Tymlos abaloparatide 3.12 mg/1.56mL Injection, Solution, 1 cartridge
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Parathyroid Hormone-Related Peptide Analog class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
Abaloparatide injection is used to treat osteoporosis (condition in which the bones become thin and weak and break easily) in women who have undergone menopause ('change in life,' end of menstrual periods), who are at high risk of fractures (broken bones) (history of fracture from osteoporosis or multiple risk factors for fracture) or who have failed or not tolerated other medications. Abaloparatide injection is also used to treat osteoporosis in men who are at high risk of fracture or who have failed or not tolerated other medications. Abaloparatide injection contains a synthetic form of a na...
Read the full MedlinePlus article ↗- Tymlos works differently from most osteoporosis medications. Instead of just slowing bone loss, it actually stimulates your bone-building cells to form new bone — making your bones...
- What exactly is Tymlos supposed to do for my bones?
- You inject Tymlos just under the skin in the belly area around your navel, once a day. Try to do it at roughly the same time each day, but it doesn't have to be tied to meals. Rota...
- How do I take it, and does it have to be at a specific time of day?
Patient education
Supplement & herbal interactions
Where does this data come from?
Ask a licensed pharmacist directly — free, answered by our team.
🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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1.2 mg / 1.56 mL
UNII Q40Q9N063P
Acetic acid is a weak organic acid commonly used in medicines as a buffer and pH adjuster. It helps maintain the proper acidity level to ensure the drug remains stable and effective in its formulation.
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7.8 mg / 1.56 mL
UNII 339NCG44TV
Phenol is a chemical compound derived from coal tar or petroleum. It serves as a preservative and antimicrobial agent in medicines, helping prevent bacterial and fungal growth to keep the product stable and safe during storage.
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7.92 mg / 1.56 mL
UNII 4550K0SC9B
Sodium acetate is a salt derived from acetic acid. It acts as a buffer to help maintain the medicine's pH stability and may serve as a preservative or solubilizer in liquid formulations.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
4 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $1,646.360 | $2,568.32 / 1.56 ml |
| Medicaid paysCMS SDUD · 12 mo | $1,789.85 | $2,792.17 / 1.56 ml |
| Medicare drug plans payPart D · Q2 2026 | $1,871.16 | $2,919.01 / 1.56 ml |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Tymlos 3.12 mg/1.56mLthis 70539-0001-02 | Radius | 1 cartridge | $1,646.360 | — | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Patent | Type | Use code | Expires |
|---|---|---|---|
| US 11680942 ↗ | Method of use | U-3322 | Jan 10, 2040 |
| US 8748382 ↗ | Method of use | U-3543 | Oct 3, 2027 |
| US 8748382 ↗ | Method of use | U-2009 | Oct 3, 2027 |
| US 11782041 ↗ | Method of use | U-2009 | Apr 30, 2038 |
| US 11782041 ↗ | Method of use | U-3543 | Apr 30, 2038 |
| US 7803770 ↗ | Method of use | U-2009 | Apr 28, 2031 |
| US RE49444 ↗ | Method of use | U-2009 | Apr 28, 2031 |
| US RE49444 ↗ | Method of use | U-3543 | Apr 28, 2031 |
| US 11255842 ↗ | Method of use | U-3322 | Jan 10, 2040 |
| US 8148333 ↗ | Drug product | — | Nov 8, 2027 |
| US 11977067 ↗ | Drug product | — | Apr 30, 2038 |
| US 10996208 ↗ | Drug product | — | Apr 30, 2038 |
Is there a generic version of TYMLOS 80 MCG DOSE PEN INJECTR?
The FDA approved a generic — why can’t I get it at my pharmacy yet?
Why do different websites show different generic release dates?
What does “FDA listed” mean?
What does a patent or protection date mean here?
What does “current Orange Book estimate” mean?
Can a generic come out before the last patent expires?
Can a generic come out after the listed dates?
What is the difference between patents and exclusivity?
Why are there multiple patent dates?
Where does this data come from?
