Teriparatide

Identification

Summary

Teriparatide is a recombinant parathyroid hormone used for the treatment of osteoporosis.

Brand Names
Forsteo, Forteo
Generic Name
Teriparatide
DrugBank Accession Number
DB06285
Background

Teriparatide (recombinant human parathyroid hormone) is a potent anabolic agent used in the treatment of osteoporosis. It is manufactured and marketed by Eli Lilly and Company.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Hormones
Protein Chemical Formula
C181H291N55O51S2
Protein Average Weight
4117.715 Da
Sequences
>Parathyroid hormone precursor - Homo sapiens (1-34)
SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF
Download FASTA Format
Synonyms
  • PTH (1-34)
  • PTH 1-34
  • Teriparatida
  • Teriparatide
  • Teriparatide recombinant human
External IDs
  • LY 333334
  • LY-333334
  • LY333334
  • ZT-034

Pharmacology

Indication

For the treatment of osteoporosis in men and postmenopausal women who are at high risk for having a fracture. Also used to increase bone mass in men with primary or hypogonadal osteoporosis who are at high risk for fracture.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Clinical trials indicate that teriparatide increases predominantly trabecular bone in the lumbar spine and femoral neck; it has less significant effects at cortical sites. The combination of teriparatide with antiresorptive agents is not more effective than teriparatide monotherapy. The most common adverse effects associated with teriparatide include injection-site pain, nausea, headaches, leg cramps, and dizziness. After a maximum of two years of teriparatide therapy, the drug should be discontinued and antiresorptive therapy begun to maintain bone mineral density.

Mechanism of action

Teriparatide is the portion of human parathyroid hormone (PTH), amino acid sequence 1 through 34 of the complete molecule which contains amino acid sequence 1 to 84. Endogenous PTH is the primary regulator of calcium and phosphate metabolism in bone and kidney. Daily injections of teriparatide stimulates new bone formation leading to increased bone mineral density.

TargetActionsOrganism
UParathyroid hormone/parathyroid hormone-related peptide receptor
binder
Humans
Absorption

Bioavailability is 95% following subcutaneous injection.

Volume of distribution
  • 0.12 L/kg
Protein binding

Not Available

Metabolism

Hepatic

Route of elimination

Peripheral metabolism of PTH is believed to occur by non-specific enzymatic mechanisms in the liver followed by excretion via the kidneys. The 24-hour urine excretion of calcium was reduced by a clinically unimportant amount (15%).

Half-life

Not Available

Clearance
  • 62 L/hr [Women]
  • 94 L/hr [Men]
Adverse Effects
Adverseeffects
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Toxicity

Effects of overexposure may include headaches, dizziness, dizziness, decreased blood pressured, decreased fetal survival, leg cramps, changes in clinical chemistry including increased in blood levels of calcium, decreased serum phosphorous, and increased urinary calcium and phosphorus.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcalabrutinibThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Acalabrutinib.
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Teriparatide.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Teriparatide.
AfatinibThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Afatinib.
AldesleukinThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Aldesleukin.
AlectinibThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Alectinib.
Aminosalicylic acidThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Aminosalicylic acid.
AmphetamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Teriparatide.
AvapritinibThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Avapritinib.
AxitinibThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Axitinib.
Interactions
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Food Interactions
  • Take with or without food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Teriparatide acetate9959P4V12N99294-94-7Not applicable
International/Other Brands
Forsteo (Eli Lilly and Company)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ForsteoInjection, solution20 μg/80μlSubcutaneousEli Lilly Nederland B.V.2020-12-23Not applicableEU flag
ForsteoInjection, solution20 μg/80μlSubcutaneousEli Lilly Nederland B.V.2020-12-23Not applicableEU flag
ForteoInjection, solution750 ug/3mLSubcutaneousEli Lilly and Company2006-11-152006-11-15US flag
ForteoInjection, solution250 ug/1mLSubcutaneousPhysicians Total Care, Inc.2005-09-062009-11-21US flag
ForteoInjection, solution250 ug/1mLSubcutaneousEli Lilly and Company2002-11-26Not applicableUS flag
ForteoSolution250 mcg / mLSubcutaneousEli Lilly & Co. Ltd.2004-07-15Not applicableCanada flag
LivogivaInjection, solution20 ?g/80?lSubcutaneousTheramex Ireland Limited2021-01-12Not applicableEU flag
LivogivaInjection, solution20 ?g/80?lSubcutaneousTheramex Ireland Limited2021-01-12Not applicableEU flag
MovymiaInjection, solution20 ?g/80?lSubcutaneousStada Arzneimittel Ag2020-12-16Not applicableEU flag
MovymiaInjection, solution20 ?g/80?lSubcutaneousStada Arzneimittel Ag2020-12-16Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-teriparatide InjectionSolution250 mcg / mLSubcutaneousApotex CorporationNot applicableNot applicableCanada flag
Teva-teriparatide InjectionSolution250 mcg / mLSubcutaneousTEVA Canada Limited2020-07-08Not applicableCanada flag

