abaloparatide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
peptides and glycopeptides	5232	247062-33-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: abaloparatide tymlos BA058 BIM-44058 abaloparatide acetate	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. Molecular weight: 3960.66 Formula: C174H300N56O49 CLOGP: LIPINSKI: None HAC: 105 HDO: 61 TPSA: 1738.60 ALOGS: ROTB: 142

Molecule

Description

Molfile Inchi Smiles

Synonyms:

abaloparatide
tymlos
BA058
BIM-44058
abaloparatide acetate

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.

Molecular weight: 3960.66
Formula: C174H300N56O49
CLOGP:
LIPINSKI: None
HAC: 105
HDO: 61
TPSA: 1738.60
ALOGS:
ROTB: 142

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company
Dec. 12, 2022	EMA	Radius Health Ireland Ltd
April 28, 2017	FDA	RADIUS HEALTH INC
March 23, 2021	PMDA	Teijin Pharma Limited

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product quality issue	1140.54	37.91	382	12610	35483	63440547
Product dose omission issue	1080.16	37.91	640	12352	233673	63242357
Headache	672.24	37.91	728	12264	632513	62843517
Palpitations	648.21	37.91	357	12635	112413	63363617
Wrong technique in product usage process	594.16	37.91	278	12714	62062	63413968
Heart rate increased	565.14	37.91	307	12685	93931	63382099
Dizziness	482.99	37.91	511	12481	429414	63046616
Bone pain	340.85	37.91	183	12809	54458	63421572
Injection site bruising	326.49	37.91	163	12829	41747	63434283
Nausea	316.72	37.91	596	12396	853875	62622155
Product storage error	298.32	37.91	113	12879	14843	63461187
Needle issue	198.24	37.91	76	12916	10300	63465730
Back pain	168.66	37.91	237	12755	263908	63212122
Fatigue	146.33	37.91	454	12538	887574	62588456
Injection site pain	131.64	37.91	147	12845	129653	63346377
Drug ineffective	126.20	37.91	30	12962	1044735	62431295
Product administered at inappropriate site	125.84	37.91	40	12952	3109	63472921
Injection site haemorrhage	104.59	37.91	64	12928	24250	63451780
Feeling abnormal	103.26	37.91	139	12853	148253	63327777
Muscle spasms	97.75	37.91	139	12853	156011	63320019
Blood calcium increased	95.94	37.91	44	12948	9306	63466724
Intentional dose omission	92.38	37.91	41	12951	8034	63467996
Vertigo	80.65	37.91	79	12913	59808	63416222
Sensory disturbance	74.63	37.91	42	12950	13630	63462400
Product use complaint	73.02	37.91	25	12967	2449	63473581
Pain in extremity	46.33	37.91	161	12831	331325	63144705
Flushing	42.77	37.91	64	12928	75023	63401007
Myalgia	41.27	37.91	92	12900	146437	63329593
Adverse event	40.52	37.91	59	12933	67500	63408530
Product dose omission in error	40.50	37.91	23	12969	7589	63468441
Anaemia	40.34	37.91	6	12986	293424	63182606

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Off label use	186.85	74.73	64	77	419460	34537330

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product quality issue	875.34	48.98	260	7723	33680	79702725
Product dose omission issue	826.58	48.98	428	7555	247109	79489296
Headache	506.44	48.98	457	7526	653315	79083090
Palpitations	426.16	48.98	221	7762	126389	79610016
Wrong technique in product usage process	378.33	48.98	172	7811	73703	79662702
Heart rate increased	372.76	48.98	199	7784	120525	79615880
Dizziness	321.82	48.98	324	7659	526117	79210288
Nausea	240.29	48.98	377	7606	956819	78779586
Bone pain	206.41	48.98	104	7879	55638	79680767
Product storage error	195.36	48.98	70	7913	16156	79720249
Injection site bruising	186.29	48.98	88	7895	40914	79695491
Back pain	133.62	48.98	158	7825	304022	79432383
Fatigue	104.06	48.98	262	7721	929465	78806940
Needle issue	101.65	48.98	41	7942	13027	79723378
Injection site pain	91.74	48.98	87	7896	129751	79606654
Product administered at inappropriate site	91.62	48.98	28	7955	3937	79732468
Feeling abnormal	89.14	48.98	94	7889	159105	79577300
Muscle spasms	75.25	48.98	90	7893	174640	79561765
Drug ineffective	64.12	48.98	15	7968	1080898	78655507
Injection site haemorrhage	64.11	48.98	38	7945	27832	79708573
Intentional dose omission	62.88	48.98	26	7957	8791	79727614
Blood calcium increased	55.54	48.98	25	7958	10375	79726030
Product use complaint	50.90	48.98	16	7967	2467	79733938

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	H05AA04	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS CALCIUM HOMEOSTASIS PARATHYROID HORMONES AND ANALOGUES Parathyroid hormones and analogues
MeSH PA	D050071	Bone Density Conservation Agents
FDA CS	M0150746	Parathyroid Hormone-Related Protein
FDA EPC	N0000193453	Parathyroid Hormone-Related Peptide Analog