🗺️ Medicaid utilization & spend
💊 Medicaid utilization by pack size
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Per unit | Per pack | Marketing start | Status |
|---|---|---|---|---|---|
| 70539-0001-02 You're viewing this | 1 CARTRIDGE in 1 BOX, UNIT-DOSE (70539-001-02) / 1.56 mL in 1 CARTRIDGE (70539-001-01) | $1,646.36 / mL | $2,568.32 | 2017-05-01 | Active |
| 70539-0001-98 | 1 CARTRIDGE in 1 BOX, UNIT-DOSE (70539-001-98) / 1.56 mL in 1 CARTRIDGE (70539-001-99) | — | — | 2017-05-01 | Active |
In Medicaid, this is the most-dispensed pack of this product — about 100% of fills over the last four reported quarters. See all packs ↓
Pack size FAQ
What quantity is in NDC 70539-0001-02?
What is the difference between NDC 70539-0001-02 and NDC 70539-0001-98?
What NDC number is used to bill for this package of Tymlos abaloparatide 3.12 mg/1.56mL Injection, Solution?
Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE 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. ( 1.2 )
1.1Treatment of Postmenopausal Women with Osteoporosis at High Risk for Fracture TYMLOS is indicated for the treatment of postmenopausal women with osteoporosis at high risk for fracture (defined as a history of osteoporotic fracture or multiple risk factors for fracture), or patients who have failed or are intolerant to other available osteoporosis therapy. In postmenopausal women with osteoporosis, TYMLOS reduces the risk of vertebral fractures and nonvertebral fractures.
1.2Treatment to Increase Bone Density in Men with Osteoporosis at High Risk for Fracture TYMLOS is indicated to increase bone density in men with osteoporosis at high risk for fracture (defined as a history of osteoporotic fracture or multiple risk factors for fracture), or patients who have failed or are intolerant to other available osteoporosis therapy.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION 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 , 5.3 )
2.1Recommended 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.
2.2Administration 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 ( 5.3 ) 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.
2.3Treatment 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.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Injection: 3120 mcg/1.56 mL (2000 mcg/mL) of abaloparatide in clear, colorless solution in a single-patient-use prefilled pen. The prefilled pen delivers 30 doses of TYMLOS, each containing 80 mcg of abaloparatide in 40 mcL. Injection: 3120 mcg/1.56 ml (2000 mcg/ml) of abaloparatide in clear, colorless solution in a single-patient-use prefilled pen.
The prefilled pen delivers 30 daily doses of 80 mcg abaloparatide in 40 mcl. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS TYMLOS is contraindicated in patients with a history of severe hypersensitivity to abaloparatide or any of the inactive ingredients of TYMLOS. Reactions have included anaphylaxis, angioedema, dyspnea, and urticaria [see Warnings and Precautions (5.1) , Adverse Reactions ( 6.2 )] . Severe hypersensitivity to abaloparatide or any of the inactive ingredients of TYMLOS. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Hypersensitivity Reactions: Anaphylaxis, angioedema, and urticaria have been reported in patients treated with parathyroid hormone analogs, including TYMLOS. If signs or symptoms of a hypersensitivity reaction occur, discontinue treatment with TYMLOS, initiate supportive care, and monitor until signs or symptoms resolve. Discontinue TYMLOS permanently in patients with a severe hypersensitivity reaction to TYMLOS.
( 5.1 ) 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. ( 5.2 ) Orthostatic Hypotension: Instruct patients to sit or lie down if symptoms develop after dose administration. ( 5.3 ) Hypercalcemia: Avoid use in patients with pre-existing hypercalcemia and those known to have an underlying hypercalcemic disorder, such as primary hyperparathyroidism.
( 5.4 ) Hypercalciuria and Urolithiasis: Monitor urine calcium if pre-existing hypercalciuria or active urolithiasis are suspected. ( 5.5 )
5.1Hypersensitivity Reactions Hypersensitivity reactions, including anaphylaxis, angioedema, and urticaria have been reported in patients treated with parathyroid hormone (PTH) analogs, including TYMLOS [see Adverse Reactions (6.2) ] . If signs or symptoms of a hypersensitivity reaction occur, discontinue treatment with TYMLOS, initiate appropriate supportive care, and monitor until signs and symptoms resolve. Discontinue TYMLOS permanently in patients with a severe hypersensitivity reaction to TYMLOS .
