Saxagliptin
Identification
- Name
- Saxagliptin
- Accession Number
- DB06335
- Description
Saxagliptin (rINN) is an orally active hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. FDA approved on July 31, 2009.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Saxagliptin (DB06335)
- Weight
- Average: 315.41
Monoisotopic: 315.194677059 - Chemical Formula
- C18H25N3O2
- Synonyms
- (1S,3S,5S)-2-((2S)-Amino(3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)acetyl)-2-azabicyclo(3.1.0)hexane-3-carbonitrile
- Saxagliptin
- Saxagliptin anhydrous
- Saxagliptina
- External IDs
- BMS 477118
- BMS-477118
Pharmacology
- Indication
Treatment of type 2 diabetes mellitus to improve glycemic control in combination with other agents or as monotherapy.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Post-administration of saxagliptin, GLP-1 and GIP levels rise up to 2- to 3- fold. Because it is very selective of DPP-4 inhibition, there are fewer systemic side effects. Saxagliptin inhibits DPP-4 enzyme activity for a 24-hour period. It also decreased glucagon concentrations and increased glucose-dependent insulin secretion from pancreatic beta cells. The half maximal inhibitory concentration (IC50) is 0.5 nmol/L. Saxagliptin did not prolong the QTc interval to a clinically significant degree.
- Mechanism of action
Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor antidiabetic for the treatment of type 2 diabetes. DPP-4 inhibitors are a class of compounds that work by affecting the action of natural hormones in the body called incretins. Incretins decrease blood sugar by increasing consumption of sugar by the body, mainly through increasing insulin production in the pancreas, and by reducing production of sugar by the liver. [Bristol-Myers Squibb Press Release] DPP-4 is a membrane associated peptidase which is found in many tissues, lymphocytes and plasma. DPP-4 has two main mechanisms of action, an enzymatic function and another mechanism where DPP-4 binds adenosine deaminase, which conveys intracellular signals via dimerization when activated. Saxagliptin forms a reversible, histidine-assisted covalent bond between its nitrile group and the S630 hydroxyl oxygen on DPP-4. The inhibition of DPP-4 increases levels active of glucagon like peptide 1 (GLP-1), which inhibits glucagon production from pancreatic alpha cells and increases production of insulin from pancreatic beta cells.
Target Actions Organism ADipeptidyl peptidase 4 inhibitorHumans - Absorption
Following a 5 mg single oral dose of saxagliptin to healthy subjects, the mean plasma AUC values for saxagliptin and its active metabolite were 78 ng•h/mL and 214 ng•h/mL, respectively. The corresponding plasma Cmax values were 24 ng/mL and 47 ng/mL, respectively. Saxagliptin did not accumulate following repeated doses. The median time to maximum concentration (Tmax) following the 5 mg once daily dose was 2 hours for saxagliptin and 4 hours for its active metabolite. Bioavailability, 2.5 - 50 mg dose = 67%
- Volume of distribution
151 L
- Protein binding
The in vitro protein binding of saxagliptin and its active metabolite in human serum is negligible (<10%).
- Metabolism
The metabolism of saxagliptin is primarily mediated by cytochrome P450 3A4/5 (CYP3A4/5). 50% of the absorbed dose will undergo hepatic metabolism. The major metabolite of saxagliptin, 5-hydroxy saxagliptin, is also a DPP4 inhibitor, which is one-half as potent as saxagliptin.
Hover over products below to view reaction partners
- Route of elimination
Saxagliptin is eliminated by both renal and hepatic pathways. Following a single 50 mg dose of 14C-saxagliptin, 24%, 36%, and 75% of the dose was excreted in the urine as saxagliptin, its active metabolite, and total radioactivity, respectively. A total of 22% of the administered radioactivity was recovered in feces representing the fraction of the saxagliptin dose excreted in bile and/or unabsorbed drug from the gastrointestinal tract.
- Half-life
Saxagliptin = 2.5 hours; 5-hydroxy saxagliptin = 3.1 hours;
- Clearance
Renal clearance, single 50 mg dose = 14 L/h
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
Adverse reactions reported in ≥5% of patients treated with saxagliptin and more commonly than in patients treated with placebo are: upper respiratory tract infection, urinary tract infection, and headache.
