Abaloparatide

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.

• TYMLOS is a human parathyroid hormone related peptide [PTHrP(1-34)] analog indicated for the: Treatment of postmenopausal women with osteoporosis at high risk for fracture or patients who have failed or are intolerant to other available osteoporosis therapy. ( 1.1 ) Treatment to increase bone density in men with osteoporosis at high risk for fracture or patients who have failed or are intolerant to other available osteoporosis therapy.ICD-10: M81.0

• TYMLOS is contraindicated in patients with a history of systemic hypersensitivity to abaloparatide or to any component of the product formulation. Reactions have included anaphylaxis, dyspnea, and urticaria [see Adverse Reactions ( 6.2 )] .contraindicated

Recommended dosage is 80 mcg subcutaneously once daily; patients should receive supplemental calcium and vitamin D if dietary intake is inadequate. ( 2.1 ) Administer as a subcutaneous injection into periumbilical region of abdomen. ( 2.2 ) Administer initially where the patient can sit or lie down in case symptoms of orthostatic hypotension occur. ( 2.2 , 5.2 ) 2.1 Recommended Dosage The recommended dosage of TYMLOS is 80 mcg administered subcutaneously once daily. Patients should receive supplemental calcium and vitamin D if dietary intake is inadequate. 2.2 Administration Instructions Administer TYMLOS as a subcutaneous injection 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. Administer the first several doses where the patient can sit or lie down if necessary, in case symptoms of orthostatic hypotension occur [see Warnings and Precautions ( 5.2 ) and Adverse Reactions ( 6.1 )] . Visually inspect TYMLOS for particulate matter and discoloration prior to administration. TYMLOS is a clear and colorless solution. Do not use if solid particles appear or if the solution is cloudy or colored. Provide appropriate training and instruction to patients and caregivers on the proper use of the TYMLOS pen. 2.3 Treatment Duration The safety and efficacy of TYMLOS have not been evaluated beyond 2 years of treatment. Use of the drug for more than 2 years during a patient's lifetime is not recommended.

Osteosarcoma: Avoid use in patients with increased risk of osteosarcoma including patients with open epiphyses, metabolic bone diseases including Paget's disease, bone metastases or history of skeletal malignancies, prior external beam or implant radiation therapy involving the skeleton, and hereditary disorders predisposing to osteosarcoma. ( 5.1 ) Orthostatic Hypotension: Instruct patients to sit or lie down if symptoms develop after dose administration. ( 5.2 ) Hypercalcemia: Avoid use in patients with pre-existing hypercalcemia and those known to have an underlying hypercalcemic disorder, such as primary hyperparathyroidism. ( 5.3 ) Hypercalciuria and Urolithiasis: Monitor urine calcium if pre-existing hypercalciuria or active urolithiasis are suspected. ( 5.4 ) 5.1 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 to 28 times the human exposure at the clinical dose of 80 mcg [see Nonclinical Toxicology ( 13.1 )] . It is unknown whether TYMLOS will cause osteosarcoma in humans. Osteosarcoma has been reported in patients treated with a PTH-analog in the post marketing setting; however, an increased risk of osteosarcoma has not been observed in observational studies in humans. There are limited data assessing the risk of osteosarcoma beyond 2 years of TYMLOS and/or use of a PTH-analog [see Dosage and Administration ( 2.3 ) and Nonclinical Toxicology ( 13.1 )] .

The following adverse reactions are described in greater detail in other sections: Orthostatic Hypotension [see Warnings and Precautions ( 5.2 )] Hypercalcemia [see Warnings and Precautions ( 5.3 )] Hypercalciuria and Urolithiasis [see Warnings and Precautions ( 5.4 )] Osteoporosis in postmenopausal women: The most common adverse reactions (incidence ≥2%) are hypercalciuria, dizziness, nausea, headache, palpitations, fatigue, upper abdominal pain, and vertigo. ( 6.1 ) Osteoporosis in men: The most common adverse reactions (incidence ≥2%) are injection site erythema, dizziness, arthralgia, injection site swelling, injection site pain, contusion, nausea, diarrhea, abdominal distension, abdominal pain, and bone pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Radius Health, Inc. at 1-855-672-3487 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice.

8.1 Pregnancy Risk Summary TYMLOS is not indicated for use in females of reproductive potential. There are no human data with TYMLOS use in pregnant women to inform any drug associated risks. Animal reproduction studies with abaloparatide have not been conducted. 8.2 Lactation Risk Summary TYMLOS 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. 8.4 Pediatric Use Safety and effectiveness of TYMLOS have not been established in pediatric patients. TYMLOS 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 [see Warnings and Precautions ( 5.1 )] . 8.5 Geriatric Use Of the total number of patients in the postmenopausal osteoporosis clinical studies of TYMLOS, 82% were age 65 years and over, and 19% were age 75 years and over. In the male osteoporosis study, 74% were age 65 years and over and 23% were age 75 years or 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.

Metabolism

Following seven days of subcutaneous administration of abaloparatide 80 mcg, the mean (SD) abaloparatide exposure was 812 (118) pg/mL for C max and 1622 (641) pg∙hr/mL for AUC 0–24 in postmenopausal women with osteoporosis. Absorption The median (range) time to peak concentration of abaloparatide 80 mcg was 0.51 hr (0.25 to 0.52 hr) following subcutaneous administration.

