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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB08882
rdf:type
n5:Drug
n5:description
Linagliptin is a DPP-4 inhibitor developed by Boehringer Ingelheim for the treatment of type II diabetes [Wikipedia]. Two pharmacological characteristics that sets linagliptin apart from other DPP-4 inhibitors is that it has a non-linear pharmacokinetic profile and is not primarily eliminated by the renal system. FDA approved on May 2, 2011.
n5:dosage
n11:271B5A6A-363D-11E5-9242-09173F13E4C5 n11:271B5A6B-363D-11E5-9242-09173F13E4C5 n11:271B5A6C-363D-11E5-9242-09173F13E4C5 n11:271B5A6D-363D-11E5-9242-09173F13E4C5 n11:271B5A6E-363D-11E5-9242-09173F13E4C5
n5:generalReferences
# Forst T, Pfutzner A: Linagliptin, a dipeptidyl peptidase-4 inhibitor with a unique pharmacological profile, and efficacy in a broad range of patients with type 2 diabetes. Expert Opin Pharmacother. 2012 Jan;13(1):101-10. doi: 10.1517/14656566.2012.642863. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22149370
n5:group
approved
n5:halfLife
Terminal half life = 131 hours. Because of this long half-life, inhibition of DPP-4 activity is sustained which indicates that once-daily dosing is appropriate. Effective half-life for accumulation of drug is 12 hours when multiple oral doses of 5 mg are given.
n5:indication
Linagliptin is used for the management of type 2 diabetes mellitus.
owl:sameAs
n14:DB08882
dcterms:title
Linagliptin
adms:identifier
n18:Linagliptin n19:D09566 n20:0597-0146-60 n21:68610 n22:DB08882
n5:mechanismOfAction
Linagliptin is a competitive and reversible dipeptidyl peptidase (DPP)-4 enzyme inhibitor that slows the breakdown of insulinotropic hormone glucagon-like peptide (GLP)-1 for better glycemic control in diabetes patients. GLP and glucose-dependent insulinotropic polypeptide (GIP) are incretin hormones that increase the production and release of insulin from pancreatic beta cells and decrease the release of glucagon from pancreatic alpha cells. This results in a overall decrease in glucose production in the liver and increase an of insulin in a glucose-dependent manner.
n5:patent
n12:2496249%20 n12:2435730%20
n5:routeOfElimination
Linagliptin is eliminated via the feces/enteroheptic system (80%) and urine (5%). This is unlike other DPP-4 inhibitors which are primarily eliminated by the renal system.
n5:synonym
BI-1356 (R)-8-(3-Aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methylquinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione Tradjenta BI 1356 Trajenta
n5:volumeOfDistribution
Vd = 1110 L
n6:hasAHFSCode
n15:68-20-05
n5:foodInteraction
Although a high fat meal reduces Cmax and increases AUC, this interaction with food is not clinically significant
n5:mixture
n16:271B5A69-363D-11E5-9242-09173F13E4C5
n5:proteinBinding
70-80% protein bound, the extent to which is concentration dependent. Because of the propensity of linagliptin to bind to plasma protein, it has a long terminal half-life and a non-linear pharmacokinetic profile. In contrast, other DPP-4 inhibitors have linear pharmacokinetic profiles which makes linagliptin unique.
n5:synthesisReference
Pietro ALLEGRINI, Emanuele ATTOLINO, Marco ARTICO, "PROCESS FOR THE PREPARATION OF LINAGLIPTIN." U.S. Patent US20120165525, issued June 28, 2012.
foaf:page
n4:tradjenta-drug.htm n10:linagliptin.html
n5:IUPAC-Name
n9:271B5A73-363D-11E5-9242-09173F13E4C5
n5:InChI
n9:271B5A79-363D-11E5-9242-09173F13E4C5
n5:Molecular-Formula
n9:271B5A78-363D-11E5-9242-09173F13E4C5
n5:Molecular-Weight
n9:271B5A75-363D-11E5-9242-09173F13E4C5
n5:Monoisotopic-Weight
n9:271B5A76-363D-11E5-9242-09173F13E4C5
n5:SMILES
n9:271B5A77-363D-11E5-9242-09173F13E4C5
n5:Water-Solubility
n9:271B5A88-363D-11E5-9242-09173F13E4C5 n9:271B5A71-363D-11E5-9242-09173F13E4C5
n5:logP
n9:271B5A6F-363D-11E5-9242-09173F13E4C5 n9:271B5A72-363D-11E5-9242-09173F13E4C5
n5:logS
n9:271B5A70-363D-11E5-9242-09173F13E4C5
n6:hasATCCode
n7:A10BH05
n5:H-Bond-Acceptor-Count
n9:271B5A7F-363D-11E5-9242-09173F13E4C5
n5:H-Bond-Donor-Count
n9:271B5A80-363D-11E5-9242-09173F13E4C5
n5:InChIKey
n9:271B5A7A-363D-11E5-9242-09173F13E4C5
n5:Polar-Surface-Area--PSA-
n9:271B5A7B-363D-11E5-9242-09173F13E4C5
n5:Polarizability
n9:271B5A7D-363D-11E5-9242-09173F13E4C5
n5:Refractivity
n9:271B5A7C-363D-11E5-9242-09173F13E4C5
n5:Rotatable-Bond-Count
n9:271B5A7E-363D-11E5-9242-09173F13E4C5
n5:absorption
Cmax, 5 mg, healthy subjects = 8.32 nmol/L; Tmax, 5 mg, healthy subjects = 1.75 hours; AUC(0-24 hours), 5 mg, healthy subjects = 119 nmol ยท h/L; Bioavailability, healthy subjects = 30%. When a dose of 5 mg once daily is given, steady state is achieved by the third dose. Although a high fat meal reduces Cmax and increases AUC, this interaction with food is not clinically significant. Linagliptin may be administered with or without food.
n5:affectedOrganism
Humans and other mammals
n5:casRegistryNumber
668270-12-0
n5:category
n5:clearance
Renal clearance, steady state = 70 mL/min
n5:Bioavailability
n9:271B5A84-363D-11E5-9242-09173F13E4C5
n5:Ghose-Filter
n9:271B5A86-363D-11E5-9242-09173F13E4C5
n5:MDDR-Like-Rule
n9:271B5A87-363D-11E5-9242-09173F13E4C5
n5:Number-of-Rings
n9:271B5A83-363D-11E5-9242-09173F13E4C5
n5:Physiological-Charge
n9:271B5A82-363D-11E5-9242-09173F13E4C5
n5:Rule-of-Five
n9:271B5A85-363D-11E5-9242-09173F13E4C5
n5:Traditional-IUPAC-Name
n9:271B5A74-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-basic-
n9:271B5A81-363D-11E5-9242-09173F13E4C5