- Affected organisms
- Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 Unlock Additional DataAbacavir Abacavir may decrease the excretion rate of Saxagliptin which could result in a higher serum level. Abametapir The serum concentration of Saxagliptin can be increased when it is combined with Abametapir. Abatacept The metabolism of Saxagliptin can be increased when combined with Abatacept. Acalabrutinib The metabolism of Saxagliptin can be decreased when combined with Acalabrutinib. Acarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Saxagliptin. Acebutolol The therapeutic efficacy of Saxagliptin can be increased when used in combination with Acebutolol. Aceclofenac Aceclofenac may decrease the excretion rate of Saxagliptin which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Saxagliptin which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Saxagliptin which could result in a higher serum level. Acetazolamide The therapeutic efficacy of Saxagliptin can be increased when used in combination with Acetazolamide. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Take with food. Food increases total drug exposure.
Products
- Product Ingredients
Ingredient UNII CAS InChI Key Saxagliptin hydrochloride Z8J84YIX6L 709031-78-7 TUAZNHHHYVBVBR-NHKADLRUSA-N Saxagliptin monohydrate 9GB927LAJW 945667-22-1 AFNTWHMDBNQQPX-NHKADLRUSA-N - Product Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataOnglyza Tablet, film coated 5 mg/1 Oral E.R. Squibb & Sons, L.L.C. 2009-07-31 2017-04-30 US 
Onglyza Tablet, film coated 5 mg Oral Astra Zeneca Ab 2009-10-01 Not applicable EU 
Onglyza Tablet, film coated 5 mg Oral Astra Zeneca Ab 2009-10-01 Not applicable EU Onglyza Tablet, film coated 5 mg/1 Oral Cardinal Health 2014-11-20 Not applicable US 
Onglyza Tablet, film coated 5 mg Oral Astra Zeneca Ab 2009-10-01 Not applicable EU Onglyza Tablet, film coated 5 mg/1 Oral Cardinal Health 2009-07-31 2017-04-30 US 
Onglyza Tablet, film coated 2.5 mg Oral Astra Zeneca Ab 2009-10-01 Not applicable EU Onglyza Tablet, film coated 2.5 mg Oral Astra Zeneca Ab 2009-10-01 Not applicable EU Onglyza Tablet, film coated 5 mg Oral Astra Zeneca Ab 2009-10-01 Not applicable EU Onglyza Tablet 2.5 mg Oral Astra Zeneca 2011-12-23 Not applicable Canada 
Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Kombiglyze XR Saxagliptin hydrochloride (2.5 mg/1) + Metformin hydrochloride (1000 mg/1) Tablet, film coated, extended release Oral E.R. Squibb & Sons, L.L.C. 2010-11-05 2017-05-31 US 
Kombiglyze XR Saxagliptin hydrochloride (5 mg/1) + Metformin hydrochloride (500 mg/1) Tablet, film coated, extended release Oral AstraZeneca Pharmaceuticals LP 2014-12-04 Not applicable US Kombiglyze XR Saxagliptin hydrochloride (2.5 mg/1) + Metformin hydrochloride (1000 mg/1) Tablet, film coated, extended release Oral AstraZeneca Pharmaceuticals LP 2014-12-04 Not applicable US 