TYMLOS is contraindicated in patients with a history of severe hypersensitivity to abaloparatide or any of the inactive ingredients of TYMLOS [ see Contraindications (4) ].
5.2Risk 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 )] . Avoid TYMLOS use in patients with (these patients are at increased baseline risk of osteosarcoma): Open epiphyses (pediatric and young adult patients) (TYMLOS is not approved in pediatric patients) [see Use in Specific Populations ( 8.4 )] . Metabolic bone diseases other than osteoporosis, including Paget's disease of the bone.
Bone metastases or a history of skeletal malignancies. Prior external beam or implant radiation therapy involving the skeleton. Hereditary disorders predisposing to osteosarcoma.
5.3Orthostatic Hypotension Orthostatic hypotension may occur with TYMLOS, 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, TYMLOS should be administered where the patient can sit or lie down if necessary [see Adverse Reactions ( 6.1 )] .
5.4Hypercalcemia TYMLOS may cause hypercalcemia. TYMLOS 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 [see Adverse Reactions ( 6.1 )] .
5.5Hypercalciuria and Urolithiasis TYMLOS may cause hypercalciuria. It is unknown whether TYMLOS may exacerbate urolithiasis in patients with active…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions are described in greater detail in other sections: Hypersensitivity Reactions [see Warnings and Precautions (5.1) ] Risk of Osteosarcoma [see Warnings and Precautions (5.2) ] Orthostatic Hypotension [see Warnings and Precautions ( 5.3 )] Hypercalcemia [see Warnings and Precautions ( 5.4 )] Hypercalciuria and Urolithiasis [see Warnings and Precautions ( 5.5 )] 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 .
6.1Clinical 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. Adverse Reactions from Clinical Trial in Postmenopausal Women with Osteoporosis The safety of TYMLOS was evaluated in a randomized, multicenter, double-blind, placebo-controlled clinical trial in postmenopausal women with osteoporosis aged 49 to 86 years (mean age 69 years) who were randomized to receive 80 mcg of TYMLOS (N = 824) or placebo (N = 821), given subcutaneously once daily for 18 months [see Clinical Studies ( 14.1 )] .
In this study, the incidence of all-cause mortality was 0.4% in the TYMLOS group and 0.6% in the placebo group. The incidence of serious adverse events was 10% in the TYMLOS group and 11% in the placebo group. The percentage of patients who discontinued study drug due to adverse events was 10% in the TYMLOS group and 6% in the placebo group.
The most common adverse reactions leading to study drug discontinuation in the TYMLOS group were nausea (2%), dizziness (1%), headache (1%), and palpitations (1%). Table 1 shows the most common adverse reactions in the trial. These adverse reactions were generally not present at baseline, occurred more commonly with TYMLOS than with placebo, and occurred in at least 2% of the patients treated with TYMLOS.
Table 1: Common Adverse Reactions Reported in Postmenopausal Women with Osteoporosis * * Adverse reactions reported in ≥2% of TYMLOS-treated patients. Preferred term TYMLOS (N=822) (%) Placebo (N=820) (%) Hypercalciuria 11 9 Dizziness 10 6 Nausea 8 3 Headache 8 6 Palpitations 5
0.4Fatigue 3 2 Abdominal pain upper 3 2 Vertigo 2 2 Orthostatic Hypotension In the clinical trial of women with postmenopausal osteoporosis, the incidence of orthostatic blood pressure decline ≥20 mmHg systolic or ≥10 mmHg diastolic at 1 hour after the first injection was 4% in the TYMLOS group and 3% in the placebo group. At later time points the incidence was generally similar between the treatment groups. Adverse reactions of orthostatic hypotension were reported in 1% of patients receiving TYMLOS and 0.5% of patients receiving placebo.
Dizziness was reported by more TYMLOS-treated patients (10%) compared to placebo (6%) [see Warnings and Precautions ( 5.3 )] . Tachycardia In women with postmenopausal osteoporosis, adverse reactions of tachycardia, including sinus tachycardia, were reported in 2% of patients receiving TYMLOS and 1% of patients in the placebo group. In 5 of the 13 patients receiving TYMLOS who experienced tachycardia, symptoms occurred within 1 hour of administration.
