Abaloparatide
Abaloparatide (Tymlos) is a 34-aa PTHrP analogue with greater RG conformation selectivity than teriparatide. FDA-approved for osteoporosis. Phase III ACTIVE trial showed superior vertebral fracture reduction with lower hypercalcemia risk.
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Compound Profile
Abaloparatide
Key Data
Research reference only
Research Focus
Preclinical data
⚠ Research & Educational Use Only. Abaloparatide is a research chemical documented here for scientific education. All information references peer-reviewed literature and preclinical/clinical study data. Not for human consumption. Not medical advice. Consult a licensed researcher or healthcare professional before any laboratory use.
- Reduces vertebral fracture risk by 86% vs placebo (ACTIVE trial, 18 months) — superior to teriparatide in this trial (78% reduction)
- Lower incidence of hypercalcemia vs teriparatide — important for patient tolerability and monitoring burden reduction
- Increases lumbar spine BMD by 11% and total hip BMD by 4.1% over 18 months
- Abaloparatide is not FDA-approved for human use. FDA-approved prescription drug (Tymlos, Radius Health/Menarini). Indicated for postmenopausal women with osteoporosis at high fracture risk.
Research At a Glance
- Reduces vertebral fracture risk by 86% vs placebo (ACTIVE trial, 18 months) — superior to teriparatide in this trial (78% reduction)
- Lower incidence of hypercalcemia vs teriparatide — important for patient tolerability and monitoring burden reduction
- Increases lumbar spine BMD by 11% and total hip BMD by 4.1% over 18 months
- RG conformation selectivity (cAMP-biased PTH1R signaling) → reduced bone resorption co-stimulation vs RG+R0 activation
In Plain English
Simple summaryAbaloparatide (Tymlos) is a synthetic 34-amino acid analogue of PTHrP (parathyroid hormone-related protein) -- not PTH itself, but a related protein that acts on the same receptor. The difference in binding profile matters: while teriparatide (PTH 1-34) fully activates the PTH1 receptor, abaloparatide preferentially engages the receptor in a conformation that produces stronger anabolic signaling and less resorptive activation. In practice, the clinical results are similar to teriparatide but with one advantage: the ACTIVE trial showed abaloparatide produced a greater reduction in non-vertebral fractures (43% vs 19% for teriparatide in a head-to-head analysis) with a lower rate of hypercalcemia. FDA-approved in 2017 for postmenopausal women with osteoporosis at high fracture risk.
- Reduces vertebral fracture risk by 86% vs placebo — superior to teriparatide in this trial (78% reduction)
- Lower incidence of hypercalcemia vs teriparatide — important for patient tolerability and monitoring burden reduction
- Increases lumbar spine BMD by 11% and total hip BMD by 4.1% over 18 months
The full scientific detail, mechanisms, citations, and dosing data, follows below.
What is Abaloparatide?
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Abaloparatide (brand name: Tymlos) is a synthetic 34-amino acid peptide analogue of parathyroid hormone-related protein (PTHrP), developed by Radius Health. It received FDA approval in 2017 for the treatment of postmenopausal women with osteoporosis at high fracture risk.
Unlike teriparatide, which is a fragment of PTH, abaloparatide is derived from PTHrP — a structurally related protein that also activates the PTH1R but with different receptor conformation preferences. This difference in conformation selectivity is the mechanistic basis for abaloparatide's claimed advantages.
**PTH1R conformation selectivity:** The PTH1R exists in two conformational states: - **R0 state**: High-affinity conformation that activates both Gs (cAMP) and Gq pathways; binding is prolonged - **RG state**: G-protein-coupled state with faster dissociation kinetics
PTH preferentially binds both R0 and RG states (sustained cAMP production), while PTHrP and abaloparatide show preferential RG-state binding (shorter, more transient cAMP signaling). It is hypothesized that this RG-bias produces a more anabolic and less bone-resorptive PTH1R activation profile — potentially explaining abaloparatide's lower hypercalcemia incidence.
**ACTIVE trial results (Miller et al., JAMA 2016):** In 2,463 postmenopausal women randomized to abaloparatide 80 mcg SC, teriparatide 20 mcg SC, or placebo over 18 months: - Vertebral fracture reduction vs placebo: abaloparatide 86%, teriparatide 78% - Non-vertebral fracture reduction vs placebo: abaloparatide 43% (significant), teriparatide 28% (non-significant) - Hypercalcemia incidence: abaloparatide 3.4%, teriparatide 6.4% - Time to non-vertebral fracture reduction was faster with abaloparatide
An innovative transdermal patch formulation (ATOM trial) delivering abaloparatide through a 5-minute skin contact patch achieved similar pharmacokinetic profiles to the SC injection and is under development as a needle-free alternative.
By the Numbers
Key Research Benefits
Documented effects observed in preclinical and clinical studies on Abaloparatide. See all Muscle & Performance peptides for comparison.
Side Effects & Risks
Adverse effects reported in the research literature. All data sourced from preclinical and clinical study reports. View all peptides' side effects →
Dosing Data from the Literature
Doses referenced below are sourced from published preclinical and clinical studies. Use the peptide dose calculator to convert these values to injection volume.
Abaloparatide (Tymlos) dosing:
Approved dose: 80 mcg SC once daily Injection site: Periumbilical region of the abdomen (avoid 2-inch radius around navel) Duration: 24 months lifetime limit (same class risk as teriparatide) Post-treatment: Continue with antiresorptive therapy (bisphosphonate preferred) to maintain BMD gains
Transdermal patch (investigational): 300 mcg patch × 5 minutes daily contact — delivers ~17 mcg systemically (ATOM trial data)
Administration in Research Settings
Standard reconstitution and administration methodology for laboratory research use.
Inject subcutaneously in the periumbilical abdomen using the prefilled autoinjector pen. Inject immediately after removing from refrigerator. Rotate sites within the recommended area.
What the research doesn't show
Like teriparatide, abaloparatide has the same animal osteosarcoma concern from high-dose rodent studies and carries the same black box warning. Treatment is limited to 2 years. The head-to-head superiority on non-vertebral fractures comes from a network meta-analysis comparison, not a direct randomized head-to-head trial, so the comparison should be interpreted with appropriate caution.
Medical Expert Videos
Physicians, researchers, and pharmacologists explain Abaloparatide, covering mechanisms of action, clinical context, and study findings.
Videos sourced from YouTube search. KnowYourPeptide does not endorse any individual creator. For research education only.
The Bottom Line
Abaloparatide has a growing body of preclinical evidence and a well-characterised safety profile in research settings. The most-studied application is: reduces vertebral fracture risk by 86% vs placebo — superior to teriparatide in this trial (78% reduction).
The most commonly reported side effect in research subjects is hypercalcemia: ~3% vs ~6% with teriparatide. It is a research chemical, not approved for human use.
Frequently Asked Questions
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Quick Reference
How It Compares
Teriparatide is the older PTH 1-34 analogue with the longest post-marketing record. Abaloparatide's biased receptor agonism theoretically produces a better anabolic-to-catabolic ratio. Romosozumab (Evenity) is the most potent bone anabolic available but has a cardiovascular safety concern that limits use. When the choice is between abaloparatide and teriparatide, the data slightly favors abaloparatide on non-vertebral fractures but both are acceptable first-line anabolics.
Compare Abaloparatide side-by-sideResearch Use Only
This information is for educational research purposes only. This is not medical advice. Consult a qualified healthcare professional.