Identification
- Summary
Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used for the management of type 2 diabetes mellitus.
- Brand Names
- Janumet, Januvia, Ristaben, Steglujan, Tesavel, Velmetia, Xelevia, Zituvio
- Generic Name
- Sitagliptin
- DrugBank Accession Number
- DB01261
- Background
Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used in conjunction with diet and exercise to improve glycemic control in patients with type 2 diabetes mellitusLabel,4,1,2. The effect of this medication leads to glucose dependent increases in insulin and decreases in glucagon to improve control of blood sugarLabel,1. Sitagliptin was granted FDA approval on October 16, 20066.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Sitagliptin (DB01261)
- Weight
- Average: 407.3136
Monoisotopic: 407.118079357 - Chemical Formula
- C16H15F6N5O
- Synonyms
- Sitagliptin
- Sitagliptina
- Sitagliptine
- Sitagliptinum
- External IDs
- LEZ-763
- LEZ763
Pharmacology
- Indication
Sitagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It is not used to treat type 1 diabetes or patients with a history of pancreatitis.9
It is also used in combination with metformin 8 or ertugliflozin.10
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used as adjunct in combination to manage Type 2 diabetes mellitus Combination Product in combination with: Ertugliflozin (DB11827) •••••••••••• ••••• Used as adjunct in combination to manage Type 2 diabetes mellitus Combination Product in combination with: Metformin (DB00331) •••••••••••• ••••• Adjunct therapy in management of Type 2 diabetes mellitus •••••••••••• ••••• - Contraindications & Blackbox Warnings
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Sitagliptin inhibits DPP-4 which leads to increased levels of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide(GIP), decreased levels of glucagon, and a stronger insulin response to glucoseLabel,4,1,2.
- Mechanism of action
Inhibition of DPP-4 by sitagliptin slows DPP-4 mediated inactivation of incretins like GLP-1 and GIPLabel,2. Incretins are released throughout the day and upregulated in response to meals as part of glucose homeostasisLabel,4. Reduced inhibition of incretins increase insulin synthesis and decrease glucagon release in a manner dependant on glucose concentrationsLabel,1. These effects lead to an overall increase in blood glucose control which is demonstrated by reduced glycosylated hemoglobin (HbA1c)Label,4.
Target Actions Organism ADipeptidyl peptidase 4 inhibitorHumans - Absorption
Sitagliptin is 87% orally bioavailable and taking it with or without food does not affect its pharmacokineticsLabel,4. Sitagliptin reaches maximum plasma concentration in 2 hours4.
- Volume of distribution
- Protein binding
- Metabolism
Sitagliptin is mostly not metabolised, with 79% of the dose excreted in the urine as the unchanged parent compoundLabel. Minor metabolic pathways are mediated mainly by cytochrome p450(CYP)3A4 and to a lesser extent by CYP2C8Label. After 18 hours, 81% of the dose has remained unchanged, while 2% has been N-sulfated to the M1 metabolite, 6% has been oxidatively desaturated and cyclized to the M2 metabolite, <1% glucuronidated at an unknown site to the M3 metabolite, <1% has been carbamoylated and glucuronidated to the M4 metabolite, 6% has been oxidatively saturated and cyclized to the M5 metabolite, and 2% has been hydroxylated at an unknown site to the M6 metabolite5. The M2 metabolite is the cis isomer while the M5 metabolite is the trans isomer of the same metabolite5.
Hover over products below to view reaction partners
- Route of elimination
Approximately 79% of sitagliptin is excreted in the urine as the unchanged parent compoundLabel. 87% of the dose is eliminated in the urine and 13% in the fecesLabel,4.
- Half-life
Approximately 12.4 hoursLabel. Other studies have reported a half life of approximately 11 hours4.