Kombiglyze XR Saxagliptin hydrochloride (5 mg/1) + Metformin hydrochloride (1000 mg/1) Tablet, film coated, extended release Oral E.R. Squibb & Sons, L.L.C. 2010-11-05 2017-03-31 US Kombiglyze XR Saxagliptin hydrochloride (5 mg/1) + Metformin hydrochloride (1000 mg/1) Tablet, film coated, extended release Oral AstraZeneca Pharmaceuticals LP 2014-12-04 Not applicable US Kombiglyze XR Saxagliptin hydrochloride (5 mg/1) + Metformin hydrochloride (500 mg/1) Tablet, film coated, extended release Oral E.R. Squibb & Sons, L.L.C. 2010-11-05 2017-04-30 US Komboglyze Saxagliptin (2.5 mg) + Metformin (1000 mg) Tablet, film coated Oral Astra Zeneca Ab 2016-09-08 Not applicable EU Komboglyze Saxagliptin (2.5 mg) + Metformin (850 mg) Tablet, film coated Oral Astra Zeneca Ab 2016-09-08 Not applicable EU Komboglyze Saxagliptin (2.5 mg) + Metformin (850 mg) Tablet, film coated Oral Astra Zeneca Ab 2016-09-08 Not applicable EU Komboglyze Saxagliptin (2.5 mg) + Metformin (1000 mg) Tablet, film coated Oral Astra Zeneca Ab 2016-09-08 Not applicable EU
Categories
- ATC Codes
- A10BD21 — Saxagliptin and dapagliflozin
- 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
- Amino Acids, Peptides, and Proteins
- Blood Glucose Lowering Agents
- Cycloparaffins
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 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
- Oligopeptides
- Peptides
- Protease Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- Alpha amino acid amides
- Alternative Parents
- N-acylpiperidines / N-acylpyrrolidines / Tertiary carboxylic acid amides / Tertiary alcohols / Cyclic alcohols and derivatives / Nitriles / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Monoalkylamines show 2 more
- Substituents
- Alcohol / Aliphatic heteropolycyclic compound / Alpha-amino acid amide / Amine / Azacycle / Carbonitrile / Carbonyl group / Carboxamide group / Cyclic alcohol / Hydrocarbon derivative show 16 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- tertiary alcohol, azabicycloalkane, monocarboxylic acid amide, adamantanes, nitrile (CHEBI:71272)
Chemical Identifiers
- UNII
- 8I7IO46IVQ
- CAS number
- 361442-04-8
- InChI Key
- QGJUIPDUBHWZPV-SGTAVMJGSA-N
- InChI
- InChI=1S/C18H25N3O2/c19-8-13-2-12-3-14(12)21(13)16(22)15(20)17-4-10-1-11(5-17)7-18(23,6-10)9-17/h10-15,23H,1-7,9,20H2/t10?,11?,12-,13+,14+,15-,17?,18?/m1/s1
- IUPAC Name
- (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxyadamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
- SMILES
- [H][C@@]12C[C@]1([H])N([C@@H](C2)C#N)C(=O)[C@@H](N)C12CC3CC(CC(O)(C3)C1)C2
References
- Synthesis Reference
Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage, "CRYSTAL FORMS OF SAXAGLIPTIN AND PROCESSES FOR PREPARING SAME." U.S. Patent US20090054303, issued February 26, 2009.
US20090054303- General References
- Rosenstock J, Sankoh S, List JF: Glucose-lowering activity of the dipeptidyl peptidase-4 inhibitor saxagliptin in drug-naive patients with type 2 diabetes. Diabetes Obes Metab. 2008 May;10(5):376-86. doi: 10.1111/j.1463-1326.2008.00876.x. Epub 2008 Mar 18. [PubMed:18355324]
- Metzler WJ, Yanchunas J, Weigelt C, Kish K, Klei HE, Xie D, Zhang Y, Corbett M, Tamura JK, He B, Hamann LG, Kirby MS, Marcinkeviciene J: Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation. Protein Sci. 2008 Feb;17(2):240-50. doi: 10.1110/ps.073253208. [PubMed:18227430]
- Crepaldi G, Carruba M, Comaschi M, Del Prato S, Frajese G, Paolisso G: Dipeptidyl peptidase 4 (DPP-4) inhibitors and their role in Type 2 diabetes management. J Endocrinol Invest. 2007 Jul-Aug;30(7):610-4. [PubMed:17848846]
- Barnett A: DPP-4 inhibitors and their potential role in the management of type 2 diabetes. Int J Clin Pract. 2006 Nov;60(11):1454-70. [PubMed:17073841]
