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 is a recombinant parathyroid hormone (PTH) analog and a potent osteoanabolic agent.2 It is made up of the first amino(N)-terminal 34 amino acids of the human PTH.2 First approved in the United States in November 2002 and in Europe in April 2003,3 teriparatide makes the first approved drug in a new category of osteoporosis therapy called anabolic therapy.2 Teriparatide is used in the treatment of osteoporosis in men and women.4,5
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Chemical Formula
- C181H291N55O51S2
- Protein Average Weight
- 4117.715 Da
- Sequences
>Sequence SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF
Download FASTA FormatReferences:
- KEGG DRUG: Teriparatide [Link]
- Synonyms
- PTH (1-34)
- PTH 1-34
- Teriparatida
- Teriparatide
- Teriparatide recombinant human
- External IDs
- LY 333334
- LY-333334
- LY333334
- ZT-034
Pharmacology
- Indication
Teriparatide is indicated:
- for the treatment of postmenopausal women with osteoporosis at high risk for fracture (defined herein as having a history of osteoporotic fracture or multiple risk factors for fracture) or who have failed or are intolerant to other available osteoporosis therapy. In postmenopausal women with osteoporosis, teriparatide reduces the risk of vertebral and nonvertebral fractures.4,5,7,8
- to increase bone mass in men with primary or hypogonadal osteoporosis at high risk for fracture or who have failed or are intolerant to other available osteoporosis therapy.4,5,7,8
- for the treatment of men and women with osteoporosis associated with sustained systemic glucocorticoid therapy (daily dosage equivalent to 5 mg or greater of prednisone) at high risk for fracture or who have failed or are intolerant to other available osteoporosis therapy.4,5,7,8
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Teriparatide is a PTH analog that works to stimulate bone formation in both men and women. It increases skeletal mass, increases markers of bone formation such as bone-specific alkaline phosphatase (BSAP) and procollagen I carboxy-terminal propeptide (PICP), and increases bone strength.4
Like endogenous PTH, teriparatide affects calcium and phosphate homeostasis. It causes a transient increase in serum calcium levels and increases urinary calcium excretion. In clinical trials, it also produced transient phosphaturia and mild transient reductions in serum phosphorus concentration.4
- Mechanism of action
Parathyroid hormone (PTH) is an endogenous hormone that regulates calcium and phosphate metabolism in bone and kidney. It regulates bone metabolism, renal tubular reabsorption of calcium and phosphate, and intestinal calcium absorption. It mediates its physiological actions by binding to the PTH receptors.4 Excess PTH - such as in certain disease states like hyperparathyroidism - can cause increased osteoclast activity and accelerated bone resorption. Interestingly, the effects of PTH depend on the dose and pattern of exposure of PTH to the bone. Continuous exposure to PTH promotes bone resorption, whereas intermittent exposure to low-dose PTH can induce bone formation more favourably than bone resorption.2
Similarly, teriparatide's skeletal effects depend upon the systemic exposure pattern. Once-daily administration of teriparatide stimulates new bone formation on trabecular and cortical (periosteal and/or endosteal) bone surfaces by preferential stimulation of osteoblastic activity over osteoclastic activity.4 Teriparatide mediates its osteoanabolic actions by binding to the N-terminal moiety to PTH type 1 receptors (PTH type 1R), which are G-protein coupled receptors expressed on various cells, including osteoblasts, osteocytes, and renal tubular cells.2 Binding of teriparatide to PTH receptors on osteoblasts activates the downstream PKA- and PKC-dependent signaling pathways that promotes anabolic effects on bone.1,2 For example, teriparatide increases expression of pro-osteoclastogenic cytokines like receptor activator of nuclear factor kappa-B ligand (RANKL) and macrophage colony-stimulating factor. It also upregulates transcriptional expression of pro-osteoblastogenic growth factors like insulin-like growth factor 1 (IGF1) and fibroblast growth factor 2 (FGF2). Teriparatide also downregulates the synthesis of sclerostin, which is a negative regulator of bone formation. It also promotes the differentiation of osteoblasts.2
Target Actions Organism UParathyroid hormone/parathyroid hormone-related peptide receptor ligandHumans - Absorption
The absolute bioavailability is approximately 95%. The peptide reaches peak serum concentrations about 30 minutes after subcutaneous injection of a 20 mcg dose and declines to non-quantifiable concentrations within three hours.4
- Volume of distribution
The volume of distribution following intravenous injection is approximately 0.12 L/kg. Teriparatide is not expected to accumulate in bone or other tissues.4
- Protein binding
There is no information available.