- Clearance
- Adverse Effects
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Animal studies in pregnancy have shown no adverse effects on the mother or offspring at normal doses, however these results are not always applicable to humans. There is a voluntary fetal exposure registry Label,7. Animal studies at 100 times the maximum recommended human dose resulted in an increase in rib malformations. Sitagliptin is excreted in the milk of rats but it is not known if it would also be expressed in human breast milk. Because many drugs are expressed in human breast milk, the risk and benefit of prescribing the medication must be considered. There is currently a lack of safety and effectiveness data in pediatric patients. No differences in safety and efficacy were observed in geriatric patients compared to younger patients, however caution should be used in this population as they are more likely to have reduced renal functionLabel. Sitagliptin has also been associated with a 34% relative risk increase for all cause infection4. There was no significant difference in patient response across sex, age, race, ethnicity, and BMI3.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Sitagliptin which could result in a higher serum level. Abametapir The serum concentration of Sitagliptin can be increased when it is combined with Abametapir. Abatacept The metabolism of Sitagliptin can be increased when combined with Abatacept. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Sitagliptin. Abiraterone The metabolism of Sitagliptin can be decreased when combined with Abiraterone. - Food Interactions
- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Sitagliptin phosphate TS63EW8X6F 654671-77-9 GQPYTJVDPQTBQC-KLQYNRQASA-N - Product Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Januvia Tablet, film coated 100 mg/1 Oral Med-Health Pharma, LLC 2011-05-11 2012-07-01 US 
Januvia Tablet, film coated 25 mg/1 Oral A-S Medication Solutions 2006-10-16 Not applicable US Januvia Tablet, film coated 100 mg Oral Merck Sharp And Dohme B.V 2016-09-08 Not applicable EU 
Januvia Tablet, film coated 25 mg Oral Merck Sharp And Dohme B.V 2016-09-08 Not applicable EU Januvia Tablet, film coated 100 mg/1 Oral Physicians Total Care, Inc. 2007-12-13 Not applicable US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ach-sitagliptin Tablet 25 mg Oral Accord Healthcare Inc 2023-05-12 Not applicable Canada 
Ach-sitagliptin Tablet 100 mg Oral Accord Healthcare Inc 2023-05-12 Not applicable Canada Ach-sitagliptin Tablet 50 mg Oral Accord Healthcare Inc 2023-05-12 Not applicable Canada Apo-sitagliptin Tablet 100 mg Oral Apotex Corporation Not applicable Not applicable Canada Apo-sitagliptin Tablet 50 mg Oral Apotex Corporation Not applicable Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Apo-sitagliptin-metformin Sitagliptin phosphate (50 mg) + Metformin hydrochloride (1000 mg) Tablet Oral Apotex Corporation Not applicable Not applicable Canada Apo-sitagliptin-metformin Sitagliptin phosphate (50 mg) + Metformin hydrochloride (850 mg) Tablet Oral Apotex Corporation Not applicable Not applicable Canada Apo-sitagliptin-metformin Sitagliptin phosphate (50 mg) + Metformin hydrochloride (500 mg) Tablet Oral Apotex Corporation Not applicable Not applicable Canada Apo-sitagliptin/metformin XR Sitagliptin phosphate (100 mg) + Metformin hydrochloride (1000 mg) Tablet, extended release Oral Apotex Corporation 2022-11-07 Not applicable Canada Apo-sitagliptin/metformin XR Sitagliptin phosphate (50 mg) + Metformin hydrochloride (1000 mg) Tablet, extended release Oral Apotex Corporation 2022-11-07 Not applicable Canada
Categories
- ATC Codes
- A10BH51 — Sitagliptin and simvastatin
- A10BH — Dipeptidyl peptidase 4 (DPP-4) inhibitors
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- A10BD — Combinations of oral blood glucose lowering drugs
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- A10BD — Combinations of oral blood glucose lowering drugs
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- A10BH — Dipeptidyl peptidase 4 (DPP-4) inhibitors
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Agents causing angioedema
- Alimentary Tract and Metabolism
- Blood Glucose Lowering Agents
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- DPP-IV Inhibitors
- Drugs that are Mainly Renally Excreted
- Drugs Used in Diabetes
- Enzyme Inhibitors
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypoglycemia-Associated Agents
- Incretins
- OAT3/SLC22A8 Substrates
- Oral Hypoglycemics
- P-glycoprotein substrates
- Protease Inhibitors
- Triazoles
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as beta amino acids and derivatives. These are amino acids having a (-NH2) group attached to the beta carbon atom.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- Beta amino acids and derivatives
- Alternative Parents
- Amphetamines and derivatives / Triazolopyrazines / Aralkylamines / Fluorobenzenes / Pyrazines / Aryl fluorides / Triazoles / Tertiary carboxylic acid amides / Heteroaromatic compounds / Azacyclic compounds show 7 more
- Substituents
- 1,2,4-triazole / Alkyl fluoride / Alkyl halide / Amine / Amphetamine or derivatives / Aralkylamine / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle show 25 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- trifluorobenzene, triazolopyrazine (CHEBI:40237)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- QFP0P1DV7Z
- CAS number
- 486460-32-6
- InChI Key
- MFFMDFFZMYYVKS-SECBINFHSA-N
- InChI
- InChI=1S/C16H15F6N5O/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22/h4,6,9H,1-3,5,7,23H2/t9-/m1/s1
- IUPAC Name
- (3R)-3-amino-1-[3-(trifluoromethyl)-5H,6H,7H,8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
- SMILES
- N[C@@H](CC(=O)N1CCN2C(C1)=NN=C2C(F)(F)F)CC1=CC(F)=C(F)C=C1F
References
- Synthesis Reference
Nurit Perlman, Marina Etinger, Valerie Niddam-Hildesheim, Mili Abramov, "Preparation of sitagliptin intermediate." U.S. Patent US20090192326, issued July 30, 2009.
