Identification

Name
Teriparatide
Accession Number
DB06285  (DB05581)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Hormones
Description

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.

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
  • Teriparatide recombinant human
External IDs
LY 333334 / LY-333334 / LY333334 / ZT-034
Product Ingredients
IngredientUNIICASInChI Key
Teriparatide acetate9959P4V12N99294-94-7Not applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ForteoInjection, solution750 ug/3mLSubcutaneousEli Lilly and Company2006-11-152006-11-15Us
ForteoSolution250 mcgSubcutaneousEli Lilly & Co. Ltd.2004-07-15Not applicableCanada
ForteoInjection, solution250 ug/1mLSubcutaneousEli Lilly & Co. Ltd.2002-11-26Not applicableUs
ForteoInjection, solution250 ug/1mLSubcutaneousPhysicians Total Care, Inc.2005-09-062009-11-21Us
International/Other Brands
Forsteo (Eli Lilly and Company)
Categories
UNII
10T9CSU89I
CAS number
52232-67-4

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.

Associated Conditions
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
Human
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]
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.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
AmitriptylineThe risk or severity of Cardiac Arrhythmia and CNS stimulation can be increased when Teriparatide is combined with Amitriptyline.
AmoxapineThe risk or severity of Cardiac Arrhythmia and CNS stimulation can be increased when Teriparatide is combined with Amoxapine.
Calcium GluceptateThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Calcium Gluceptate.
CitalopramThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Citalopram.
ColesevelamColesevelam can cause a decrease in the absorption of Teriparatide resulting in a reduced serum concentration and potentially a decrease in efficacy.
ColestipolColestipol can cause a decrease in the absorption of Teriparatide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Conjugated estrogensThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Conjugated estrogens.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Teriparatide.
DuloxetineThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Duloxetine.
EstroneThe therapeutic efficacy of Teriparatide can be decreased when used in combination with Estrone.
Food Interactions
Not Available

