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| Primary information |
|---|
| ID | 10631 |
| Therapeutic ID | Th1129 |
| Protein Name | Tesamorelin |
| Sequence | >Th1129_Tesamorelin
YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL
|
| Molecular Weight | 5005.76 |
| Chemical Formula | C216H360N72O63S |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | 26 and 38 minutes in healthy subjects and HIV-infected patients, respectively. |
| 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 | NA |
| Metabolism | NA |
| Absorption | NA |
| NA |
| Clearance | NA |
| Categories | NA |
| Patents Number | US5861379 |
| Date of Issue | 19-01-1999 |
| Date of Expiry | 26-05-2020 |
| Drug Interaction | NA |
| Target | Growth hormone-releasing hormone receptor |
| Brand Name | Egrifta |
| Company | Theratechnologies |
| Brand Description | Theratechnologies |
| Prescribed For | excess abdominal fat in HIV-infected patients with lipodystrophy |
| Chemical Name | NA |
| 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. |
| Physical 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 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |