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Abaloparatide: Drug information

Abaloparatide: Drug information
(For additional information see "Abaloparatide: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Tymlos
Pharmacologic Category
  • Parathyroid Hormone Analog
Dosing: Adult

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

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]).

Dosing: Kidney Impairment: Adult

No dosage adjustment necessary.

Dosing: Hepatic Impairment: Adult

There is no dosage adjustment provided in the manufacturer's labeling

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

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]

Generic Equivalent Available: US

No

Medication Guide and/or Vaccine Information Statement (VIS)

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

Administration: Adult

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.

Use: Labeled Indications

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.

Adverse Reactions

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

Contraindications

Hypersensitivity (eg, anaphylaxis, dyspnea, urticaria) to abaloparatide or any component of the formulation.

Warnings/Precautions

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.

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Pregnancy Considerations

Abaloparatide is not indicated for use in females of reproductive potential. Animal reproduction studies have not been conducted.

Breastfeeding Considerations

It is not known if abaloparatide is present in breast milk. Abaloparatide is not indicated for use in females of reproductive potential.

Dietary Considerations

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).

Monitoring Parameters

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).

Mechanism of Action

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).

Pharmacokinetics

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)

Pharmacokinetics: Additional Considerations

Renal function impairment: 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.

Pricing: US

Solution Pen-injector (Tymlos Subcutaneous)

3120MCG/1.56ML (per mL): $1,761.03

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

  1. Bone HG, Cosman F, Miller PD, et al. ACTIVExtend: 24 months of alendronate after 18 months of abaloparatide or placebo for postmenopausal osteoporosis. J Clin Endocrinol Metab. 2018;103(8):2949-2957. [PubMed 29800372]
  2. Camacho PM, Petak SM, Binkley N, et al. American Association of Clinical Endocrinologists and American College of Endocrinology clinical practice guidelines for the diagnosis and treatment of postmenopausal osteoporosis–2020 update. Endocr Pract. 2020;26(suppl 1):1-46. doi:10.4158/GL-2020-0524SUPPL [PubMed 32427503]
  3. Cosman F, de Beur SJ, LeBoff MS, et al; National Osteoporosis Foundation. Clinician's guide to prevention and treatment of osteoporosis. Osteoporos Int. 2014;25(10):2359-2381. doi:10.1007/s00198-014-2794-2 [PubMed 25182228]
  4. Eastell R, Rosen CJ, Black DM, Cheung AM, Murad MH, Shoback D. Pharmacological management of osteoporosis in postmenopausal women: an Endocrine Society clinical practice guideline. J Clin Endocrinol Metab. 2019;104(5):1595-1622. doi:10.1210/jc.2019-00221 [PubMed 30907953]
  5. Harsløf T, Langdahl BL. New horizons in osteoporosis therapies. Curr Opin Pharmacol. 2016;28:38-42. doi:10.1016/j.coph.2016.02.012 [PubMed 26989807]
  6. IOM (Institute of Medicine). Dietary Reference Intakes for Calcium and Vitamin D. The National Academies Press; 2011.
  7. Leder BZ. Parathyroid hormone and parathyroid hormone-related protein analogs in osteoporosis therapy. Curr Osteoporos Rep. 2017;15(2):110-119. doi:10.1007/s11914-017-0353-4 [PubMed 28303448]
  8. Miller PD, Hattersley G, Riis BJ, et al; ACTIVE Study Investigators. Effect of abaloparatide vs placebo on new vertebral fractures in postmenopausal women with osteoporosis: a randomized clinical trial. JAMA. 2016;316(7):722-733. doi:10.1001/jama.2016.11136 [PubMed 27533157]
  9. North American Menopause Society. Management of osteoporosis in postmenopausal women: the 2021 position statement of The North American Menopause Society. Menopause. 2021;28(9):973-997. doi:10.1097/GME.0000000000001831 [PubMed 34448749]
  10. Rosen HN, Drezner MK. Overview of the management of osteoporosis in postmenopausal women. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed November 4, 2021.
  11. Tymlos (abaloparatide) [prescribing information]. Boston, MA: Radius Health Inc; December 2021.
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