| Primary information |
|---|
| ThPP ID | Th1069 |
| Therapeutic Peptide/Protein Name | Pegvisomant |
| Sequence | FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQT view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 22129 |
| Chemical Formula | C990H1532N262O300S7 |
| Isoelectric Point | 5.27 |
| Hydrophobicity | -0.411 |
| Melting Point (℃) | 76 |
| Half Life | 6 days |
| Description | Pegvisomant is a highly selective growth hormone (GH) receptor antagonist. It is used to treat acromegaly. Unlike dopamine or somatostatin analogs (which inhibit growth hormone secretion), this drug actually blocks the hepatic (GH-mediated) production of insulin like growth factor (IGF-1), which is the main mediator of growth hormone activity. |
| Indication/Disease | Pegvisomant is a growth hormone receptor antagonist used for the treatment of acromegaly. |
| Pharmacodynamics | Somavert is used for the treatment of acromegaly, which arises from excessive IGF-1 levels. Somavert selectively binds to growth hormone (GH) receptors on cell surfaces, where it blocks the binding of endogenous GH, and thus interferes with GH signal transduction. Inhibition of GH action results in decreased serum concentrations of insulin-like growth factor-I (IGF-I), and IGF binding protein-3 (IGFBP-3). This reduces the symptoms of acromegaly. |
| Mechanism of Action | Somavert selectively binds to growth hormone (GH) receptors on cell surfaces, where it blocks the binding of endogenous GH. This leads to the normalization of serum IGF-1 levels. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | 7 L |
| Clearance | 36 ± 28 mL/h [SC doses ranging from 10 to 20 mg/day] |
| Categories | Hormone Replacement Agents |
| Patents Number | US5849535 |
| Date of Issue | 26/03/01 |
| Date of Expiry | 26/03/21 |
| Drug Interaction | Dihydrocodeine opioids may diminish the therapeutic effect of pegvisomant. It is recommended to monitor therapy |
| Target | N.A. |
| Information of corresponding available drug in the market |
|---|
| Brand Name | SOMAVERT |
| Company | Pfizer |
| Brand Discription | SOMAVERT contains pegvisomant, an analog of human growth hormone (GH) that has been structurally altered to act as a GH receptor antagonist.Pegvisomant is a protein of recombinant DNA origin containing 191 amino acid residues to which several polyethylene glycol (PEG) polymers are covalently bound (predominantly 4 to 6 PEG/protein molecule). The molecular weight of the protein of pegvisomant is 21,998 Daltons. |
| Prescribed for | SOMAVERT is indicated for the treatment of acromegaly in patients who have had an inadequate response to surgery or radiation therapy, or for whom these therapies are not appropriate. The goal of treatment is to normalize serum insulin-like growth factor-I (IGF-I) levels. |
| Chemical Name | N.A. |
| Formulation | SOMAVERT is available in single-dose sterile vials containing 10, 15, or 20 mg of pegvisomant protein (approximately 10, 15, and 20 U activity, respectively). Each vial also contains 1.36 mg of glycine, 36.0 mg of mannitol, 1.04 mg of sodium phosphate dibasic anhydrous, and 0.36 mg of sodium phosphate monobasic monohydrate |
| Physcial Appearnce | SOMAVERT for injection is supplied as a Sterile, white lyophilized powder |
| Route of Administration | Subcutaneous Injection |
| Recommended Dosage | The recommended loading dose of SOMAVERT is 40 mg given subcutaneously, under healthcare provider supervision. Increase the dosage by 5 mg increments every 4-6 weeks if IGF-I concentrations are elevated.Decrease the dosage by 5 mg decrements every 4-6 weeks if IGF-I concentrations are below the normal range. |
| Contraindication | None. |
| Side Effects | Hypoglycemia associated with GH lowering in patients with Diabetes Mellitus, Liver test elevations, Cross-reactivity with GH assay, Lipohypertrophy, Systemic hypersensitivity, pain, nausea ,diarrhea, dizziness, Sinusitis |
| Useful Link | http://www.rxlist.com/somavert-drug.htm http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=222a28ca-70c3-474c-850e-fae39eaaf40f |
| PubMed ID | 20444908, 18778113, 17207591, 16311417, 15134290, 15006735, 14499709, 12200225, 11932320 |
| 3-D Structure | Th1069 (View) or (Download) |