Detailed description page of ThPDB2

This page displays user query in tabular form.

Th1213 details
Primary information
ID10850
Therapeutic IDTh1213
Protein NameInsulin Degludec
Sequence>Th1213_Insulin_Degludec GIVEQCCTSICSLYQLENYCN
Molecular Weight6103.97
Chemical FormulaC274H411N65O81S6
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
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.
ToxicityObserve for signs and symptoms of hypoglycemia, hypokalemia, and fluid retention and heart failure with concomitant use of Thiazolidinediones. Pregnancy Category C
MetabolismAll insulin degludec metabolites are inactive.
AbsorptionIn patients with type 1 diabetes, after 8 days of once daily subcutaneous dosing with 0.4 U/kg, maximum degludec concentrations of 4472 pmol/L were attained at a median of 9 hours (tmax). After the first dose of, median onset of appearance was around one hour. The glucose lowering effect lasted at least 42 hours after the last of 8 once-daily injections. Insulin degludec concentration reach steady state levels after 3-4 days.
NA
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 units/kg.
CategoriesNA
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetInsulin receptor,Insulin-like growth factor 1 receptor
Brand NameTresiba
CompanyNovo Nordisk
Brand DescriptionNovo Nordisk
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).
Physical Appearance sterile, 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 Link 1Link
Useful Link 2NA
RemarksNA