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Th1129 details

Primary information
ID 1603
ThPP ID Th1129
Therapeutic Peptide/Protein Name Tesamorelin
Sequence YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL view full sequnce in fasta
Functional Classification Ib
Molecular Weight 5135.9
Chemical Formula C221H366N72O67S â€¢ xC2H4O2 where x averages 7.4 acetate counter ions per peptide molecule
Isoelectric Point N.A.
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life 26 and 38 minutes
Description Stabilized 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/Disease 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.
Pharmacodynamics 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.
Toxicity Diarrhea, congestive heart failure, peripheral neuropathy, and loss of mobility were the four serious adverse events reported during the clinical studies
Metabolism No formal metabolism studies have been performed in humans.
Absorption The absolute bioavailability was determined to be less than 4% in healthy adult subjects following a 2 mg subcutaneous dose.
Volume of Distribution 9.4Â±3.1 L/kg in healthy subjects.10.5Â±6.1 L/kg in HIV-infected patients.
Clearance N.A.
Categories N.A.
Patents Number US5861379
Date of Issue 30/11/15
Date of Expiry 27/05/19
Drug Interaction N.A.
Target Growth hormone-releasing hormone receptor
Information of corresponding available drug in the market
Brand Name Egrifta
Company Theratechnologies
Brand Discription EGRIFTA 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 â€¢ x C2H4O2 (x â‰ˆ7) and its molecular weight (free base) is 5135.9 Daltons.
Prescribed for excess abdominal fat in HIV-infected patients with lipodystrophy
Chemical Name N.A.
Formulation After 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 Appearance EGRIFTA is a sterile, white to off-white, preservative-free lyophilized powder for subcutaneous injection
Route of Administration Subcutaneous
Recommended Dosage The recommended dose of EGRIFTA is 2 mg injected subcutaneously once a day.
Contraindication Disruption of the Hypothalamic-pituitary Axis, Active Malignancy, Hypersensitivity and Pregnancy
Side Effects rash, 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 ID 22926095, 22298602, 22096409, 22050344, 21687371
3-D Structure Th1129 (View) or (Download)

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

Primary information
ID	1603
ThPP ID	Th1129
Therapeutic Peptide/Protein Name	Tesamorelin
Sequence	YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL view full sequnce in fasta
Functional Classification	Ib
Molecular Weight	5135.9
Chemical Formula	C221H366N72O67S â€¢ xC2H4O2 where x averages 7.4 acetate counter ions per peptide molecule
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	26 and 38 minutes
Description	Stabilized 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/Disease	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.
Pharmacodynamics	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.
Toxicity	Diarrhea, congestive heart failure, peripheral neuropathy, and loss of mobility were the four serious adverse events reported during the clinical studies
Metabolism	No formal metabolism studies have been performed in humans.
Absorption	The absolute bioavailability was determined to be less than 4% in healthy adult subjects following a 2 mg subcutaneous dose.
Volume of Distribution	9.4Â±3.1 L/kg in healthy subjects.10.5Â±6.1 L/kg in HIV-infected patients.
Clearance	N.A.
Categories	N.A.
Patents Number	US5861379
Date of Issue	30/11/15
Date of Expiry	27/05/19
Drug Interaction	N.A.
Target	Growth hormone-releasing hormone receptor
Information of corresponding available drug in the market
Brand Name	Egrifta
Company	Theratechnologies
Brand Discription	EGRIFTA 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 â€¢ x C2H4O2 (x â‰ˆ7) and its molecular weight (free base) is 5135.9 Daltons.
Prescribed for	excess abdominal fat in HIV-infected patients with lipodystrophy
Chemical Name	N.A.
Formulation	After 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 Appearance	EGRIFTA is a sterile, white to off-white, preservative-free lyophilized powder for subcutaneous injection
Route of Administration	Subcutaneous
Recommended Dosage	The recommended dose of EGRIFTA is 2 mg injected subcutaneously once a day.
Contraindication	Disruption of the Hypothalamic-pituitary Axis, Active Malignancy, Hypersensitivity and Pregnancy
Side Effects	rash, 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 ID	22926095, 22298602, 22096409, 22050344, 21687371
3-D Structure	Th1129 (View) or (Download)