ABALOPARATIDE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208743lbl.pdf | https://www.centerwatch.com/drug-information/fda-approved-drugs/drug/100201/tymlos-abaloparatide- | https://www.ncbi.nlm.nih.gov/pubmed/29241341

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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Parathyroid hormone receptor 1 Target ID: CHEMBL1793 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24078470	Agonist 2470		0.087 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Osteoporosis 96 Sources: https://www.centerwatch.com/drug-information/fda-approved-drugs/drug/100201/tymlos-abaloparatide-	Primary		Approved 8043	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

Title	Date	PubMed
Effect of a sequential treatment combining abaloparatide and alendronate for the management of postmenopausal osteoporosis.	2018 Feb	29251010
Correction to: Geography of Fracture Incidence in Postmenopausal Women with Osteoporosis Treated with Abaloparatide.	2018 Jun	29383409
Geography of Fracture Incidence in Postmenopausal Women with Osteoporosis Treated with Abaloparatide.	2018 Jun	29285549
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	29260289
Abaloparatide: Review of a Next-Generation Parathyroid Hormone Agonist.	2018 May	29241341

Patents

Sample Use Guides

In Vivo Use Guide

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

In Vitro Use Guide

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

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