- Kulasa K, Edelman S: Saxagliptin: the evidence for its place in the treatment of type 2 diabetes mellitus. Core Evid. 2010 Oct 21;5:23-37. [PubMed:21042540]
- Russell S: Incretin-based therapies for type 2 diabetes mellitus: a review of direct comparisons of efficacy, safety and patient satisfaction. Int J Clin Pharm. 2013 Apr;35(2):159-72. doi: 10.1007/s11096-012-9729-9. Epub 2012 Dec 22. [PubMed:23263796]
- Ali S, Fonseca V: Saxagliptin overview: special focus on safety and adverse effects. Expert Opin Drug Saf. 2013 Jan;12(1):103-9. doi: 10.1517/14740338.2013.741584. Epub 2012 Nov 9. [PubMed:23137182]
- Golightly LK, Drayna CC, McDermott MT: Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. doi: 10.2165/11632930-000000000-00000. [PubMed:22686547]
- External Links
- Human Metabolome Database
- HMDB0015634
- KEGG Drug
- D08996
- PubChem Compound
- 11243969
- PubChem Substance
- 99443245
- ChemSpider
- 9419005
- BindingDB
- 50225074
- 1546030
- ChEBI
- 71272
- ChEMBL
- CHEMBL385517
- PharmGKB
- PA165958362
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Saxagliptin
- AHFS Codes
- 68:20.05 — Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
- FDA label
- Download (492 KB)
- MSDS
- Download (479 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Basic Science Type 2 Diabetes Mellitus 1 4 Completed Treatment BMI >30 kg/m2 / Pre-Diabetic 1 4 Completed Treatment Coronary Artery Disease (CAD) / Type 2 Diabetes Mellitus 1 4 Completed Treatment Diabetes Mellitus 1 4 Completed Treatment Diabetes Mellitus, Non-Insulin-Dependent / Heart Failure / Type 2 Diabetes Mellitus 1 4 Completed Treatment Diabetes Mellitus, Non-Insulin-Dependent / Type 2 Diabetes Mellitus 1 4 Completed Treatment Heart Failure / Type 2 Diabetes Mellitus 1 4 Completed Treatment Inadequate Glycaemic Control / Type 2 Diabetes Mellitus 1 4 Completed Treatment Type 2 Diabetes Mellitus 11 4 Enrolling by Invitation Basic Science Hypertriglyceridemias / Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, extended release Oral 1 g Tablet, extended release Oral 500 mg Tablet, film coated Oral 500 mg Tablet, film coated, extended release Oral Tablet, film coated, extended release Oral 1000 mg Tablet Oral 5 mg Tablet, film coated, extended release Oral 500 mg Tablet, extended release Oral 1000 mg Tablet Oral Tablet, film coated Oral Tablet, coated Oral 2.5 mg Tablet Oral 2.5 mg Tablet, film coated Oral 2.5 mg/1 Tablet, film coated Oral 2.5 mg Tablet, film coated Oral 5 mg/1 Tablet, film coated Oral 5 mg Tablet, coated Oral 5 mg Tablet Oral 1000 MG Tablet Oral 850 MG - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataUS6395767 No 2002-05-28 2021-02-16 US USRE44186 No 2013-04-30 2023-07-31 US US7951400 No 2011-05-31 2028-11-30 US US8628799 No 2014-01-14 2025-07-13 US US8501698 No 2013-08-06 2027-06-20 US US6414126 No 2002-07-02 2020-10-04 US US6515117 No 2003-02-04 2020-10-04 US US6936590 No 2005-08-30 2020-10-04 US US9198925 No 2015-12-01 2020-10-04 US US7919598 No 2011-04-05 2029-12-16 US US8361972 No 2013-01-29 2028-03-21 US US8716251 No 2014-05-06 2028-03-21 US US8221786 No 2012-07-17 2028-03-21 US US9339472 No 2016-05-17 2025-07-13 US US9616028 No 2017-04-11 2030-11-12 US Additional Data Available- Filed OnFiled OnAvailable for Purchase
The date on which a patent was filed with the relevant government.
