fold, respectively, in subjects with severe renal impairment, compared to subjects with normal renal function. Patients with severe renal impairment may have increased abaloparatide exposure that may increase the risk of adverse reactions; therefore, monitor for adverse reactions.1
Common Adverse Effects
The most common adverse reactions (incidence ≥2%) are hypercalciuria, dizziness, nausea, headache, palpitations, fatigue, upper abdominal pain, and vertigo.1
It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:
No specific drug-drug interaction studies have been performed.1
Mechanism of Action
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 bone mineral density (BMD) and bone mineral content (BMC) that correlated with increases in bone strength at vertebral and/or nonvertebral sites.1
Advice to Patients
Advise the patient to read the FDA-approved patient labeling.1
Risk of Osteosarcoma
Advise patients that abaloparatide caused a dose-dependent increase in the incidence of osteosarcoma in male and female rats and that it is unknown whether abaloparatide will cause osteosarcoma in humans.
Instruct patients to promptly report signs and symptoms of possible osteosarcoma such as persistent localized pain or occurrence of a new soft tissue mass that is tender to palpation.1
Advise patients that abaloparatide may cause hypercalcemia, and discuss the symptoms of hypercalcemia (e.g., nausea, vomiting, constipation, lethargy, muscle weakness).1
Instruct patients to promptly report signs and symptoms of hypercalcemia. 1
Advise patients to sit or lie down if they feel lightheaded or have palpitations after the injection until their symptoms resolve. If these symptoms persist or worsen, advise patients to consult their healthcare provider before continuing treatment.
Use of Abaloparatide Pen
Instruct patients and caregivers who administer abaloparatide on how to properly use the abaloparatide pen and to follow sharps disposal recommendations. Advise patients not to share their abaloparatide pen or needles with other patients and not to transfer the contents of the pen to a syringe.
Advise patients that each abaloparatide pen can be used for up to 30 days, and after the 30-day use period to discard the abaloparatide pen, even if it still contains unused solution.1
AHFS First Release. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
2000 mcg/1 mL
Radius Health Inc.
AHFS Drug Information. © Copyright 2018, Selected Revisions August 28, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. Radius Health, Inc.. Tymlos (abaloparatide) SUBCUTANEOUS prescribing information. 2017 Apr.
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- Drug class: parathyroid hormone and analogs
Other brands: Tymlos