| Primary information |
|---|
| ThPP ID | Th1033 |
| Therapeutic Peptide/Protein Name | Oprelvekin |
| Sequence | GPPPGPPRVSPDPRAELDSTVLLTRSLLADTRQLAAQLRDKFPADGDHNL view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 19047.2 |
| Chemical Formula | C854H1411N253O235S2 |
| Isoelectric Point | 11.16 |
| Hydrophobicity | -0.07 |
| Melting Point (℃) | N.A. |
| Half Life | 6.9 ± 1.7 hours |
| Description | Oprelvekin, the active ingredient in Neumega is recombinant Interleukin eleven, which is produced in Escherichia coli by recombinant DNA technology. The protein has a molecular mass of approximately 19,000 daltons, and is non-glycosylated. The polypeptide is 177 amino acids in length (the natural IL-11 has 178). This alteration has not resulted in measurable differences in bioactivity either in vitro or in vivo. The primary hematopoietic activity of Neumega is stimulation of megakaryocytopoiesis and thrombopoiesis. In mice and nonhuman primate studies Neumega has shown potent thrombopoietic activity in compromised hematopoiesis, including moderately to severely myelosuppressed animals. In these studies, Neumega improved platelet nadirs and accelerated platelet recoveries compared to controls. In animal studies Oprelvekin also has non-hematopoetic activities. This includes the regulation of intestinal epithelium growth (enhanced healing of gastrointestinal lesions), the inhibition of adipogenesis, the induction of acute phase protein synthesis (e.g., fibrinogen), and inhibition of macrophageal released pro-inflammatory cytokines. |
| Indication/Disease | Increases reduced platelet levels due to chemotherapy. |
| Pharmacodynamics | Oprelvekin is indicated for the prevention of severe thrombocytopenia and the reduction of the need for platelet transfusions following myelosuppressive chemotherapy in adult patients with nonmyeloid malignancies who are at high risk of severe thrombocytopenia. The primary hematopoietic activity of Oprelvekin is stimulation of megakaryocytopoiesis and thrombopoiesis. Oprelvekin has shown potent thrombopoietic activity in individuals with compromised hematopoiesis |
| Mechanism of Action | Oprelvekin binds to the interleukin 11 receptor which leads to a cascade of signal transduction events. IL-11 is a thrombopoietic growth factor that directly stimulates the proliferation of hematopoietic stem cells and megakaryocyte progenitor cells and induces megakaryocyte maturation resulting in increased platelet production. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | Absolute bioavailability is over 80%. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Antineoplastic Agents |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | Dihydrocodeine may increase the serum levels of opioid analgesics. It is recommended to monitor therapy for the signs and symptoms of respiratory depression and enhanced sedation. |
| Target | Interleukin-11 receptor subunit alpha |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Neumega |
| Company | Genetics Institute Inc |
| Brand Discription | Interleukin eleven (IL-11) is a thrombopoietic growth factor that directly stimulates the proliferation of hematopoietic stem cells and megakaryocyte progenitor cells and induces megakaryocyte maturation resulting in increased platelet production. IL-11 i |
| Prescribed for | Prevention of severe reductions in the number of blood clotting cells (platelets) caused by some chemotherapy |
| Chemical Name | N.A. |
| Formulation | Neumega is formulated in single-use vials containing 5 mg of oprelvekin (specific activity approximately 8 x 106 Units/mg) as a sterile, lyophilized powder with 23 mg Glycine, USP, 1.6 mg Dibasic Sodium Phosphate Heptahydrate, USP, and 0.55 mg Monobasic S |
| Physcial Appearnce | Sterile, lyophilized powder |
| Route of Administration | It must be Subcutaneous Injection not in the muSub |
| Recommended Dosage | The recommended dose of Neumega in adults with severe renal impairment(creatinine clearance<30 mL/min) is 25 µg/kg. An estimate of the patient's creatinine clearance(CLcr) in mL/min is required. CLcr in mL/min may be estimated from a spot serum creatinine determination. |
| Contraindication | In patients with a history of hypersensitivity to Neumega or any component of the product. |
| Side Effects | Chills; constipation; cough; diarrhea; dizziness; fever; flushing; hair loss; headache; increased cough; indigestion; inflammation or sores of the mouth or lips; joint pain; loss of appetite; mild swelling of the arms and legs; muscle pain; nausea; nervousness. |
| Useful Link | http://www.pfizer.com/files/products/uspi_neumega.pdf |
| PubMed ID | 28293407, 25270293, 28293407, 25713465, 25270293, 18698585, 18031104, 18020592, 15734010 |
| 3-D Structure | Th1033 (View) or (Download) |