Learn more
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Sparingly soluble FDA label - Predicted Properties
Property Value Source Water Solubility 2.26 mg/mL ALOGPS logP 0.88 ALOGPS logP -0.08 ChemAxon logS -2.1 ALOGPS pKa (Strongest Acidic) 14.74 ChemAxon pKa (Strongest Basic) 7.9 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 4 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 90.35 Å2 ChemAxon Rotatable Bond Count 2 ChemAxon Refractivity 83.99 m3·mol-1 ChemAxon Polarizability 34.22 Å3 ChemAxon Number of Rings 5 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 + 0.9894 Blood Brain Barrier + 0.8823 Caco-2 permeable - 0.5446 P-glycoprotein substrate Substrate 0.5909 P-glycoprotein inhibitor I Non-inhibitor 0.696 P-glycoprotein inhibitor II Non-inhibitor 0.7875 Renal organic cation transporter Non-inhibitor 0.7903 CYP450 2C9 substrate Non-substrate 0.8618 CYP450 2D6 substrate Non-substrate 0.7519 CYP450 3A4 substrate Substrate 0.5944 CYP450 1A2 substrate Non-inhibitor 0.8448 CYP450 2C9 inhibitor Non-inhibitor 0.8017 CYP450 2D6 inhibitor Non-inhibitor 0.8198 CYP450 2C19 inhibitor Non-inhibitor 0.81 CYP450 3A4 inhibitor Non-inhibitor 0.8641 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9032 Ames test Non AMES toxic 0.7569 Carcinogenicity Non-carcinogens 0.9122 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.7529 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9912 hERG inhibition (predictor II) Non-inhibitor 0.832
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
- 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
- Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG: Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem. 2005 Jul 28;48(15):5025-37. [PubMed:16033281]
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
- Upreti VV, Boulton DW, Li L, Ching A, Su H, Lacreta FP, Patel CG: Effect of rifampicin on the pharmacokinetics and pharmacodynamics of saxagliptin, a dipeptidyl peptidase-4 inhibitor, in healthy subjects. Br J Clin Pharmacol. 2011 Jul;72(1):92-102. doi: 10.1111/j.1365-2125.2011.03937.x. [PubMed:21651615]
- Patel CG, Kornhauser D, Vachharajani N, Komoroski B, Brenner E, Handschuh del Corral M, Li L, Boulton DW: Saxagliptin, a potent, selective inhibitor of DPP-4, does not alter the pharmacokinetics of three oral antidiabetic drugs (metformin, glyburide or pioglitazone) in healthy subjects. Diabetes Obes Metab. 2011 Jul;13(7):604-14. doi: 10.1111/j.1463-1326.2011.01381.x. [PubMed:21332626]
- Scheen AJ: Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions. Clin Pharmacokinet. 2010 Sep;49(9):573-88. doi: 10.2165/11532980-000000000-00000. [PubMed:20690781]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- 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
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Upreti VV, Boulton DW, Li L, Ching A, Su H, Lacreta FP, Patel CG: Effect of rifampicin on the pharmacokinetics and pharmacodynamics of saxagliptin, a dipeptidyl peptidase-4 inhibitor, in healthy subjects. Br J Clin Pharmacol. 2011 Jul;72(1):92-102. doi: 10.1111/j.1365-2125.2011.03937.x. [PubMed:21651615]
- Patel CG, Kornhauser D, Vachharajani N, Komoroski B, Brenner E, Handschuh del Corral M, Li L, Boulton DW: Saxagliptin, a potent, selective inhibitor of DPP-4, does not alter the pharmacokinetics of three oral antidiabetic drugs (metformin, glyburide or pioglitazone) in healthy subjects. Diabetes Obes Metab. 2011 Jul;13(7):604-14. doi: 10.1111/j.1463-1326.2011.01381.x. [PubMed:21332626]
- Scheen AJ: Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions. Clin Pharmacokinet. 2010 Sep;49(9):573-88. doi: 10.2165/11532980-000000000-00000. [PubMed:20690781]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
- Gene Name
- ABCC1
- Uniprot ID
- P33527
- Uniprot Name
- Multidrug resistance-associated protein 1
- Molecular Weight
- 171589.5 Da
References
- Scheen AJ: Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions. Clin Pharmacokinet. 2010 Sep;49(9):573-88. doi: 10.2165/11532980-000000000-00000. [PubMed:20690781]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Organic anion transporter, capable of transporting pharmacological substances such as digoxin, ouabain, thyroxine, methotrexate and cAMP. May participate in the regulation of membrane transport of ...
- Gene Name
- SLCO4C1
- Uniprot ID
- Q6ZQN7
- Uniprot Name
- Solute carrier organic anion transporter family member 4C1
- Molecular Weight
- 78947.525 Da
References
- Golightly LK, Drayna CC, McDermott MT: Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. doi: 10.2165/11632930-000000000-00000. [PubMed:22686547]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Golightly LK, Drayna CC, McDermott MT: Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. doi: 10.2165/11632930-000000000-00000. [PubMed:22686547]
Drug created on March 19, 2008 10:24 / Updated on January 19, 2021 22:53