- Metabolism
No metabolism studies have been performed with teriparatide. Peripheral metabolism of PTH is believed to occur by non-specific enzymatic mechanisms in the liver.4
- Route of elimination
No excretion studies have been performed with teriparatide. It is believed to be excreted via the kidneys.4
- Half-life
The half-life of teriparatide in serum was approximately one hour following subcutaneous administration.4
- Clearance
Systemic clearance of teriparatide is approximately 62 L/hour in women and 94 L/hour in men. It exceeds the rate of normal liver plasma flow, consistent with both hepatic and extra-hepatic clearance.4
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The subcutaneous and intravenous lethal dose (LD) in rats are 1000 µg/m3 and 300 µg/m3, respectively.6
Few post-marketing reports illustrate cases of medication errors where patients accidentally received up to a single 800 mcg dose of teriparatide, which is 40 times the recommended dose. Patients experienced nausea, weakness or lethargy, and hypotension. No deaths have been reported from teriparatide overdose. Additional signs, symptoms, and complications of overdosage may include a delayed hypercalcemic effect, vomiting, dizziness, and headache.4
There is no specific antidote for a teriparatide overdosage. Treatment of suspected overdosage should include discontinuation of teriparatide, monitoring of serum calcium and phosphorus, and implementation of appropriate supportive measures, such as hydration.4
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcalabrutinib The therapeutic efficacy of Teriparatide can be decreased when used in combination with Acalabrutinib. Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Teriparatide. Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Teriparatide. Afatinib The therapeutic efficacy of Teriparatide can be decreased when used in combination with Afatinib. Aldesleukin The therapeutic efficacy of Teriparatide can be decreased when used in combination with Aldesleukin. Alectinib The therapeutic efficacy of Teriparatide can be decreased when used in combination with Alectinib. Aminosalicylic acid The therapeutic efficacy of Teriparatide can be decreased when used in combination with Aminosalicylic acid. Amphetamine The risk or severity of adverse effects can be increased when Amphetamine is combined with Teriparatide. Avapritinib The therapeutic efficacy of Teriparatide can be decreased when used in combination with Avapritinib. Axitinib The therapeutic efficacy of Teriparatide can be decreased when used in combination with Axitinib. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Teriparatide acetate 9959P4V12N 99294-94-7 Not applicable - International/Other Brands
- Forsteo (Eli Lilly and Company)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Forsteo Injection, solution 20 μg/80μl Subcutaneous Eli Lilly Nederland B.V. 2020-12-23 Not applicable EU 
Forsteo Injection, solution 20 μg/80μl Subcutaneous Eli Lilly Nederland B.V. 2020-12-23 Not applicable EU Forteo Injection, solution 750 ug/3mL Subcutaneous Eli Lilly and Company 2006-11-15 2006-11-15 US 
Forteo Injection, solution 250 ug/1mL Subcutaneous Physicians Total Care, Inc. 2005-09-06 2009-11-21 US Forteo Solution 250 mcg / mL Subcutaneous Eli Lilly & Co. Ltd. 2004-07-15 Not applicable Canada 
Forteo Injection, solution 250 ug/1mL Subcutaneous Eli Lilly and Company 2002-11-26 Not applicable US Kauliv Injection, solution 20 µg/80µl Strides Pharma (Cyprus) Limited 2023-03-14 Not applicable EU Kauliv Injection, solution 20 µg/80µl Strides Pharma (Cyprus) Limited 2023-03-14 Not applicable EU Livogiva Injection, solution 20 ?g/80?l Subcutaneous Theramex Ireland Limited 2021-01-12 Not applicable EU Livogiva Injection, solution 20 ?g/80?l Subcutaneous Theramex Ireland Limited 2021-01-12 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-teriparatide Injection Solution 250 mcg / mL Subcutaneous Apotex Corporation Not applicable Not applicable Canada Teva-teriparatide Injection Solution 250 mcg / mL Subcutaneous TEVA Canada Limited 2020-07-08 Not applicable Canada