TYMLOS has been associated with a dose-dependent increase in heart rate which developed within 15 minutes after injection and resolved in about 6 hours [see Clinical Pharmacology ( 12.2 )] . Injection Site Reactions Duri…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS No specific drug-drug interaction studies have been performed [see Clinical Pharmacology ( 12.3 )] .
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy 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.
8.2Lactation 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.
8.4Pediatric 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 ( 5.2 )] .
8.5Geriatric 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.
8.6Renal Impairment No dosage adjustment is required for patients with mild, moderate, or severe renal impairment. A study of a single dose of TYMLOS 80 mcg given subcutaneously was conducted in subjects with normal renal function or mild, moderate, or severe renal impairment. The maximal concentration (C max ) 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 [see Clinical Pharmacology ( 12.3 )] .
🤰 Pregnancy ▾
8.1Pregnancy 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.
🧒 Pediatric Use ▾
8.4Pediatric 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 ( 5.2 )] .
🧓 Geriatric Use ▾
8.5Geriatric 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.
🆘 Overdosage ▾
10 OVERDOSAGE 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.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism 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. Once-daily administration of abaloparatide stimulates new bone formation on trabecular and cortical bone surfaces by stimulation of osteoblastic activity.
In rats and monkeys, abaloparatide had an anabolic effect on bone, demonstrated by increases in BMD and bone mineral content (BMC) that correlated with increases in bone strength at vertebral and/or nonvertebral sites [see Nonclinical Toxicology ( 13.2 )] .
12.2Pharmacodynamics Effects on Markers of Bone Turnover A dose-finding study of abaloparatide administered once daily for 24 weeks in postmenopausal women with osteoporosis demonstrated a dose-response relationship for BMD and bone formation markers. Daily administration of TYMLOS to postmenopausal women with osteoporosis for 18 months increased the bone formation marker serum procollagen type I N-propeptide (sPINP) and the bone resorption marker serum collagen type I cross-linked C-telopeptide (sCTX). The increase in geometric mean sPINP levels peaked at Month 1 at 93% above baseline in postmenopausal women then decreased slowly over time to 45% above baseline at Month 18.
The increase in geometric mean sCTX levels in postmenopausal women peaked at Month 3 at 26% above baseline then decreased to baseline levels by Month 18. Daily administration of TYMLOS to men with osteoporosis for 12 months increased the bone formation marker sPINP and the bone resorption marker sCTX. The increase in geometric mean sPINP levels peaked at Month 1 at 133% above baseline in men then decreased slowly over time to 84% above baseline at Month 12.
The increase in geometric mean sCTX levels in men peaked at Month 6 at 46% above baseline and was 35% above baseline by Month 12. Cardiac Electrophysiology A 4-way cross-over thorough QT/QTc study was conducted in 55 healthy subjects who received single doses of placebo, subcutaneous doses of abaloparatide at 80 mcg and 240 mcg (three times the recommended dose), and moxifloxacin 400 mg orally. Abaloparatide increased heart rate, with a mean peak increase of 15 beats per minute (bpm) and 20 bpm at the first time point (15 minutes) after dosing with 80 mcg and 240 mcg, respectively.
There were no clinically meaningful effects of abaloparatide on QTcI (individually corrected QT intervals) or cardiac electrophysiology.
12.3Pharmacokinetics 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. The absolute bioavailability of abaloparatide in healthy women after subcutaneous administration of an 80 mcg dose was 36%.
Distribution The in vitro plasma protein binding of abaloparatide was approximately 70%. The volume of distribution was approximately 50 L. Elimination Excretion The mean (SD) half-life of abaloparatide is approximately 1 h.
The peptide fragments are primarily eliminated through renal excretion. Metabolism No specific metabolism or excretion studies have been performed with TYMLOS. The metabolism of abaloparatide is consistent with non-specific proteolytic degradation into smaller peptide fragments, followed by elimination by renal clearance.