In a clinical study, accidental overdose was reported in a patient who received 400 mcg in one day (5 times the recommended clinical dose); dosing was temporarily interrupted. The patient experienced asthenia, headache, nausea, and vertigo. Serum calcium was not assessed on the day of the overdose, but on the following day the patient's serum calcium was within the normal range. The effects of overdose may include hypercalcemia, nausea, vomiting, dizziness, tachycardia, orthostatic hypotension, and headache. Overdos age Management There is no specific antidote for TYMLOS. Treatment of suspected overdose should include discontinuation of TYMLOS, monitoring of serum calcium and phosphorus, and implementation of appropriate supportive measures, such as hydration. Based on the molecular weight, plasma protein binding and volume of distribution, abaloparatide is not expected to be dialyzable.

• Apr 28, 2017NDANDA208743Radius

1. 1Headache4,23817%
2. 2Nausea3,28113%
3. 3Dizziness3,18513%
4. 4Fatigue2,77911%
5. 5Heart Rate Increased2,1768.7%
6. 6Product Dose Omission Issue2,1758.7%
7. 7Arthralgia1,8597.4%
8. 8Palpitations1,8197.3%
9. 9Bone Pain1,4445.8%
10. 10Back Pain1,3105.2%
11. 11Pain1,2915.2%
12. 12Injection Site Bruising9843.9%
13. 13Pain In Extremity9743.9%
14. 14Product Quality Issue9153.7%
15. 15Injection Site Pain8613.4%

The 10 most recently updated of 25 ClinicalTrials.gov registrations naming Abaloparatide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Abaloparatide Added to Ongoing Denosumab vs Continued Denosumab Alone
  Active not recruiting · Phase 4 · Interventional · 70 enrolled · Hospital for Special Surgery, New York
  NCT04467983updated 2026-06-08
• Abaloparatide Before Total Knee Arthroplasty
  Completed · Phase 4 · Interventional · 58 enrolled · University of Wisconsin, Madison
  NCT04167163updated 2026-06-05
• MicroRNA and Markers and Therapeutic Response to Romosozumab and Abaloparatide in Postmenopausal Osteoporosis
  Recruiting · Interventional · 42 enrolled · Istituto Auxologico Italiano
  NCT07616401updated 2026-06-01
• The Effect of Osteoporotic Medications on Vertebral Bone Quality Score
  Not yet recruiting · Phase 2 · Interventional · 60 enrolled · State University of New York at Buffalo
  NCT07587775updated 2026-05-14
• Abaloparatide vs. Placebo in Post-Menopausal Women and Abaloparatide in Men Receiving Initial Spinal Fusion Surgery
  Active not recruiting · Phase 2 · Interventional · 96 enrolled · Hospital for Special Surgery, New York
  NCT03841058updated 2026-04-28
• Sequential Therapies After Osteoanabolic Treatment
  Recruiting · Observational · 150 enrolled · 424 General Military Hospital
  NCT06164795updated 2025-04-27
• To Evaluate the Efficacy and Safety of Abaloparatide Injection (QLG2128) in the Treatment of Postmenopausal Women With Osteoporosis and at High Risk of Fracture
  Not yet recruiting · Phase 3 · Interventional · 282 enrolled · Qilu Pharmaceutical Co., Ltd.
  NCT06898060updated 2025-03-27
• A Single-center, Open, Randomized, Single-dose, Cross-over Bioequivalence Study to Evaluate the Effects of the Test Formulation Abalparatide Injection and the Reference Formulation Abalparatide Injection (Tymlos®) in Healthy Adult Subjects
  Not yet recruiting · Phase 1 · Interventional · 32 enrolled · The Affiliated Hospital of Qingdao University
  NCT06753864updated 2024-12-31
• PTH Analog Type II Odontoid Fracture
  Terminated · Phase 2 · Interventional · 22 enrolled · David Lunardini
  NCT04760782updated 2024-09-19
• Abaloparatide and Pelvic Fracture Healing
  Completed · Phase 2 · Interventional · 48 enrolled · Hospital for Special Surgery, New York
  NCT04249232updated 2024-06-14

Frequently asked questions

How does Abaloparatide work?

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.

What is Abaloparatide used for?

According to FDA labeling, Abaloparatide carries indications including: TYMLOS is a human parathyroid hormone related peptide [PTHrP(1-34)] analog indicated for the: Treatment of postmenopausal women with osteoporosis at high risk for fracture or patients who have failed or are intolerant to other available osteoporosis therapy. ( 1.1 ) Treatment to increase bone density in men with osteoporosis at high risk for fracture or patients who have failed or are intolerant to other available osteoporosis therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Abaloparatide?

Abaloparatide is classified as Parathyroid hormones and analogues, Parathyroid Hormone-Related Peptide Analog, Parathormone Receptor Agonists, Bone Formation Stimulation, Bone Resorption Stimulation.

What are the brand names for Abaloparatide?

Abaloparatide is marketed under brand names including Tymlos.

What are the contraindications for Abaloparatide?

Abaloparatide labeling lists contraindications including: TYMLOS is contraindicated in patients with a history of systemic hypersensitivity to abaloparatide or to any component of the product formulation. Reactions have included anaphylaxis, dyspnea, and urticaria [see Adverse Reactions ( 6.2 )] .. Always consult the full prescribing information and a clinician.