abaloparatide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
peptides and glycopeptides 5232 247062-33-5

Description:

MoleculeDescription

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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

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

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Palpitations 704.85 31.92 358 12679 136370 90479040
Headache 637.47 31.92 694 12343 862052 89753358
Heart rate increased 611.92 31.92 306 12731 112596 90502814
Product dose omission issue 483.75 31.92 371 12666 291316 90324094
Dizziness 451.96 31.92 485 12552 588799 90026611
Bone pain 404.49 31.92 191 12846 61792 90553618
Nausea 338.60 31.92 583 12454 1109733 89505677
Product quality issue 312.49 31.92 174 12863 79151 90536259
Injection site bruising 254.25 31.92 132 12905 52175 90563235
Back pain 222.49 31.92 250 12787 316925 90298485
Wrong technique in product usage process 210.50 31.92 130 12907 71441 90543969
Fatigue 179.26 31.92 461 12576 1153562 89461848
Intentional dose omission 138.34 31.92 62 12975 17721 90597689
Blood calcium increased 123.26 31.92 51 12986 12007 90603403
Myalgia 117.29 31.92 135 12902 174990 90440420
Product storage error 115.56 31.92 57 12980 20184 90595226
Drug ineffective 97.54 31.92 39 12998 1384259 89231151
Therapy interrupted 94.22 31.92 69 12968 50039 90565371
Illness 89.01 31.92 82 12955 81887 90533523
Product administered at inappropriate site 80.37 31.92 28 13009 4123 90611287
Feeling abnormal 80.03 31.92 109 12928 167126 90448284
Muscle spasms 76.54 31.92 133 12904 251750 90363660
Vertigo 76.10 31.92 70 12967 69741 90545669
Arthralgia 74.41 31.92 263 12774 778259 89837151
Sensory disturbance 72.24 31.92 38 12999 15375 90600035
Injection site pain 69.54 31.92 104 12933 173595 90441815
Injection site haemorrhage 67.23 31.92 45 12992 28273 90587137
Pain in extremity 67.14 31.92 178 12859 450351 90165059
Product dose omission in error 62.12 31.92 38 12999 20465 90594945
Needle issue 61.48 31.92 33 13004 13901 90601509
Growing pains 50.75 31.92 8 13029 28 90615382
Pollakiuria 47.92 31.92 39 12998 32966 90582444
Injection site erythema 46.76 31.92 64 12973 98438 90516972
Blood alkaline phosphatase increased 44.38 31.92 44 12993 48035 90567375
Flushing 42.77 31.92 58 12979 88433 90526977
Hypercalcaemia 42.58 31.92 37 13000 34203 90581207
Blood pressure decreased 39.13 31.92 51 12986 74844 90540566
Tachycardia 38.69 31.92 76 12961 157597 90457813
Product use complaint 36.29 31.92 15 13022 3518 90611892
Acute kidney injury 34.96 31.92 3 13034 320384 90295026
Head discomfort 34.14 31.92 24 13013 16309 90599101
Blood parathyroid hormone increased 33.31 31.92 14 13023 3423 90611987
General physical health deterioration 32.31 31.92 6 13031 355109 90260301

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Off label use 67.92 43.63 47 274 638288 41982726

