U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
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

Targets

Primary TargetPharmacologyConditionPotency
0.087 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TYMLOS

Approved Use

TYMLOS 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 Date

1.49325126E12
PubMed

PubMed

TitleDatePubMed
Effect of a sequential treatment combining abaloparatide and alendronate for the management of postmenopausal osteoporosis.
2018 Feb
Correction to: Geography of Fracture Incidence in Postmenopausal Women with Osteoporosis Treated with Abaloparatide.
2018 Jun
Geography of Fracture Incidence in Postmenopausal Women with Osteoporosis Treated with Abaloparatide.
2018 Jun
Abaloparatide, a novel PTH receptor agonist, increased bone mass and strength in ovariectomized cynomolgus monkeys by increasing bone formation without increasing bone resorption.
2018 Mar
Abaloparatide: Review of a Next-Generation Parathyroid Hormone Agonist.
2018 May
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
cAMP signaling potency of Abaloparatide in PTHR1-expressing cells was found to be approximately 5-fold greater than that of PTH (1–34) (EC50 = ∼0.087 vs ∼0.44nM; P = .0009).
Name Type Language
ABALOPARATIDE
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
ABALOPARATIDE [INN]
Common Name English
BA-058
Code English
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-2-MEALA-LYS-LEU-HIS-THR-ALA-NH2
Common Name English
ABALOPARATIDE [USAN]
Common Name English
TYMLOS
Brand Name English
ABALOPARATIDE [WHO-DD]
Common Name English
BIM-44058
Code English
C2.29-METHYL(22-L-GLUTAMIC ACID(F>E),23-L-LEUCINE(F>L),25-L-GLUTAMIC ACID(H>E),26-L-LYSINE(H>K),28-L-LEUCINE(I>L),30-L-LYSINE(E>K), 31-L-LEUCINE(I>L))HUMAN PARATHYROID HORMONE-RELATED PROTEIN-(1-34)-PROTEINAMIDE
Common Name English
BA058
Code English
ABALOPARATIDE [ORANGE BOOK]
Common Name English
ABALOPARATIDE [MI]
Common Name English
Classification Tree Code System Code
NDF-RT N0000193453
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
Code System Code Type Description
EVMPD
SUB180168
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY
CAS
247062-33-5
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY
INN
9794
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY
ChEMBL
CHEMBL3301581
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY
DRUG CENTRAL
5232
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY
CAS
506422-98-6
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
ALTERNATIVE
FDA UNII
AVK0I6HY2U
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY
PUBCHEM
76943386
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY
RXCUI
1921069
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY
MERCK INDEX
M12003
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY
DRUG BANK
DB05084
Created by admin on Mon Jun 28 00:59:13 UTC 2021 , Edited by admin on Mon Jun 28 00:59:13 UTC 2021
PRIMARY