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. [PubMed:18319498]
  2. Close P, Neuprez A, Reginster JY: Developments in the pharmacotherapeutic management of osteoporosis. Expert Opin Pharmacother. 2006 Aug;7(12):1603-15. [PubMed:16872263]
External Links
KEGG Drug
D06078
PubChem Substance
347910346
ChEMBL
CHEMBL525610
Therapeutic Targets Database
DAP000396
PharmGKB
PA451620
Drugs.com
Drugs.com Drug Page
Wikipedia
Teriparatide
ATC Codes
H05AA02 — Teriparatide
AHFS Codes
  • 68:24.00 — Parathyroid
MSDS
Download (24.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers1
1CompletedTreatmentBone Loss / Periodontitis1
1CompletedTreatmentDrug Safety1
1CompletedTreatmentDrug Safety and Bioavailability1
1CompletedTreatmentOsteoporosis, Post-Menopausal1
1CompletedTreatmentPostmenopausal Osteoporosis (PMO)2
1CompletedTreatmentBone destruction1
1Unknown StatusBasic ScienceBone destruction1
2Active Not RecruitingTreatmentAdult Idiopathic Generalized Osteoporosis1
2Active Not RecruitingTreatmentAnorexia Nervosa (AN) / Bone destruction1
2Active Not RecruitingTreatmentDiabetic Neuropathic Arthropathy1
2Active Not RecruitingTreatmentOsteogenesis Imperfecta1
2Active Not RecruitingTreatmentBone destruction1
2CompletedPreventionKnee Osteoarthritis (Knee OA)1
2CompletedTreatmentBone destruction / Bone Loss / Spinal Cord Injuries (SCI)2
2CompletedTreatmentColles' Fracture1
2CompletedTreatmentLow Bone Mineral Density / Postmenopausal Osteoporosis (PMO)1
2CompletedTreatmentOsteoporosis, Post-Menopausal1
2CompletedTreatmentPostmenopausal Osteoporosis (PMO)1
2CompletedTreatmentBone destruction9
2CompletedTreatmentParathyroid deficiency2
2RecruitingTreatmentAutosomal Dominant Hypocalcemia / Autosomal Dominant Hypocalcemia or OR Primary Hypoparathyroidism Related to Other Cause But Complicated by Hypercalciuria Under Treatment1
2RecruitingTreatmentCartilage Degeneration / Knee Osteoarthritis (Knee OA)1
2RecruitingTreatmentOsteoporotic Fractures1
2TerminatedPreventionAgnogenic Myeloid Metaplasia / Aplastic Anaemia (AA) / Chronic Lymphocytic Leukaemia (CLL) / Chronic Myeloid Leukemia (CML) / Hodgkins Disease (HD) / Leukemia, Lymphocytic, Acute / Leukemia, Myelocytic, Acute / Malignant Lymphomas1
2TerminatedTreatmentHypocalcemia1
2TerminatedTreatmentHypoparathyroidism Post-surgical1
2TerminatedTreatmentImplants1
2TerminatedTreatmentBone destruction1
2Unknown StatusTreatmentBone destruction / Osteopenia1
2WithdrawnTreatmentBone destruction / Osteopenia1
2WithdrawnTreatmentShoulder Fractures / Trochanteric Fractures1
2, 3CompletedTreatmentBone destruction / Fracture Bone / Menopause1
2, 3CompletedTreatmentParathyroid deficiency1
3CompletedTreatmentBack Pain / Postmenopausal Osteoporosis (PMO) / Vertebral Fractures1
3CompletedTreatmentDiGeorge's syndrome / Parathyroid deficiency1
3CompletedTreatmentFemur Neck Fracture2
3CompletedTreatmentBone destruction / Osteopenia1
3CompletedTreatmentOsteoporosis, Post-Menopausal3
3CompletedTreatmentPostmenopausal Osteoporosis (PMO)4
3CompletedTreatmentBone destruction / Postmenopausal Osteoporosis (PMO)1
3CompletedTreatmentBone destruction11
3Not Yet RecruitingTreatmentUnstable Intertrochanteric Fracture1
3RecruitingTreatmentNon Displaced Atypical Femoral Fractures1
3Unknown StatusTreatmentLow Bone Mass in Anorexia Nervosa Patients1
3WithdrawnTreatmentHumeral Fractures / Osteoporosis, Age-Related1
4Active Not RecruitingTreatmentPostmenopausal Osteoporosis (PMO)1
4Active Not RecruitingTreatmentRheumatoid Arthritis1
4Active Not RecruitingTreatmentSpinal Stenosis1
4CompletedTreatmentAtypical Femoral Fractures / Bone destruction1
4CompletedTreatmentBone destruction / Bone Loss / Spinal Cord Injuries (SCI)1
4CompletedTreatmentHumeral Fractures1
4CompletedTreatmentOsteogenesis Imperfecta1
4CompletedTreatmentOsteoporosis, Osteopenia1
4CompletedTreatmentOsteoporosis, Post-Menopausal2
4CompletedTreatmentPostmenopausal Osteoporosis (PMO)7
4CompletedTreatmentBone destruction10
4RecruitingDiagnosticPostmenopausal Osteoporosis (PMO) / Type 2 Diabetes Mellitus1
4RecruitingTreatmentFracture, Ankle1
4SuspendedTreatmentBone Marrow Oedema Syndrome / High Turnover Bone Disease / Quality of Life1
4TerminatedTreatmentBone destruction1
4Unknown StatusTreatmentFracture Bone1
4Unknown StatusTreatmentPostmenopausal Osteoporosis With Pathological Fracture1
Not AvailableActive Not RecruitingNot AvailableOsteoporosis, Steroid Induced / Postmenopausal Osteoporosis (PMO)1
Not AvailableActive Not RecruitingNot AvailablePostmenopausal Osteoporosis (PMO) / Quality of Life / Vertebral Fractures1
Not AvailableActive Not RecruitingNot AvailableBone destruction1
Not AvailableActive Not RecruitingOtherLow Bone Density1
Not AvailableActive Not RecruitingTreatmentBone destruction1
Not AvailableCompletedNot AvailableBone destruction / Postmenopausal Osteoporosis (PMO)1
Not AvailableCompletedNot AvailableBone destruction4
Not AvailableCompletedDiagnosticHyperparathyroidism, Secondary1
Not AvailableRecruitingNot AvailableBone destruction1
Not AvailableRecruitingTreatmentAdult Degenerative Lumbar Scoliosis / Lumbar Spondylolisthesis / Lumbar Spondylosis1
Not AvailableRecruitingTreatmentChronic Renal Failure (CRF)1
Not AvailableTerminatedTreatmentFracture of Pelvis1
Not AvailableUnknown StatusTreatmentBone destruction1
Not AvailableWithdrawnTreatmentBone destruction1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Eli Lilly & Co.
  • Physicians Total Care Inc.
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous250 ug/1mL
Injection, solutionSubcutaneous750 ug/3mL
SolutionSubcutaneous250 mcg
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)
CA2314313No2005-02-082018-12-08Canada
CA2325371No2004-08-172019-08-19Canada
US6770623No1998-12-082018-12-08Us
US6977077No1999-08-192019-08-19Us
US7163684No1999-08-192019-08-19Us
US7351414No1999-08-192019-08-19Us
US7550434No1998-12-082018-12-08Us
US7144861No1998-12-082018-12-08Us
US7517334No2005-03-252025-03-25Us

Properties

State
Liquid
Experimental Properties
Not Available

Taxonomy

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

Targets

Kind
Protein
Organism
Human
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. [PubMed:11752352]
  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. [PubMed:10514480]

Drug created on March 19, 2008 10:21 / Updated on October 15, 2018 04:36