| 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 • 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 | 9.4±3.1 L/kg in healthy subjects.10.5±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 • x C2H4O2 (x ≈7) 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) |