Categories

ATC Codes
H05AA02 — Teriparatide
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
10T9CSU89I
CAS number
52232-67-4

References

General References
  1. Stroup J, Kane MP, Abu-Baker AM: Teriparatide in the treatment of osteoporosis. Am J Health Syst Pharm. 2008 Mar 15;65(6):532-9. doi: 10.2146/ajhp070171. [Article]
  2. Close P, Neuprez A, Reginster JY: Developments in the pharmacotherapeutic management of osteoporosis. Expert Opin Pharmacother. 2006 Aug;7(12):1603-15. [Article]
KEGG Drug
D06078
PubChem Substance
347910346
RxNav
32915
ChEMBL
CHEMBL525610
Therapeutic Targets Database
DAP000396
PharmGKB
PA451620
Drugs.com
Drugs.com Drug Page
Wikipedia
Teriparatide
MSDS
Download (24.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingDiagnosticPostmenopausal Osteoporosis / Type 2 Diabetes Mellitus1
4CompletedTreatmentAdult Degenerative Lumbar Scoliosis / Lumbar Spondylolisthesis / Spondylosis Lumbar1
4CompletedTreatmentAtypical Femoral Fractures / Osteoporosis1
4CompletedTreatmentBone Loss / Osteoporosis / Spinal Cord Injuries (SCI)1
4CompletedTreatmentHumeral Fractures1
4CompletedTreatmentOsteogenesis Imperfecta (OI)1
4CompletedTreatmentOsteoporosis10
4CompletedTreatmentOsteoporosis, Osteopenia1
4CompletedTreatmentPostmenopausal Osteoporosis10
4CompletedTreatmentRheumatoid Arthritis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Eli Lilly & Co.
  • Physicians Total Care Inc.
Dosage Forms
FormRouteStrength
SolutionSubcutaneous250 mcg
Injection, solutionSubcutaneous20 μg/80μl
SolutionSubcutaneous
Injection, solutionSubcutaneous250 mcg/1ml
Injection, solutionSubcutaneous250 ug/1mL
Injection, solutionSubcutaneous750 ug/3mL
Injection, solutionSubcutaneous
Injection, solutionSubcutaneous750 mcg/3ml
Injection, solutionParenteral; Subcutaneous20 mcg/80mcL
Injection, solutionSubcutaneous20 mcg/80ml
Injection, solutionSubcutaneous20 ?g/80?l
SolutionSubcutaneous250 mcg/1ml
SolutionSubcutaneous750 mcg
Injection, solutionParenteral
Powder1 g/1g
Injection, solutionSubcutaneous250 mcg/ml
Injection, solutionParenteral; Subcutaneous20 MCG/80MCG
Injection, solutionSubcutaneous20 mcg/80mcL
SolutionSubcutaneous250 mcg / mL
Prices
Unit descriptionCostUnit
Forteo 750 mcg/3 ml pen295.26USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2314313No2005-02-082018-12-08Canada flag
CA2325371No2004-08-172019-08-19Canada flag
US6770623No2004-08-032018-12-08US flag
US6977077No2005-12-202019-08-19US flag
US7163684No2007-01-162019-08-19US flag
US7351414No2008-04-012019-08-19US flag
US7550434No2009-06-232018-12-08US flag
US7144861No2006-12-052018-12-08US flag
US7517334No2009-04-142025-03-25US flag

Properties

State
Liquid
Experimental Properties
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Protein self-association
Specific Function
This is a receptor for parathyroid hormone and for parathyroid hormone-related peptide. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and also a phosphatid...
Gene Name
PTH1R
Uniprot ID
Q03431
Uniprot Name
Parathyroid hormone/parathyroid hormone-related peptide receptor
Molecular Weight
66359.98 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Ferrari SL, Behar V, Chorev M, Rosenblatt M, Bisello A: Endocytosis of ligand-human parathyroid hormone receptor 1 complexes is protein kinase C-dependent and involves beta-arrestin2. Real-time monitoring by fluorescence microscopy. J Biol Chem. 1999 Oct 15;274(42):29968-75. [Article]

Drug created on March 19, 2008 16:21 / Updated on October 18, 2021 04:56