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| Primary information |
|---|
| ID | 10415 |
| Therapeutic ID | Th1069 |
| Protein Name | Pegvisomant |
| Sequence | >Th1069_Pegvisomant
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
|
| 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 | NA |
| Metabolism | NA |
| Absorption | NA |
| 7 L |
| Clearance | 36 ± 28 mL/h [SC doses ranging from 10 to 20 mg/day] |
| Categories | Acromegaly, Amino Acids, Peptides, and Proteins, Anterior Pituitary Lobe Hormones and Analogues, Cholinesterase Inhibitors, Cytochrome P-450 CYP3A Inducers, Cytochrome P-450 CYP3A4 Inducers, Cytochrome P-450 CYP3A4 Inducers (strength unknown), Cytochrome P-450 Enzyme Inducers, Growth Hormone Receptor Antagonist, Growth Hormone Receptor Antagonists, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Hypoglycemia-Associated Agents, Pegylated agents, Peptide Hormones, Peptides, Pituitary and Hypothalamic Hormones and Analogues, Pituitary Hormones, Pituitary Hormones, Anterior, Somatotropin Antagonists, Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins |
| Patents Number | US5849535 |
| Date of Issue | 15-Dec-1998 |
| Date of Expiry | 25-Mar-2017 |
| Drug Interaction | Dihydrocodeine opioids may diminish the therapeutic effect of pegvisomant. It is recommended to monitor therapy |
| Target | Growth hormone receptor |
| Brand Name | SOMAVERT |
| Company | Pfizer |
| Brand Description | Pfizer |
| 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 | NA |
| 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 |
| Physical Appearance | 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 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |