| Primary information |
|---|
| ThPP ID | Th1213 |
| Therapeutic Peptide/Protein Name | Insulin Degludec |
| Sequence | A chain GIVEQCCTSICSLYQLENYCN; B chain FVNQHLCGSHL view full sequnce in fasta |
| Functional Classification | Ia |
| Molecular Weight | 6103.97 |
| Chemical Formula | C274H411N65O81S6 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting Point (℃) | NA |
| Half Life | approximately 25 hours |
| Description | Insulin degludec differs from human insulin in that the amino acid threonine in position B30 has been omitted and a side-chain consisting of glutamic acid and a C16 fatty acid has been attached. |
| Indication/Disease | Indicated to improve glycemic control in adults with diabetes mellitus. |
| Pharmacodynamics | The glucose-lowering effect of TRESIBA after 8 days of once-daily dosing was measured in a euglycemic glucose clamp study enrolling 21 patients with type 1 diabetes. Figure 2 shows the pharmacodynamic effect of TRESIBA over time following 8 once-daily subcutaneous injections of 0.4 U/kg of TRESIBA in patients with type 1 diabetes. |
| Mechanism of Action | The primary activity of insulin, including TRESIBA, is regulation of glucose metabolism. Insulin and its analogs lower blood glucose by stimulating peripheral glucose uptake, especially by skeletal muscle and fat, and by inhibiting hepatic glucose production. Insulin also inhibits lipolysis and proteolysis, and enhances protein synthesis. TRESIBA forms multi-hexamers when injected into the subcutaneous tissue resulting in a subcutanous insulin degludec depot. The protracted time action profile of TRESIBA is predominantly due to delayed absorption of insulin degludec from the subcutaneous tissue to the systemic circulation and to a lesser extent due to binding of insulin-degludec to circulating albumin. |
| Toxicity | NA |
| Metabolism | The affinity of insulin degludec to serum albumin corresponds to a plasma protein binding of > 99% in human plasma. The results of the in vitro protein binding studies demonstrate that there is no clinically relevant interaction between insulin degludec and other protein bound drugs. |
| Absorption | After the first dose of TRESIBA, median onset of appearance was around one hour. Insulin degludec concentration reach steady state levels after 3-4 days of TRESIBA administration |
| Volume of Distribution | NA |
| Clearance | The mean apparent clearance of insulin degludec is 0.03 L/kg (2.1 L/h in 70 kg individual) after single subcutaneous dose of 0.4 U/kg. |
| Categories | NA |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | NA |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Tresiba |
| Company | Novo Nordisk |
| Brand Discription | TRESIBA (insulin degludec injection) is a long-acting basal human insulin analog for subcutaneous injection. Insulin degludec is produced by a process that includes expression of recombinant DNA in Saccharomyces cerevisiae followed by chemical modification. |
| Prescribed for | TRESIBA is indicated to improve glycemic control in adults with diabetes mellitus. |
| Chemical Name | LysB29(Ns-hexadecandioyl-y-Glu) des(B30) human insulin |
| Formulation | 100 units/mL (U-100) or 200 units/mL (U-200). |
| Physcial Appearnce | sterile, aqueous, clear, and colorless solution |
| Route of Administration | Subcutaneous |
| Recommended Dosage | Inject TRESIBA subcutaneously once-daily at any time of day. The recommended starting dose of TRESIBA in insulin naive patients with type 1 diabetes is approximately one-third to one-half of the total daily insulin dose. As a general rule, 0.2 to 0.4 units of insulin per kilogram of body weight can be used to calculate the initial total daily insulin dose in insulin naive patients with type 1 diabetes. The recommended starting dose of TRESIBA in insulin naive patients with type 2 diabetes mellitus is 10 units once daily. |
| Contraindication | During episodes of hypoglycemia; In patients with hypersensitivity to TRESIBA or one of its excipients. |
| Side Effects | Hypoglycemia; Hypersensitivity and allergic reactions; Hypokalemia. |
| Useful Link | http://www.rxlist.com/tresiba-drug/side-effects-interactions.htm |
| PubMed ID | 25941658, 24673155, 24118819, 23448197, 28250698, 28295934, 28282219, 28275957, 28234565 |
| 3-D Structure | Th1213 (View) or (Download) |