Specific Populations Male and Female Subjects Mean serum abaloparatide concentration-time profiles observed in a study conducted in healthy men with a mean (±SD) age of 53.1 (±6.9) years were comparable to those observed in the healthy women with a mean (±SD) age of 53.7 (±7.1) years using the same dosing regimen. Geriatric Patients No age-related differences in abaloparatide pharmacokinetics were observed in men and postmen…
🧬 Mechanism of Action ▾
12.1Mechanism 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. Once-daily administration of abaloparatide stimulates new bone formation on trabecular and cortical bone surfaces by stimulation of osteoblastic activity.
In rats and monkeys, abaloparatide had an anabolic effect on bone, demonstrated by increases in BMD and bone mineral content (BMC) that correlated with increases in bone strength at vertebral and/or nonvertebral sites [see Nonclinical Toxicology ( 13.2 )] .
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING
16.1How Supplied TYMLOS (abaloparatide) injection is a clear and colorless solution, available as a pre-assembled single-patient-use disposable pen (NDC 70539-001-01) packaged in a cardboard carton (NDC 70539-001-02) with the Instructions for Use and Medication Guide. Each disposable pen embodies a glass cartridge that contains 3120 mcg of abaloparatide in 1.56 mL (2000 mcg/mL). Each pen provides a 30-day supply for once daily injection of 80 mcg abaloparatide in 40 mcL.
Sterile needles are not included.
16.2Storage and Handling Before first use, store TYMLOS under refrigeration between 2°C to 8°C (36°F to 46°F). After first use, store for up to 30 days at 20°C to 25°C (68°F to 77°F). Do not freeze or subject to heat.
📦 Storage and Handling ▾
16.2Storage and Handling Before first use, store TYMLOS under refrigeration between 2°C to 8°C (36°F to 46°F). After first use, store for up to 30 days at 20°C to 25°C (68°F to 77°F). Do not freeze or subject to heat.
📋 Description ▾
11 DESCRIPTION TYMLOS injection for subcutaneous administration contains abaloparatide, a synthetic 34 amino acid peptide. Abaloparatide is an analog of human parathyroid hormone related peptide, PTHrP(1-34). It has 41% homology to hPTH(1-34) (human parathyroid hormone 1-34) and 76% homology to hPTHrP(1-34) (human parathyroid hormone-related peptide 1-34).
Abaloparatide has a molecular formula of C 174 H 300 N 56 O 49 and a molecular weight of 3961 daltons with the amino acid sequence shown below: Ala-Val-Ser-Glu-His-Gln-Leu-Leu-His-Asp-Lys-Gly-Lys-Ser-Ile-Gln-Asp-Leu-Arg-Arg-Arg-Glu-Leu-Leu-Glu-Lys-Leu-Leu-Aib-Lys-Leu-His-Thr-Ala-NH 2 TYMLOS injection is supplied as a sterile, colorless, clear solution in a glass cartridge which is pre-assembled into a disposable single-patient-use pen. The pen is intended to deliver 30 once daily abaloparatide doses of 80 mcg in 40 mcL.
Each cartridge contains 1.56 mL of TYMLOS solution which contains 3.12 mg of abaloparatide, and the following inactive ingredients: 1.2 mg glacial acetic acid, 7.8 mg phenol, 7.92 mg sodium acetate trihydrate, and water for injection to a target pH range of 5.1 to 5.2.
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling ( Medication Guide and Instructions for Use ). Hypersensitivity Reactions Advise patients that serious hypersensitivity reactions, including anaphylaxis, angioedema, and urticaria, can occur with TYMLOS. Advise patients to discontinue TYMLOS and promptly seek immediate medical attention if signs or symptoms of hypersensitivity reactions occur [see Contraindications ( 4 ), Warnings and Precautions ( 5.1 )] .
Risk of Osteosarcoma Advise patients that the active ingredient in TYMLOS, abaloparatide, caused a dose-dependent increase in the incidence of osteosarcoma in male and female rats and that it is unknown whether TYMLOS will cause osteosarcoma in humans [see Warnings and Precautions ( 5.2 )] . 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. Hypercalcemia Advise patients that TYMLOS may cause hypercalcemia and discuss the symptoms of hypercalcemia (e.g., nausea, vomiting, constipation, lethargy, muscle weakness) [see Warnings and Precautions ( 5.4 )] .
Instruct patients to promptly report signs and symptoms of hypercalcemia. Orthostatic Hypotension 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 [see Dosage and Administration ( 2.2 )] .