US20090192326- General References
- Herman GA, Stevens C, Van Dyck K, Bergman A, Yi B, De Smet M, Snyder K, Hilliard D, Tanen M, Tanaka W, Wang AQ, Zeng W, Musson D, Winchell G, Davies MJ, Ramael S, Gottesdiener KM, Wagner JA: Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther. 2005 Dec;78(6):675-88. [Article]
- Herman GA, Bergman A, Liu F, Stevens C, Wang AQ, Zeng W, Chen L, Snyder K, Hilliard D, Tanen M, Tanaka W, Meehan AG, Lasseter K, Dilzer S, Blum R, Wagner JA: Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol. 2006 Aug;46(8):876-86. [Article]
- Karasik A, Aschner P, Katzeff H, Davies MJ, Stein PP: Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin. 2008 Feb;24(2):489-96. doi: 10.1185/030079908X261069 . [Article]
- Richter B, Bandeira-Echtler E, Bergerhoff K, Lerch C: Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes. Vasc Health Risk Manag. 2008;4(4):753-68. [Article]
- Vincent SH, Reed JR, Bergman AJ, Elmore CS, Zhu B, Xu S, Ebel D, Larson P, Zeng W, Chen L, Dilzer S, Lasseter K, Gottesdiener K, Wagner JA, Herman GA: Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C]sitagliptin in humans. Drug Metab Dispos. 2007 Apr;35(4):533-8. doi: 10.1124/dmd.106.013136. Epub 2007 Jan 12. [Article]
- FDA Drug Approval Package: Sitagliptin [Link]
- Merck Pregnancy Registry: Sitagliptin [Link]
- FDA Approved Drug Products: JANUMET (sitagliptin and metformin hydrochloride) tablets, for oral use [Link]
- FDA Approved Drug Products: JANUVIA (sitagliptin) tablets, for oral use [Link]
- FDA Approved Drug Products: STEGLUJAN (ertugliflozin and sitagliptin) tablets, for oral use [Link]
- FDA Approved Drug Products: JANUVIA (sitagliptin) tablets, for oral use, 2022 [Link]
- External Links
- Human Metabolome Database
- HMDB0015390
- KEGG Drug
- D08516
- PubChem Compound
- 4369359
- PubChem Substance
- 46505822
- ChemSpider
- 3571948
- BindingDB
- 11162
- 593411
- ChEBI
- 40237
- ChEMBL
- CHEMBL1422
- ZINC
- ZINC000001489478
- Therapeutic Targets Database
- DAP000639
- PharmGKB
- PA164748978
- PDBe Ligand
- 715
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Sitagliptin
- PDB Entries
- 1x70 / 4ffw / 7y4g
- FDA label
- Download (405 KB)
- MSDS
- Download (22.3 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Basic Science Hypertension 1 4 Completed Not Available Healthy Subjects (HS) 1 4 Completed Basic Science Atherosclerosis / Diabetes 1 4 Completed Basic Science Healthy Subjects (HS) 1 4 Completed Basic Science Healthy Subjects (HS) / Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- AQ Pharmaceuticals Inc.
