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1603 details
Primary information
ThPP IDTh1129
Therapeutic Peptide/Protein NameTesamorelin
SequenceYADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL view full sequnce in fasta
Functional ClassificationIb
Molecular Weight5135.9
Chemical FormulaC221H366N72O67S • xC2H4O2 where x averages 7.4 acetate counter ions per peptide molecule
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life26 and 38 minutes
DescriptionStabilized synthetic peptide analogue of Growth Hormone Releasing Hormone (GHRH). It is used to treat excess abdominal fat in HIV-infected patients with lipodystrophy. It is a metabolic condition characterized by insulin resistance, fat redistribution and hyperlipidemia associated with antiretroviral therapy for HIV infection.
Indication/DiseaseTesamorelin 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.
PharmacodynamicsTesamorelin stimulates growth hormone secretion, and subsequently increases IGF-1 and IGFBP-3 levels.
Mechanism of ActionBy 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.
ToxicityDiarrhea, congestive heart failure, peripheral neuropathy, and loss of mobility were the four serious adverse events reported during the clinical studies
MetabolismNo formal metabolism studies have been performed in humans.
AbsorptionThe absolute bioavailability was determined to be less than 4% in healthy adult subjects following a 2 mg subcutaneous dose.
Volume of Distribution9.4±3.1 L/kg in healthy subjects.10.5±6.1 L/kg in HIV-infected patients.
ClearanceN.A.
CategoriesN.A.
Patents NumberUS5861379
Date of Issue30/11/15
Date of Expiry27/05/19
Drug InteractionN.A.
TargetGrowth hormone-releasing hormone receptor
Information of corresponding available drug in the market
Brand NameEgrifta
CompanyTheratechnologies
Brand DiscriptionEGRIFTA contains tesamorelin (as the acetate salt), an analog of human growth hormone-releasing factor (GRF). The peptide precursor of tesamorelin acetate is produced synthetically and is comprised of the 44 amino acid sequence of human GRF. Tesamorelin acetate is made by attaching a hexenoyl moiety, a C6 chain with a double bond at position 3, to the tyrosine residue at the N-terminal part of the molecule. The molecular formula of tesamorelin acetate is C221H366N72O67S • x C2H4O2 (x ≈7) and its molecular weight (free base) is 5135.9 Daltons.
Prescribed forexcess abdominal fat in HIV-infected patients with lipodystrophy
Chemical NameN.A.
FormulationAfter reconstitution with the supplied diluent (Sterile Water for Injection, USP), a solution of EGRIFTA is clear and colorless. Each single-use vial of EGRIFTA contains 2 mg of tesamorelin as the free base (2.2 mg tesamorelin acetate, anhydrous) and the following inactive ingredient: 100 mg mannitol, USP.
Physcial AppearnceEGRIFTA is a sterile, white to off-white, preservative-free lyophilized powder for subcutaneous injection
Route of AdministrationSubcutaneous
Recommended DosageThe recommended dose of EGRIFTA is 2 mg injected subcutaneously once a day.
ContraindicationDisruption of the Hypothalamic-pituitary Axis, Active Malignancy, Hypersensitivity and Pregnancy
Side Effectsrash, urticaria, arthralgia, extremity pain, peripheral edema, hyperglycemia, carpal tunnel syndrome, erythema, pruritis, pain, urticaria, irritation, swelling, hemorrhage
Useful Link http://www.rxlist.com/egrifta-drug.htm http://www.egrifta.com/ http://www.drugs.com/egrifta.html
PubMed ID22926095, 22298602, 22096409, 22050344, 21687371
3-D StructureTh1129 (View) or (Download)