Saxagliptin

Identification

Summary

Saxagliptin is an DPP-4 inhibitor used for the management of type 2 diabetes mellitus.

Brand Names
Kombiglyze, Komboglyze, Onglyza, Qtern, Qternmet
Generic Name
Saxagliptin
DrugBank Accession Number
DB06335
Background

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
Thumb
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.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.

TargetActionsOrganism
ADipeptidyl peptidase 4
inhibitor
Humans
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
Medicalerrors
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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.

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.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Saxagliptin which could result in a higher serum level.
AbametapirThe serum concentration of Saxagliptin can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Saxagliptin can be increased when combined with Abatacept.
AcalabrutinibThe metabolism of Saxagliptin can be decreased when combined with Acalabrutinib.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Saxagliptin.
AcebutololThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Acebutolol.
AceclofenacAceclofenac may decrease the excretion rate of Saxagliptin which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Saxagliptin which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Saxagliptin which could result in a higher serum level.
AcetazolamideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Acetazolamide.
Interactions
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Food Interactions
  • Take with food. Food increases total drug exposure.

Products

Products
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Product Ingredients
IngredientUNIICASInChI Key
Saxagliptin hydrochlorideZ8J84YIX6L709031-78-7TUAZNHHHYVBVBR-NHKADLRUSA-N
Saxagliptin monohydrate9GB927LAJW945667-22-1AFNTWHMDBNQQPX-NHKADLRUSA-N
Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2016-09-08Not applicableEU flag
OnglyzaTablet, film coated2.5 mgOralAstra Zeneca Ab2016-09-08Not applicableEU flag
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2016-09-08Not applicableEU flag
OnglyzaTablet, film coated2.5 mgOralAstra Zeneca Ab2016-09-08Not applicableEU flag
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2016-09-08Not applicableEU flag
OnglyzaTablet, film coated5 mg/1OralAstraZeneca Pharmaceuticals LP2014-11-20Not applicableUS flag0310 610520180913 8702 13a6565
OnglyzaTablet, film coated5 mg/1OralE.R. Squibb & Sons, L.L.C.2009-07-312017-04-30US flag00003 4215 11 nlmimage10 c33ce1e7
OnglyzaTablet5 mgOralAstra Zeneca2009-10-29Not applicableCanada flag
OnglyzaTablet, film coated2.5 mgOralAstra Zeneca Ab2016-09-08Not applicableEU flag
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2016-09-08Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-saxagliptinTablet2.5 mgOralApotex Corporation2021-03-29Not applicableCanada flag
Apo-saxagliptinTablet5 mgOralApotex Corporation2021-03-29Not applicableCanada flag
Sandoz SaxagliptinTablet5 mgOralSandoz Canada Incorporated2021-03-08Not applicableCanada flag
Sandoz SaxagliptinTablet2.5 mgOralSandoz Canada Incorporated2021-03-08Not applicableCanada flag
Teva-saxagliptinTablet5 mgOralTEVA Canada LimitedNot applicableNot applicableCanada flag
Teva-saxagliptinTablet2.5 mgOralTEVA Canada LimitedNot applicableNot applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
KOMBIGLYZE ® XR 5 MG/ 1000 MGSaxagliptin (5 mg) + Metformin hydrochloride (1000 mg)Tablet, extended releaseOral2012-06-16Not applicableColombia flag
Kombiglyze XRSaxagliptin hydrochloride (5 mg/1) + Metformin hydrochloride (500 mg/1)Tablet, film coated, extended releaseOralAstraZeneca Pharmaceuticals LP2014-12-04Not applicableUS flag
Kombiglyze XRSaxagliptin hydrochloride (5 mg/1) + Metformin hydrochloride (1000 mg/1)Tablet, film coated, extended releaseOralE.R. Squibb & Sons, L.L.C.2010-11-052017-03-31US flag
Kombiglyze XRSaxagliptin hydrochloride (2.5 mg/1) + Metformin hydrochloride (1000 mg/1)Tablet, film coated, extended releaseOralAstraZeneca Pharmaceuticals LP2014-12-04Not applicableUS flag00310 6125 60 nlmimage10 d049e84f
Kombiglyze XRSaxagliptin hydrochloride (5 mg/1) + Metformin hydrochloride (1000 mg/1)Tablet, film coated, extended releaseOralAstraZeneca Pharmaceuticals LP2014-12-04Not applicableUS flag
Kombiglyze XRSaxagliptin hydrochloride (5 mg/1) + Metformin hydrochloride (500 mg/1)Tablet, film coated, extended releaseOralE.R. Squibb & Sons, L.L.C.2010-11-052017-04-30US flag
Kombiglyze XRSaxagliptin hydrochloride (2.5 mg/1) + Metformin hydrochloride (1000 mg/1)Tablet, film coated, extended releaseOralE.R. Squibb & Sons, L.L.C.2010-11-052017-05-31US flag00003 4222 16 nlmimage10 f215f93f
KOMBIGLYZE XR (TABLETS 5 MG/1000 MG)Saxagliptin (5 MG) + Metformin hydrochloride (1 g)Tablet, film coatedOralบริษัท แอสตร้าเซนเนก้า (ประเทศไทย) จำกัด2016-07-07Not applicableThailand flag
Kombiglyze XR Tablet 2.5/1000mgSaxagliptin hydrochloride (2.5 mg) + Metformin hydrochloride (1000 mg)Tablet, film coated, extended releaseOralASTRAZENECA SDN. BHD.2020-09-08Not applicableMalaysia flag
Kombiglyze XR Tablet 5/1000mgSaxagliptin (5 mg) + Metformin hydrochloride (1000 mg)TabletOralASTRAZENECA SDN. BHD.2020-09-08Not applicableMalaysia flag