- A-S Medication Solutions LLC
- Lake Erie Medical and Surgical Supply
- Merck & Co.
- Murfreesboro Pharmaceutical Nursing Supply
- Physicians Total Care Inc.
- Resource Optimization and Innovation LLC
- Dosage Forms
Form Route Strength Tablet Oral 28.345 mg Tablet Oral 54.475 mg Tablet Oral Tablet, coated Oral Tablet Oral Tablet, film coated Oral Tablet, film coated, extended release Oral Tablet, extended release Oral Tablet, film coated, extended release Oral 1000 mg Tablet, film coated, extended release Oral 500 mg Tablet, film coated Oral 1000.0 mg Tablet, film coated Oral 500.0 mg Tablet, film coated Oral 850.0 mg Tablet Oral 100 mg Tablet Oral 25 mg Tablet Oral 50 mg Tablet, film coated Oral 100 mg/1 Tablet, film coated Oral 128.5 MG Tablet, film coated Oral 25 mg/1 Tablet, film coated Oral 50 mg/1 Tablet, film coated Oral 64.25 MG Tablet Oral 56.690 mg Tablet, coated Oral 25 mg Tablet Oral 850.000 mg Tablet Oral 100 mg/1 Tablet Oral 25 mg/1 Tablet Oral 50 mg/1 Tablet, film coated Oral Tablet, film coated Tablet, film coated Oral 25 MG Tablet, film coated Oral 50 MG Tablet, film coated Oral 100 mg Tablet, coated Oral Tablet Oral 25.000 mg Tablet, coated Oral 100 mg Tablet, coated Oral 50 mg - Prices
Unit description Cost Unit Januvia 90 25 mg tablet Bottle 686.36USD bottle Januvia 30 100 mg tablet Bottle 228.81USD bottle Januvia 50 mg tablet 7.48USD tablet Januvia 100 mg tablet 7.33USD tablet Januvia 25 mg tablet 7.33USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2536251 No 2009-08-04 2024-08-27 Canada CA2450740 No 2006-02-14 2022-07-05 Canada US7326708 Yes 2008-02-05 2027-05-24 US US6699871 Yes 2004-03-02 2023-01-26 US US7125873 Yes 2006-10-24 2023-01-26 US US8414921 Yes 2013-04-09 2029-01-21 US US6340475 No 2002-01-22 2016-09-19 US US6635280 No 2003-10-21 2016-09-19 US US6303661 No 2001-10-16 2017-04-24 US US6890898 No 2005-05-10 2019-02-02 US US7078381 No 2006-07-18 2019-02-02 US US7459428 No 2008-12-02 2019-02-02 US US8168637 No 2012-05-01 2022-06-26 US US8080580 No 2011-12-20 2030-07-13 US US9439901 No 2016-09-13 2030-10-21 US US9308204 No 2016-04-12 2030-10-21 US US10925871 No 2015-02-25 2035-02-25 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 1.5 Not Available - Predicted Properties
Property Value Source Water Solubility 0.034 mg/mL ALOGPS logP 1.95 ALOGPS logP 1.26 Chemaxon logS -4.1 ALOGPS pKa (Strongest Basic) 8.78 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 77.04 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 87.49 m3·mol-1 Chemaxon Polarizability 32.66 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9438 Caco-2 permeable - 0.6415 P-glycoprotein substrate Substrate 0.6509 P-glycoprotein inhibitor I Inhibitor 0.7141 P-glycoprotein inhibitor II Inhibitor 0.5248 Renal organic cation transporter Inhibitor 0.592 CYP450 2C9 substrate Non-substrate 0.9277 CYP450 2D6 substrate Non-substrate 0.7228 CYP450 3A4 substrate Substrate 0.6412 CYP450 1A2 substrate Non-inhibitor 0.7178 CYP450 2C9 inhibitor Inhibitor 0.6111 CYP450 2D6 inhibitor Non-inhibitor 0.538 CYP450 2C19 inhibitor Inhibitor 0.7048 CYP450 3A4 inhibitor Inhibitor 0.5358 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.8336 Ames test Non AMES toxic 0.5487 Carcinogenicity Non-carcinogens 0.7973 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.8093 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7076 hERG inhibition (predictor II) Inhibitor 0.6936
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 187.387655 predictedDarkChem Lite v0.1.0 [M-H]- 178.88033 predictedDeepCCS 1.0 (2019) [M+H]+ 188.490855 predictedDarkChem Lite v0.1.0 [M+H]+ 181.2759 predictedDeepCCS 1.0 (2019) [M+Na]+ 187.386255 predictedDarkChem Lite v0.1.0 [M+Na]+ 187.91936 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Virus receptor activity
- Specific Function
- Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by bindi...