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Osteoporosis	indication	64859006	DOID:11476
At risk of osteoporotic fracture	indication	391040000
Hypercalcemia	contraindication	66931009	DOID:12678
Bone metastases	contraindication	94222008
Renal impairment	contraindication	236423003
Pregnancy, function	contraindication	289908002
Breastfeeding (mother)	contraindication	413712001
Skeletal malignancies	contraindication	443679004
Risk for osteosarcoma	contraindication
Unexplained elevations of serum alkaline phosphatase	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.19	acidic
pKa2	3.57	acidic
pKa3	3.97	acidic
pKa4	4.19	acidic
pKa5	4.57	acidic
pKa6	12.15	acidic
pKa7	12.45	acidic
pKa8	12.49	acidic
pKa9	12.69	acidic
pKa10	12.78	acidic
pKa11	13.03	acidic
pKa12	13.05	acidic
pKa13	13.1	acidic
pKa14	13.33	acidic
pKa15	13.34	acidic
pKa16	13.45	acidic
pKa17	13.56	acidic
pKa18	13.6	acidic
pKa19	13.66	acidic
pKa20	13.74	acidic
pKa21	13.86	acidic
pKa22	13.89	acidic
pKa23	13.94	acidic
pKa24	11.5	Basic
pKa25	11.26	Basic
pKa26	11.01	Basic
pKa27	10.81	Basic
pKa28	10.55	Basic
pKa29	10.3	Basic
pKa30	9.94	Basic
pKa31	8.42	Basic
pKa32	7.16	Basic
pKa33	6.69	Basic
pKa34	6.21	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
3.12MG/1.56ML (2MG/ML)	TYMLOS	RADIUS HEALTH INC	N208743	April 28, 2017	RX	SOLUTION	SUBCUTANEOUS	8748382	Oct. 3, 2027	METHOD OF TREATING POSTMENOPAUSAL WOMEN WITH OSTEOPOROSIS AT HIGH RISK FOR FRACTURE.
3.12MG/1.56ML (2MG/ML)	TYMLOS	RADIUS HEALTH INC	N208743	April 28, 2017	RX	SOLUTION	SUBCUTANEOUS	8748382	Oct. 3, 2027	TREATMENT TO INCREASE BONE DENSITY IN MEN WITH OSTEOPOROSIS AT HIGH RISK FOR FRACTURE
3.12MG/1.56ML (2MG/ML)	TYMLOS	RADIUS HEALTH INC	N208743	April 28, 2017	RX	SOLUTION	SUBCUTANEOUS	7803770	April 28, 2031	METHOD OF TREATING POSTMENOPAUSAL WOMEN WITH OSTEOPOROSIS AT HIGH RISK FOR FRACTURE.
3.12MG/1.56ML (2MG/ML)	TYMLOS	RADIUS HEALTH INC	N208743	April 28, 2017	RX	SOLUTION	SUBCUTANEOUS	RE49444	April 28, 2031	METHOD OF TREATING POSTMENOPAUSAL WOMEN WITH OSTEOPOROSIS AT HIGH RISK FOR FRACTURE.
3.12MG/1.56ML (2MG/ML)	TYMLOS	RADIUS HEALTH INC	N208743	April 28, 2017	RX	SOLUTION	SUBCUTANEOUS	RE49444	April 28, 2031	TREATMENT TO INCREASE BONE DENSITY IN MEN WITH OSTEOPOROSIS AT HIGH RISK FOR FRACTURE
3.12MG/1.56ML (2MG/ML)	TYMLOS	RADIUS HEALTH INC	N208743	April 28, 2017	RX	SOLUTION	SUBCUTANEOUS	11255842	Jan. 10, 2040	USE FOR DETECTING NEUTRALIZING ANTIBODIES
3.12MG/1.56ML (2MG/ML)	TYMLOS	RADIUS HEALTH INC	N208743	April 28, 2017	RX	SOLUTION	SUBCUTANEOUS	11680942	Jan. 10, 2040	USE FOR DETECTING NEUTRALIZING ANTIBODIES

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
3.12MG/1.56ML (2MG/ML)	TYMLOS	RADIUS HEALTH INC	N208743	April 28, 2017	RX	SOLUTION	SUBCUTANEOUS	Sept. 20, 2024	INFORMATION ADDED TO CLINICAL PHARMACOLOGY SECTION
3.12MG/1.56ML (2MG/ML)	TYMLOS	RADIUS HEALTH INC	N208743	April 28, 2017	RX	SOLUTION	SUBCUTANEOUS	Dec. 19, 2025	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

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Parathyroid hormone/parathyroid hormone-related peptide receptor	GPCR	Q03431	PTH1R_HUMAN	AGONIST	IC50	9.70		SCIENTIFIC LITERATURE	DRUG LABEL

External reference:

ID	Source
AVK0I6HY2U	UNII
4036650	VANDF
C4042342	UMLSCUI
CHEMBL3301581	ChEMBL_ID
76943386	PUBCHEM_CID
DB05084	DRUGBANK_ID
D10885	KEGG_DRUG
9794	INN_ID
8299	IUPHAR_LIGAND_ID
256732	MMSL
32684	MMSL
d08578	MMSL
017204	NDDF
735229000	SNOMEDCT_US
763500008	SNOMEDCT_US
1921069	RXNORM
C000596789	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Tymlos	HUMAN PRESCRIPTION DRUG LABEL	1	70539-001	INJECTION, SOLUTION	2000 ug	SUBCUTANEOUS	NDA	31 sections
Tymlos	HUMAN PRESCRIPTION DRUG LABEL	1	70539-001	INJECTION, SOLUTION	2000 ug	SUBCUTANEOUS	NDA	31 sections
Tymlos	HUMAN PRESCRIPTION DRUG LABEL	1	70539-001	INJECTION, SOLUTION	2000 ug	SUBCUTANEOUS	NDA	31 sections