Categories

ATC Codes
A10BD21 — Saxagliptin and dapagliflozinA10BD25 — Metformin, saxagliptin and dapagliflozinA10BH03 — SaxagliptinA10BD10 — Metformin and saxagliptin
Drug Categories
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)
Affected organisms
Not Available

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
  1. 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. [Article]
  2. 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. [Article]
  3. 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. [Article]
  4. 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. [Article]
  5. 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. [Article]
  6. 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. [Article]
  7. 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. [Article]
  8. 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. [Article]
Human Metabolome Database
HMDB0015634
KEGG Drug
D08996
PubChem Compound
11243969
PubChem Substance
99443245
ChemSpider
9419005
BindingDB
50225074
RxNav
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
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedTreatmentBMI >30 kg/m2 / Pre-Diabetic1
4CompletedTreatmentCoronary Artery Disease (CAD) / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent / Heart Failure / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent / Type 2 Diabetes Mellitus1
4CompletedTreatmentHeart Failure / Type 2 Diabetes Mellitus1
4CompletedTreatmentInadequate Glycaemic Control / Type 2 Diabetes Mellitus1
4CompletedTreatmentType 1 Diabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus11

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coated, extended releaseOral
Tablet, extended releaseOral
Tablet, coatedOral
TabletOral
TabletOral2.5 mg
TabletOral5 mg
Tablet, film coatedOral
Tablet, film coatedOral2.5 mg
Tablet, film coatedOral2.5 mg/1
Tablet, film coatedOral5 mg
Tablet, film coatedOral5 mg/1
Tablet, coatedOral
Tablet, film coatedOral
TabletOral
Tablet, coatedOral5 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6395767No2002-05-282021-02-16US flag
USRE44186No2013-04-302023-07-31US flag
US7951400No2011-05-312028-11-30US flag
US8628799No2014-01-142025-07-13US flag
US8501698Yes2013-08-062027-12-20US flag
US6414126No2002-07-022020-10-04US flag
US6515117Yes2003-02-042026-04-04US flag
US6936590No2005-08-302020-10-04US flag
US9198925No2015-12-012020-10-04US flag
US7919598No2011-04-052029-12-16US flag
US8361972Yes2013-01-292028-09-21US flag
US8716251No2014-05-062028-03-21US flag
US8221786No2012-07-172028-03-21US flag
US9339472No2016-05-172025-07-13US flag
US9616028No2017-04-112030-11-12US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySparingly solubleFDA label
Predicted Properties
PropertyValueSource
Water Solubility2.26 mg/mLALOGPS
logP0.88ALOGPS
logP-0.08ChemAxon
logS-2.1ALOGPS
pKa (Strongest Acidic)14.74ChemAxon
pKa (Strongest Basic)7.9ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area90.35 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity83.99 m3·mol-1ChemAxon
Polarizability34.22 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9894
Blood Brain Barrier+0.8823
Caco-2 permeable-0.5446
P-glycoprotein substrateSubstrate0.5909
P-glycoprotein inhibitor INon-inhibitor0.696
P-glycoprotein inhibitor IINon-inhibitor0.7875
Renal organic cation transporterNon-inhibitor0.7903
CYP450 2C9 substrateNon-substrate0.8618
CYP450 2D6 substrateNon-substrate0.7519
CYP450 3A4 substrateSubstrate0.5944
CYP450 1A2 substrateNon-inhibitor0.8448
CYP450 2C9 inhibitorNon-inhibitor0.8017
CYP450 2D6 inhibitorNon-inhibitor0.8198
CYP450 2C19 inhibitorNon-inhibitor0.81
CYP450 3A4 inhibitorNon-inhibitor0.8641
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9032
Ames testNon AMES toxic0.7569
CarcinogenicityNon-carcinogens0.9122
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7529 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9912
hERG inhibition (predictor II)Non-inhibitor0.832
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets
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Details
1. Dipeptidyl peptidase 4
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
  1. 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. [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
  1. 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. [Article]
  2. 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. [Article]
  3. 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. [Article]
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
  1. 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. [Article]
  2. 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. [Article]
  3. 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. [Article]

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
  1. 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. [Article]
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
  1. 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. [Article]
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
  1. 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. [Article]

Drug created on March 19, 2008 16:24 / Updated on May 15, 2021 12:14