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Palpitations 530.45 35.81 258 8729 158954 110421358
Headache 521.59 35.81 484 8503 881893 109698419
Heart rate increased 422.16 35.81 214 8773 143620 110436692
Product dose omission issue 387.48 35.81 269 8718 321513 110258799
Dizziness 335.53 35.81 343 8644 697850 109882462
Product quality issue 311.23 35.81 143 8844 77156 110503156
Bone pain 292.31 35.81 130 8857 65003 110515309
Nausea 290.16 35.81 422 8565 1235268 109345044
Injection site bruising 181.94 35.81 87 8900 51176 110529136
Back pain 178.47 35.81 183 8804 370813 110209499
Wrong technique in product usage process 161.57 35.81 96 8891 87252 110493060
Fatigue 128.65 35.81 295 8692 1215663 109364649
Intentional dose omission 122.88 35.81 50 8937 20030 110560282
Therapy interrupted 97.95 35.81 57 8930 49765 110530547
Product storage error 96.14 35.81 43 8944 21685 110558627
Myalgia 74.47 35.81 91 8896 222290 110358022
Product administered at inappropriate site 72.54 35.81 24 8963 5369 110574943
Feeling abnormal 68.84 35.81 79 8908 180632 110399680
Blood calcium increased 68.18 35.81 32 8955 18008 110562304
Pain in extremity 67.04 35.81 132 8855 486986 110093326
Drug ineffective 65.94 35.81 21 8966 1520519 109059793
Injection site pain 63.13 35.81 75 8912 177847 110402465
Illness 61.52 35.81 52 8935 82119 110498193
Arthralgia 57.84 35.81 166 8821 779466 109800846
Muscle spasms 57.21 35.81 90 8897 278067 110302245
Vertigo 55.05 35.81 50 8937 86820 110493492
Needle issue 47.67 35.81 25 8962 17815 110562497
Sensory disturbance 45.36 35.81 24 8963 17405 110562907
Injection site haemorrhage 45.14 35.81 30 8957 32998 110547314
Flushing 41.91 35.81 47 8940 104689 110475623
Product dose omission in error 38.67 35.81 24 8963 23488 110556824

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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
CHEBI has role CHEBI:50646 bone density conservation agent

Related Drugs by ATC class:

H05AA Parathyroid hormones and analogues 3 drugs
palopegteriparatideparathyroid hormoneteriparatide

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

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
3.12MG/1.56ML (2MG/ML) TYMLOS RADIUS 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 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 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 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 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 N208743 April 28, 2017 RX SOLUTION SUBCUTANEOUS 11782041 April 30, 2038 METHOD OF TREATING POSTMENOPAUSAL WOMEN WITH OSTEOPOROSIS AT HIGH RISK FOR FRACTURE.
3.12MG/1.56ML (2MG/ML) TYMLOS RADIUS N208743 April 28, 2017 RX SOLUTION SUBCUTANEOUS 11782041 April 30, 2038 TREATMENT TO INCREASE BONE DENSITY IN MEN WITH OSTEOPOROSIS AT HIGH RISK FOR FRACTURE
3.12MG/1.56ML (2MG/ML) TYMLOS RADIUS N208743 April 28, 2017 RX SOLUTION SUBCUTANEOUS 11255842 Jan. 10, 2040 USE FOR DETECTING NEUTRALIZING ANTIBODIES
3.12MG/1.56ML (2MG/ML) TYMLOS RADIUS N208743 April 28, 2017 RX SOLUTION SUBCUTANEOUS 11680942 Jan. 10, 2040 USE FOR DETECTING NEUTRALIZING ANTIBODIES

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Parathyroid hormone/parathyroid hormone-related peptide receptor GPCR AGONIST IC50 9.70 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
AVK0I6HY2U UNII
4036650 VANDF
C4042342 UMLSCUI
CHEBI:755265 CHEBI
CHEMBL3301581 ChEMBL_ID
76943386 PUBCHEM_CID
DB05084 DRUGBANK_ID
D10885 KEGG_DRUG
9794 INN_ID
C000596789 MESH_SUPPLEMENTAL_RECORD_UI
8299 IUPHAR_LIGAND_ID
735229000 SNOMEDCT_US
763500008 SNOMEDCT_US
256732 MMSL
32684 MMSL
d08578 MMSL
017204 NDDF
1921069 RXNORM
AVK0I6HY2U INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tymlos HUMAN PRESCRIPTION DRUG LABEL 1 70539-001 INJECTION, SOLUTION 3.12 mg SUBCUTANEOUS NDA 30 sections