Categories
- ATC Codes
- H05AA02 — Teriparatide
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Bone Anabolic Agents
- Bone Density Conservation Agents
- Calcium Homeostasis
- Calcium-Regulating Hormones and Agents
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Parathyroid Agents
- Parathyroid Hormones and Analogues
- Peptide Hormones
- Peptides
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- Thyroid Products
- 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
- 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]
- Vall H, Parmar M: Teriparatide . [Article]
- Quattrocchi E, Kourlas H: Teriparatide: a review. Clin Ther. 2004 Jun;26(6):841-54. doi: 10.1016/s0149-2918(04)90128-2. [Article]
- FDA Approved Drug Products: FORTEO (teriparatide) injection, for subcutaneous use [Link]
- EMA Approved Drug Products: Sondelbay (teriparatide) Subcutaneous Injection [Link]
- Eli Lilly and Company: Forteo (Teriparatide) MSDS [Link]
- EMA Approved Drug Products: Kauliv (teriparatide) Subcutaneous Injection [Link]
- Health Canada Approved Drug Products: FORTEO (teriparatide) Subcutaneous Injection [Link]
- External Links
- KEGG Drug
- D06078
- PubChem Substance
- 347910346
- 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
Phase Status Purpose Conditions Count 4 Completed Diagnostic Postmenopausal Osteoporosis / Type 2 Diabetes Mellitus 1 4 Completed Other Postmenopausal Osteoporosis 1 4 Completed Treatment Adult Degenerative Lumbar Scoliosis / Spondylolisthesis, Lumbar Region / Spondylosis Lumbar 1 4 Completed Treatment Atypical Femoral Fractures / Osteoporosis 1 4 Completed Treatment Bone Loss / Osteoporosis / Spinal Cord Injuries 1 4 Completed Treatment Humeral Fractures 1 4 Completed Treatment Osteogenesis Imperfecta (OI) 1 4 Completed Treatment Osteoporosis 10 4 Completed Treatment Osteoporosis, Osteopenia 1 4 Completed Treatment Postmenopausal Osteoporosis 10
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Eli Lilly & Co.
- Physicians Total Care Inc.
- Dosage Forms
Form Route Strength Injection, solution Subcutaneous 20 μg/80μl Solution Subcutaneous 20 mcg/80mcL Injection, solution Subcutaneous 250 mcg/1ml Injection, solution Subcutaneous 250 ug/1mL Injection, solution Subcutaneous 750 ug/3mL Solution Subcutaneous 250 mcg / mL Injection, solution Subcutaneous Injection, solution Subcutaneous 750 mcg/3ml Solution Subcutaneous 250 mcg Injection, solution 20 µg/80µl Injection, solution Parenteral; Subcutaneous 20 mcg/80mcL Injection, solution Subcutaneous 20 mcg/80ml Injection, solution Subcutaneous 20 ?g/80?l Solution Subcutaneous 250 mcg/1ml Solution Subcutaneous 750 mcg Injection, solution Parenteral Powder 1 g/1g Injection, solution Subcutaneous 250 mcg/ml Injection, solution Parenteral; Subcutaneous 20 MCG/80MCG Injection, solution Subcutaneous 20 mcg/80mcL Solution Subcutaneous 0.25 mg - Prices
Unit description Cost Unit Forteo 750 mcg/3 ml pen 295.26USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2314313 No 2005-02-08 2018-12-08 Canada CA2325371 No 2004-08-17 2019-08-19 Canada US6770623 No 2004-08-03 2018-12-08 US US6977077 No 2005-12-20 2019-08-19 US US7163684 No 2007-01-16 2019-08-19 US US7351414 No 2008-04-01 2019-08-19 US US7550434 No 2009-06-23 2018-12-08 US US7144861 No 2006-12-05 2018-12-08 US US7517334 No 2009-04-14 2025-03-25 US
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- 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
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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]
- Vall H, Parmar M: Teriparatide . [Article]
Drug created at March 19, 2008 16:21 / Updated at May 26, 2023 16:43