Note: Assess serum calcium prior to initiation; avoid use in patients with preexisting hypercalcemia or hypercalcemic disorder. Correct vitamin D deficiency (eg, to a 25-hydroxyvitamin D level ≥20 ng/mL [≥50 nmol/L]) prior to initiating therapy and ensure adequate calcium and vitamin D intake during therapy; however, use caution to avoid hypercalcemia (ES [Eastell 2019]; NAMS 2021; Rosen 2021; manufacturer’s labeling).
Osteoporosis, postmenopausal, fracture risk reduction:
Note: For use as initial therapy in patients with very high fracture risk, including those with a T-score less than –3, a T-score less than –2.5 with fragility fracture history, or severe or multiple prior vertebral fractures. May also be used as an alternative agent in patients with high fracture risk in whom first-line therapies are ineffective or cannot be used (AACE/ACE [Camacho 2020]; ES [Eastell 2019]). Prior to use, evaluate and treat any potential causes of secondary osteoporosis (eg, severe vitamin D deficiency) (NOF [Cosman 2014]).
SUBQ: 80 mcg once daily.
Duration of therapy: Duration of abaloparatide (and/or teriparatide) therapy should not exceed 2 years due to limited data with use beyond this; fracture reduction efficacy has been demonstrated over a period of 18 months (Bone 2018; Miller 2016; manufacturer’s labeling).
Discontinuation/interruption of therapy: Following a course of abaloparatide, switch to antiresorptive therapy (eg, with a bisphosphonate or denosumab) to maintain bone density gains (ES [Eastell 2019]).
No dosage adjustment necessary.
There is no dosage adjustment provided in the manufacturer's labeling
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Pen-injector, Subcutaneous:
Tymlos: 3120 mcg/1.56 mL (1.56 mL) [contains phenol]
No
An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:
Tymlos: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/208743s009lbl.pdf#page=18
SUBQ: Inject subcutaneously into the periumbilical region of the abdomen. Rotate the site of the injection every day and administer at approximately the same time every day. Do not administer intravenously or intramuscularly. Initial doses should occur under circumstances in which the patient may sit or lie down, in the event of orthostasis.
Osteoporosis, postmenopausal, fracture risk reduction: Treatment of postmenopausal osteoporosis in patients who are at high risk for fracture. May also be used in patients in whom other available osteoporosis therapy has failed or cannot be taken.
Limitations of use: Cumulative lifetime duration of abaloparatide (and/or teriparatide) therapy should not exceed 2 years.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Endocrine & metabolic: Increased uric acid (25%)
Genitourinary: Hypercalciuria (11% to 20%)
Immunologic: Antibody development (49%; neutralizing antibodies: 68%; antibody formation was not found to have any clinical significance)
Local: Erythema at injection site (58%)
1% to 10%:
Cardiovascular: Orthostatic hypotension (1% to 4%), palpitations (5%), sinus tachycardia (≤2%), tachycardia (≤2%)
Endocrine & metabolic: Hypercalcemia (3%)
Gastrointestinal: Nausea (8%), upper abdominal pain (3%)
Local: Pain at injection site (9%), swelling at injection site (10%)
Nervous system: Dizziness (10%), fatigue (3%), headache (8%)
Postmarketing:
Dermatologic: Pruritus (including injection site pruritus), skin rash (including rash at injection site)
Gastrointestinal: Abdominal distension, abdominal pain, constipation, diarrhea, vomiting
Hypersensitivity: Hypersensitivity reaction, nonimmune anaphylaxis
Local: Bleeding at injection site, bruising at injection site
Nervous system: Insomnia, lethargy, malaise, pain
Neuromuscular & skeletal: Arthralgia, asthenia, limb pain, muscle spasm (leg and back), ostealgia
Respiratory: Dyspnea
Hypersensitivity (eg, anaphylaxis, dyspnea, urticaria) to abaloparatide or any component of the formulation.
Concerns related to adverse effects:
• Hypercalcemia: May cause or exacerbate hypercalcemia; use is not recommended in patients with preexisting hypercalcemia or with an underlying hypercalcemic disorder (eg, primary hyperparathyroidism).
• Orthostatic hypotension: May cause orthostatic hypotension. Transient orthostatic hypotension usually occurs within 4 hours of dosing.
• Osteosarcoma: In animal studies, abaloparatide has been associated with an increase in osteosarcoma; risk was dependent on both dose and duration. Avoid use in patients with an increased risk of osteosarcoma (including Paget disease, bone metastases or skeletal malignancies, hereditary disorders predisposing to osteosarcoma, prior external beam or implant radiation therapy involving the skeleton, or in patients with open epiphyses).
Disease-related concerns:
• Urolithiasis: Use may cause hypercalciuria; use with caution in patients with active or recent urolithiasis because of risk of exacerbation.
None known.
There are no known significant interactions.
Abaloparatide is not indicated for use in females of reproductive potential. Animal reproduction studies have not been conducted.
It is not known if abaloparatide is present in breast milk. Abaloparatide is not indicated for use in females of reproductive potential.
Ensure adequate calcium and vitamin D intake; if dietary intake is inadequate, dietary supplementation is recommended. Patients should consume:
Calcium: 1,000 mg/day (males: 50 to 70 years of age) or 1,200 mg/day (females ≥51 years of age and males ≥71 years of age) (IOM 2011; NOF [Cosman 2014]).
Vitamin D: 800 to 1,000 units/day (age ≥50 years) (NOF [Cosman 2014]). Recommended dietary allowance (RDA): 600 units/day (age ≤70 years) or 800 units/day (age ≥71 years) (IOM 2011).
Orthostatic hypotension; serum calcium; urinary calcium (patients with suspected active urolithiasis or preexisting hypercalciuria).
Bone mineral density (BMD) should be evaluated at baseline and ~1 to 2 years following initiation of therapy (AACE/ACE [Camacho 2020]; ES [Eastell 2019]; NOF [Cosman 2014]); may consider monitoring biochemical markers of bone turnover (eg, serum P1NP) at baseline, 3 months, and 6 months, to assess treatment response (ES [Eastell 2019]; Miller 2016).
Abaloparatide is an analog of human parathyroid hormone related peptide (PTHrP[1-34]), which acts as an agonist at the PTH1 receptor (PTH1R). This results in stimulation of osteoblast function and increased bone mass (Harslof 2016; Leder 2017).
Distribution: Vd: ~50 L
Protein binding: ~70%
Metabolism: Hepatic (nonspecific proteolysis)
Bioavailability: 36%
Half-life elimination: 1.7 hours
Time to peak: 0.51 hours (range: 0.25 to 0.52 hours)
Excretion: Urine (as peptide fragments)
Altered kidney function: Maximum serum concentration increased 1-, 1.3- and 1.4-fold in patients with mild, moderate and severe renal impairment, respectively. AUC increased 1.2-, 1.7- and 2.1-fold in patients with mild, moderate and severe renal impairment, respectively.
Solution Pen-injector (Tymlos Subcutaneous)
3120MCG/1.56ML (per mL): $1,761.03
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