==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1822 details
Primary information
ThPP IDTh1213
Therapeutic Peptide/Protein NameInsulin Degludec
SequenceA chain GIVEQCCTSICSLYQLENYCN; B chain FVNQHLCGSHL view full sequnce in fasta
Functional ClassificationIa
Molecular Weight6103.97
Chemical FormulaC274H411N65O81S6
Isoelectric PointNA
HydrophobicityNA
Melting Point (℃)NA
Half Lifeapproximately 25 hours
DescriptionInsulin 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/DiseaseIndicated to improve glycemic control in adults with diabetes mellitus.
PharmacodynamicsThe 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 ActionThe 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.
ToxicityNA
MetabolismThe 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.
AbsorptionAfter 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 DistributionNA
ClearanceThe 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.
CategoriesNA
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetNA
Information of corresponding available drug in the market
Brand NameTresiba
CompanyNovo Nordisk
Brand DiscriptionTRESIBA (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 forTRESIBA is indicated to improve glycemic control in adults with diabetes mellitus.
Chemical NameLysB29(Ns-hexadecandioyl-y-Glu) des(B30) human insulin
Formulation100 units/mL (U-100) or 200 units/mL (U-200).
Physcial Appearncesterile, aqueous, clear, and colorless solution
Route of AdministrationSubcutaneous
Recommended DosageInject 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.
ContraindicationDuring episodes of hypoglycemia; In patients with hypersensitivity to TRESIBA or one of its excipients.
Side EffectsHypoglycemia; Hypersensitivity and allergic reactions; Hypokalemia.
Useful Linkhttp://www.rxlist.com/tresiba-drug/side-effects-interactions.htm
PubMed ID25941658, 24673155, 24118819, 23448197, 28250698, 28295934, 28282219, 28275957, 28234565
3-D StructureTh1213 (View) or (Download)