Abaloparatide (brand name 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. 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. 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. Abaloparatide was approved in April 28, 2017 by the FDA (as Tymlos) for the treatment of postmenopausal women with osteoporosis at high risk for fracture.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1793 |
0.087 nM [EC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | TYMLOS Approved UseTYMLOS is indicated for the treatment of postmenopausal women with osteoporosis at high risk
for fracture defined as a history of osteoporotic fracture, 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. Launch Date2017 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Correction to: Geography of Fracture Incidence in Postmenopausal Women with Osteoporosis Treated with Abaloparatide. | 2018-06 |
|
| Geography of Fracture Incidence in Postmenopausal Women with Osteoporosis Treated with Abaloparatide. | 2018-06 |
|
| Abaloparatide: Review of a Next-Generation Parathyroid Hormone Agonist. | 2018-05 |
|
| Abaloparatide, a novel PTH receptor agonist, increased bone mass and strength in ovariectomized cynomolgus monkeys by increasing bone formation without increasing bone resorption. | 2018-03 |
|
| Effect of a sequential treatment combining abaloparatide and alendronate for the management of postmenopausal osteoporosis. | 2018-02 |
Patents
Sample Use Guides
Recommended dose is 80 ug subcutaneously once daily; patients should receive supplemental calcium and vitamin D if dietary intake is inadequate.
Administer as a subcutaneous injection into periumbilical region of abdomen. Administer initially where the patient can sit or lie down in case symptoms of orthostatic hypotension occur.
Route of Administration:
Other
| Substance Class |
Protein
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| Protein Type | HORMONE |
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| Sequence Type | COMPLETE |
| Record UNII |
C4LQA2B9H4
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| Record Status |
Validated (UNII)
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| Record Version |
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C4LQA2B9H4
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D11563
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ACTIVE MOIETY |
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Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO ACID SUBSTITUTION | [1_29] | SITE_SPECIFIC | ALANINE | .ALPHA.-AMINOISOBUTYRIC ACID | 1E7ZW41IQU | |
| MOIETY | ACETATE ION | 569DQM74SC | ||||
| AMINO ACID SUBSTITUTION | [1_34] | SITE_SPECIFIC | ALANINE | ALANINAMIDE, L- | GOD06L4T27 |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT:SEQUENCE(CALCULATED) | CHEMICAL |
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| Volume of Distribution | PHARMACOKINETIC |
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| Biological Half-life | PHARMACOKINETIC |
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