Identification
- Summary
Tesamorelin is a growth hormone releasing factor (GRF) analog used to reduce excessive abdominal fat in HIV patients who have developed lipodystrophy.
- Brand Names
- Egrifta
- Generic Name
- Tesamorelin
- DrugBank Accession Number
- DB08869
- Background
Tesamorelin is a stabilized synthetic peptide analogue of the hypothalamic peptide, Growth Hormone Releasing Hormone (GHRH) indicated for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. Lipodystrophy is a metabolic condition characterized by insulin resistance, fat redistribution, and hyperlipidemia associated with antiretroviral therapy for HIV infection.
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
>results for sequence "Egrifta Sequence" starting "TyrAlaAspAla" YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL
Download FASTA Format- Synonyms
- GHRH(1-44)
- N-[(3E)-1-oxo-3-hexenyl]Somatoliberin (human pancreatic islet)
- Tesamorelin
- External IDs
- TH-9507
- TH9507
Pharmacology
- Indication
Tesamorelin acetate is a synthetic analogue of human hypothalamic Growth Hormone Releasing Factor (hGRF) indicated to induce and maintain a reduction of excess abdominal fat in HIV-infected patients with lipodystrophy.
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
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Lipodystrophy •••••••••••• - Contraindications & Blackbox Warnings
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Tesamorelin stimulates growth hormone secretion, and subsequently increases IGF-1 and IGFBP-3 levels.
- Mechanism of action
By acting on the pituitary cells in the brain, tesamorelin stimulates production and release of the endogenous hormone (hGRF). Tesamorelin therapy predisposes the patient to glucose intolerance and can also increase the risk of type 2 diabetes, so the drug is contraindicated in pregnancy.
Target Actions Organism AGrowth hormone-releasing hormone receptor binderHumans - Absorption
The absolute bioavailability was determined to be less than 4% in healthy adult subjects following a 2 mg subcutaneous dose.
- Volume of distribution
9.4±3.1 L/kg in healthy subjects. 10.5±6.1 L/kg in HIV-infected patients.
- Protein binding
Not Available
- Metabolism
No formal metabolism studies have been performed in humans.
- Route of elimination
Not Available
- Half-life
26 and 38 minutes in healthy subjects and HIV-infected patients, respectively.
- Clearance
Not Available
- Adverse Effects
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Diarrhea, congestive heart failure, peripheral neuropathy, and loss of mobility were the four serious adverse events reported during the clinical studies
- 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 softwareCortisone acetate The serum concentration of the active metabolites of Cortisone acetate can be reduced when Cortisone acetate is used in combination with Tesamorelin resulting in a loss in efficacy. Prednisolone The serum concentration of the active metabolites of Prednisolone can be reduced when Prednisolone is used in combination with Tesamorelin resulting in a loss in efficacy. Prednisone The serum concentration of the active metabolites of Prednisone can be reduced when Prednisone is used in combination with Tesamorelin resulting in a loss in efficacy. - Food Interactions
- No interactions found.
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 Tesamorelin acetate LGW5H38VE3 901758-09-6 Not applicable - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Egrifta Kit; Powder, for solution 1 mg / vial Subcutaneous Theratechnologies 2015-06-23 2022-09-30 Canada 
Egrifta Kit 1 mg/1mL Subcutaneous Theratechnologies Inc. 2014-07-14 2020-07-31 US 
Egrifta Kit 1 mg/1mL Subcutaneous Emd Serono 2010-12-16 2014-11-30 US Egrifta Kit; Powder, for solution 2 mg / vial Subcutaneous Theratechnologies Not applicable Not applicable Canada Egrifta Kit 2 mg/0.5mL Subcutaneous Theratechnologies Inc. 2019-07-01 2019-07-01 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Egrifta Tesamorelin acetate (2 mg/2mL) + Water (1 mL/1mL) Kit Subcutaneous EMD Serono, Inc. 2012-09-05 2016-10-31 US
Categories
