| Mechanism of Action | hGH binds to the human growth hormone receptor (GHR). Upon binding, hGH causes dimerization of GHR, activation of the GHR-associated JAK2 tyrosine kinase, and tyrosyl phosphorylation of both JAK2 and GHR. These events recruit and/or activate a variety of signaling molecules, including MAP kinases, insulin receptor substrates, phosphatidylinositol 3' phosphate kinase, diacylglycerol, protein kinase C, intracellular calcium, and Stat transcription factors. These signaling molecules contribute to the GH-induced changes in enzymatic activity, transport function, and gene expression that ultimately culminate in changes in growth and metabolism. |
| Drug Interaction | The therapeutic efficacy of Somatropin recombinant can be decreased when used in combination with Bazedoxifene, Chlorotrianisene, Conjugated Equine Estrogens, Cortisone acetate, Dienestrol, Diethylstilbestrol, Estradiol, Estriol, Estrone, Ethinyl Estradiol. |
| Primary information |
|---|
| ID | 1850 |
| ThPP ID | Th1237 |
| Therapeutic Peptide/Protein Name | Somatropin recombinant |
| Sequence | FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQT view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 22129 |
| Chemical Formula | C990H1532N262O300S7 |
| Isoelectric Point | 5.27 |
| Hydrophobicity | -0.411 |
| Melting Point (℃) | 76 °C at |
| Half Life | NA |
| Description | Recombinant human growth hormone (somatotropin) 191 residues, MW 22.1 kD, synthesized in E. coli |
| Indication/Disease | For treatment of dwarfism, acromegaly and prevention of HIV-induced weight loss |
| Pharmacodynamics | Used in the treatment of dwarfism and growth failure, growth hormone (hGH) stimulates skeletal growth in pediatric patients with growth failure due to a lack of adequate secretion of endogenous GH. Skeletal growth is accomplished at the epiphyseal plates at the ends of a growing bone. Growth and metabolism of epiphyseal plate cells are directly stimulated by GH and one of its mediators, IGF-I (insulin-like growth factor). |
| Mechanism of Action | hGH binds to the human growth hormone receptor (GHR). Upon binding, hGH causes dimerization of GHR, activation of the GHR-associated JAK2 tyrosine kinase, and tyrosyl phosphorylation of both JAK2 and GHR. These events recruit and/or activate a variety of signaling molecules, including MAP kinases, insulin receptor substrates, phosphatidylinositol 3' phosphate kinase, diacylglycerol, protein kinase C, intracellular calcium, and Stat transcription factors. These signaling molecules contribute to the GH-induced changes in enzymatic activity, transport function, and gene expression that ultimately culminate in changes in growth and metabolism. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| Volume of Distribution | NA |
| Clearance | 2.3 +/- 1.8 mL/min/kg [GHD patients (IV 33 ng/kg/min)] |
| Categories | Hormones, Hormone Substitutes, and Hormone Antagonists |
| Patents Number | CA1326439,CA2252535 |
| Date of Issue | Mostly fro |
| Date of Expiry | Mostly 202 |
| Drug Interaction | The therapeutic efficacy of Somatropin recombinant can be decreased when used in combination with Bazedoxifene, Chlorotrianisene, Conjugated Equine Estrogens, Cortisone acetate, Dienestrol, Diethylstilbestrol, Estradiol, Estriol, Estrone, Ethinyl Estradiol. |
| Target | Growth hormone receptor, Prolactin receptor |
| Information of corresponding available drug in the market |
|---|
| Brand Name | NutropinAQ |
| Company | Genentech Inc. |
| Brand Discription | Nutropin AQ [somatropin (rDNA origin)] for Injection is a human growth hormone (hGH) produced by recombinant DNA technology. Nutropin AQ has 191 amino acid residues and a molecular weight of 22,125 daltons. The amino acid sequence of the product is identical to that of pituitary-derived hGH. Nutropin AQ may contain not more than fifteen percent deamidated GH at expiration. The deamidated form of GH has been extensively characterized and has been shown to be safe and fully active. |
| Prescribed for | Treating certain children or adults when the body does not produce enough growth hormone. It is also used to treat certain children who are not growing normally due to Turner syndrome or other conditions (eg, chronic kidney problems, idiopathic short stature). |
| Chemical Name | NA |
| Formulation | Each pen cartridge or NuSpin contain either 5 mg, 10 mg or 20 mg of somatropin formulated in 17.4 mg sodium chloride, 5 mg phenol, 4 mg polysorbate 20, and 10 mM sodium citrate |
| Physcial Appearance | Sterile liquid |
| Route of Administration | Subcutaneous |
| Recommended Dosage | A weekly dosage of up to 0.3 mg/kg of body weight divided into daily subcutaneous injections is recommended for Idiopathic Short Stature (ISS) |
| Contraindication | Acute Critical Illness, Prader-Willi Syndrome (PWS) In Children, Active Malignancy, Diabetic Retinopathy, Hypersensitivity, Closed Epiphysis |
| Side Effects | Abnormal or decreased touch sensation, bleeding, blistering, burning, coldness, discoloration of the skin, feeling of pressure, hives, infection, inflammation, itching, lumps, numbness, pain, rash, redness, scarring, soreness, stinging, swelling, tenderness, tingling, ulceration, or warmth at the injection site |
| Useful Link | https://www.drugs.com/cdi/nutropin-aq.html , https://www.medicines.org.uk/emc/medicine/14244 , http://www.rxlist.com/nutropin-aq-drug/side-effects-interactions.htm |
| PubMed ID | 2688, 2903866, 16702112, 5675429 |
| 3-D Structure | N.A. |