- Gene Name
- DPP4
- Uniprot ID
- P27487
- Uniprot Name
- Dipeptidyl peptidase 4
- Molecular Weight
- 88277.935 Da
References
- Herman GA, Stevens C, Van Dyck K, Bergman A, Yi B, De Smet M, Snyder K, Hilliard D, Tanen M, Tanaka W, Wang AQ, Zeng W, Musson D, Winchell G, Davies MJ, Ramael S, Gottesdiener KM, Wagner JA: Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther. 2005 Dec;78(6):675-88. [Article]
- Bergman AJ, Stevens C, Zhou Y, Yi B, Laethem M, De Smet M, Snyder K, Hilliard D, Tanaka W, Zeng W, Tanen M, Wang AQ, Chen L, Winchell G, Davies MJ, Ramael S, Wagner JA, Herman GA: Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers. Clin Ther. 2006 Jan;28(1):55-72. [Article]
- Gallwitz B: Therapies for the treatment of type 2 diabetes mellitus based on incretin action. Minerva Endocrinol. 2006 Jun;31(2):133-47. [Article]
- Herman GA, Bergman A, Liu F, Stevens C, Wang AQ, Zeng W, Chen L, Snyder K, Hilliard D, Tanen M, Tanaka W, Meehan AG, Lasseter K, Dilzer S, Blum R, Wagner JA: Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol. 2006 Aug;46(8):876-86. [Article]
- Miller S, St Onge EL: Sitagliptin: a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Ann Pharmacother. 2006 Jul-Aug;40(7-8):1336-43. [Article]
- Karasik A, Aschner P, Katzeff H, Davies MJ, Stein PP: Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin. 2008 Feb;24(2):489-96. doi: 10.1185/030079908X261069 . [Article]
- Pratley RE, Salsali A: Inhibition of DPP-4: a new therapeutic approach for the treatment of type 2 diabetes. Curr Med Res Opin. 2007 Apr;23(4):919-31. [Article]
- Lyseng-Williamson KA: Sitagliptin. Drugs. 2007;67(4):587-97. [Article]
- Hermansen K, Kipnes M, Luo E, Fanurik D, Khatami H, Stein P: Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin. Diabetes Obes Metab. 2007 Sep;9(5):733-45. Epub 2007 Jun 26. [Article]
- Gallwitz B: Sitagliptin: Profile of a novel DPP-4 inhibitor for the treatment of type 2 diabetes. Drugs Today (Barc). 2007 Jan;43(1):13-25. [Article]
- Richter B, Bandeira-Echtler E, Bergerhoff K, Lerch C: Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes. Vasc Health Risk Manag. 2008;4(4):753-68. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Nadkarni P, Chepurny OG, Holz GG: Regulation of glucose homeostasis by GLP-1. Prog Mol Biol Transl Sci. 2014;121:23-65. doi: 10.1016/B978-0-12-800101-1.00002-8. [Article]
- Gallwitz B: Novel Therapeutic Approaches in Diabetes. Endocr Dev. 2016;31:43-56. doi: 10.1159/000439372. Epub 2016 Jan 19. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Scheen AJ: Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab. 2010 Aug;12(8):648-58. doi: 10.1111/j.1463-1326.2010.01212.x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Scheen AJ: Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab. 2010 Aug;12(8):648-58. doi: 10.1111/j.1463-1326.2010.01212.x. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Scheen AJ: Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab. 2010 Aug;12(8):648-58. doi: 10.1111/j.1463-1326.2010.01212.x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- Curator comments
- Substrate profile was demonstrated in vitro using human OAT3 expressed on CHO-K1 cells.
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
References
- VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]
Drug created at May 16, 2007 17:36 / Updated at February 20, 2024 23:55