- ATC Codes
- H01AC06 — Tesamorelin
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Anterior Pituitary Lobe Hormones and Analogues
- Growth Hormone Releasing Factor Analog
- Growth Hormone-Releasing Hormone
- Growth Substances
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypothalamic Hormones
- Increased GHRH Activity
- Lipodystrophy
- Nerve Tissue Proteins
- Neuropeptides
- Peptide Hormones
- Peptides
- Pituitary and Hypothalamic Hormones and Analogues
- Pituitary Hormone-Releasing Hormones
- Proteins
- Somatotropin Agonists
- Somatropin and Somatropin Agonists
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- 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
- MQG94M5EEO
- CAS number
- 218949-48-5
References
- General References
- Spooner LM, Olin JL: Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. Ann Pharmacother. 2012 Feb;46(2):240-7. doi: 10.1345/aph.1Q629. Epub 2012 Jan 31. [Article]
- McLarnon A: Neuroendocrinology: Tesamorelin can improve cognitive function. Nat Rev Endocrinol. 2012 Oct;8(10):568. doi: 10.1038/nrendo.2012.151. Epub 2012 Aug 28. [Article]
- Bedimo R: Growth hormone and tesamorelin in the management of HIV-associated lipodystrophy. HIV AIDS (Auckl). 2011;3:69-79. doi: 10.2147/HIV.S14561. Epub 2011 Jul 10. [Article]
- Dhillon S: Spotlight on tesamorelin in HIV-associated lipodystrophy. BioDrugs. 2011 Dec 1;25(6):405-8. doi: 10.2165/11208290-000000000-00000. [Article]
- Garg A: Acquired and inherited lipodystrophies. N Engl J Med. 2004 Mar 18;350(12):1220-34. [Article]
- Patel A, Gandhi H, Upaganlawar A: Tesamorelin: A hope for ART-induced lipodystrophy. J Pharm Bioallied Sci. 2011 Apr;3(2):319-20. doi: 10.4103/0975-7406.80763. [Article]
- Campbell RM, Lee Y, Rivier J, Heimer EP, Felix AM, Mowles TF: GRF analogs and fragments: correlation between receptor binding, activity and structure. Peptides. 1991 May-Jun;12(3):569-74. [Article]
- External Links
- UniProt
- P01286
- KEGG Drug
- D09015
- PubChem Compound
- 56928011
- PubChem Substance
- 347827804
- ChemSpider
- 34999256
- 1044584
- ChEBI
- 63626
- ChEMBL
- CHEMBL1237026
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Tesamorelin
- FDA label
- Download (1.53 MB)
- MSDS
- Download (568 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Recruiting Treatment Bodycomposition / HIV Lipodystrophy Syndrome / Human Growth Hormone Deficiency 1 4 Terminated Prevention Diabetic Retinopathy (DR) / Human Immunodeficiency Virus (HIV) Infections 1 3 Completed Treatment Human Immunodeficiency Virus (HIV) Infections / Lipodystrophies 2 2 Active Not Recruiting Treatment Fatty Liver / Fatty Liver, Non-alcoholic Fatty Liver Disease, NAFLD / Liver Fat / Obesity / Obesity, Abdominal 1 2 Active Not Recruiting Treatment Mild Cognitive Impairment (MCI) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Kit Subcutaneous Kit Subcutaneous 1 mg/1mL Kit Subcutaneous 2 mg/2mL Kit; powder, for solution Subcutaneous 1 mg / vial Kit; powder, for solution Subcutaneous 2 mg / vial Solution Subcutaneous 2.000 mg Kit Subcutaneous 2 mg/0.5mL - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7144577 No 2006-12-05 2020-07-14 US US7316997 No 2008-01-08 2023-08-14 US US5861379 No 1999-01-19 2020-05-26 US US8314066 No 2012-11-20 2023-08-14 US US8435945 No 2013-05-07 2023-08-14 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source isoelectric point 10.54 http://www.phosphosite.org/proteinAction.do?id=19016&showAllSites=true
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General Function
- Peptide hormone binding
- Specific Function
- Receptor for GRF, coupled to G proteins which activate adenylyl cyclase. Stimulates somatotroph cell growth, growth hormone gene transcription and growth hormone secretion.
- Gene Name
- GHRHR
- Uniprot ID
- Q02643
- Uniprot Name
- Growth hormone-releasing hormone receptor
- Molecular Weight
- 47401.53 Da
References
- Spooner LM, Olin JL: Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. Ann Pharmacother. 2012 Feb;46(2):240-7. doi: 10.1345/aph.1Q629. Epub 2012 Jan 31. [Article]
Drug created at May 01, 2013 00:36 / Updated at April 19, 2024 20:55