Use of TYMLOS Pen Instruct patients and caregivers who administer TYMLOS on how to properly use the TYMLOS pen and to follow sharps disposal recommendations [see Dosage and Administration ( 2.2 )] . Advise patients not to share their TYMLOS pen or needles with other patients and not to transfer the contents of the pen to a syringe. Advise patients that each TYMLOS pen can be used for up to 30 days, and after the 30-day use period, to discard the TYMLOS pen, even if it still contains unused solution [see How Supplied/Storage and Handling ( 16.2 )] .
Manufactured for: Radius Health, Inc. 22 Boston Wharf Road, 7th Floor Boston, MA 02210 TYMLOS is a registered trademark of Radius Health, Inc. Copyright © 2017, Radius Health, Inc.
All rights reserved. US-PI-000001-v12.0
💬 Medication Guide ▾
MEDICATION GUIDE TYMLOS ® (tim lows') (abaloparatide) injection, for subcutaneous use What is the most important information I should know about TYMLOS? TYMLOS may cause serious side effects including: Allergic (hypersensitivity) reactions, including anaphylaxis. Stop taking TYMLOS and get medical help right away if you have any of the following symptoms of an allergic reaction: swelling of your face, lips, mouth, or tongue breathing problems fainting, dizziness, feeling lightheaded (low blood pressure) fast heartbeat itching rash hives Possible bone cancer (osteosarcoma).
During animal drug testing, the medicine in TYMLOS caused some rats to develop a bone cancer called osteosarcoma. It is not known if people who take TYMLOS will have a higher chance of getting osteosarcoma. Tell your healthcare provider right away if you have pain in your bones, pain in any areas of your body that does not go away, or any new or unusual lumps or swelling under your skin that is tender to touch.
What is TYMLOS? TYMLOS is a prescription medicine used to: treat osteoporosis in postmenopausal women who are at high risk for bone fracture, or who cannot use another osteoporosis treatment or other osteoporosis treatments did not work well. TYMLOS can decrease the chance of having a fracture of the spine and other bones in postmenopausal women with thinning and weakening bones (osteoporosis) increase bone density in men with osteoporosis who are at high risk for bone fracture, or who cannot use another osteoporosis treatment or other osteoporosis treatments did not work well It is not known if TYMLOS is safe and effective for children 18 years and younger.
TYMLOS should not be used in children and young adults whose bones are still growing. It is not recommended that people use TYMLOS for more than 2 years during their lifetime. Do not take TYMLOS: if you have had a severe allergic reaction to abaloparatide, or any of the other ingredients in TYMLOS.
Ask your healthcare provider if you are not sure. See the end of this Medication Guide for a complete list of ingredients in TYMLOS. Before you take TYMLOS, tell your healthcare provider about all of your medical conditions, including if you: have Paget's disease of the bone or other bone disease. have or have had cancer in your bones. have or have had radiation therapy involving your bones. have or have had too much calcium in your blood. have or have had an increase in your parathyroid hormone (hyperparathyroidism). will have trouble injecting yourself with the TYMLOS pen and do not have someone who can help you. are pregnant or plan to become pregnant.
TYMLOS is not for pregnant women. are breastfeeding or plan to breastfeed. It is not known if TYMLOS passes into your breast milk. You and your healthcare provider should decide if you will take TYMLOS or breastfeed.
You should not do both. Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Know the medicines you take.
Keep a list of them to show your healthcare provider or pharmacist each time you get a new medicine. How should I use TYMLOS? Read the detailed Instructions for Use provided with your medicine.
Use TYMLOS exactly as your healthcare provider tells you to use it. Do not try to inject TYMLOS yourself until you or your caregiver receive training from a healthcare provider on the right way to use the TYMLOS pen. You should receive your first several injections of TYMLOS where you can sit or lie down, if necessary, until you know how it affects you.
Inject TYMLOS 1 time each day into your lower stomach area (abdomen) just under your skin (subcutaneous). Avoid giving your injection within the 2-inch area around your belly button (navel). Talk to your healthcare provider about how to change (rotate) your injection site for each injection.
Do not give TYMLOS in your veins (intravenously) or deep into your muscles (intramuscularly). You can take T…