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

Similar Structures

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

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Pharmacology

Indication

Treatment of type 2 diabetes mellitus to improve glycemic control in combination with other agents or as monotherapy.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Patient Characteristics	Dose Form
Used as adjunct in combination to manage	Type 2 diabetes mellitus	Combination Product in combination with: Metformin (DB00331), Dapagliflozin (DB06292)	••••••••••••	•••••••••• •••••••• •• ••••• ••••••••••• ••••••••	••••••
Used in combination to manage	Type 2 diabetes mellitus	Combination Product in combination with: Metformin (DB00331), Dapagliflozin (DB06292)	••••••••••••	•••••••••• •••••••• •• ••••• ••••••••••• ••••••••	••••••
Used as adjunct in combination to manage	Type 2 diabetes mellitus	Combination Product in combination with: Metformin (DB00331)	••••••••••••
Used as adjunct in combination to manage	Type 2 diabetes mellitus	Combination Product in combination with: Dapagliflozin (DB06292)	••••••••••••	•••••••••• ••••••• •••• •••••••••••••
Used as adjunct in combination to manage	Type 2 diabetes mellitus	Combination Product in combination with: Dapagliflozin (DB06292)	••••••••••••	••••••• ••••••• •••• ••••••••••••• ••• •••••••••••

Contraindications & Blackbox Warnings

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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.

Target	Actions	Organism
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.

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Saxagliptin
- 5-hydroxy saxagliptin

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

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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

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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
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Abacavir	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.

Food Interactions

Take with food. Food increases total drug exposure.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Saxagliptin hydrochloride	Z8J84YIX6L	709031-78-7	TUAZNHHHYVBVBR-NHKADLRUSA-N
Saxagliptin hydrochloride dihydrate	4N19ON48ZN	1073057-20-1	AJXATZPZZXZZRE-ZEGDOHPJSA-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
Onglyza	Tablet, film coated	5 mg	Oral	Astra Zeneca Ab	2016-09-08	Not applicable
Onglyza	Tablet, film coated	5 mg	Oral	Astra Zeneca Ab	2016-09-08	Not applicable
Onglyza	Tablet, film coated	5 mg	Oral	Astra Zeneca Ab	2016-09-08	Not applicable
Onglyza	Tablet, film coated	5 mg/1	Oral	Cardinal Health 107, LLC	2014-11-20	Not applicable
Onglyza	Tablet, film coated	5 mg/1	Oral	Cardinal Health	2009-07-31	2017-04-30

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Apo-saxagliptin	Tablet	5 mg	Oral	Apotex Corporation	2021-03-29	Not applicable
Apo-saxagliptin	Tablet	2.5 mg	Oral	Apotex Corporation	2021-03-29	Not applicable
Pro-saxagliptin	Tablet	2.5 mg	Oral	Pro Doc Limitee	Not applicable	Not applicable
Pro-saxagliptin	Tablet	5 mg	Oral	Pro Doc Limitee	Not applicable	Not applicable
Sandoz Saxagliptin	Tablet	2.5 mg	Oral	Sandoz Canada Incorporated	2021-03-08	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
KOMBIGLYZE ® XR 5 MG/ 1000 MG	Saxagliptin (5 mg) + Metformin hydrochloride (1000 mg)	Tablet, extended release	Oral	ASTRAZENECA COLOMBIA S.A.S.	2012-06-16	Not applicable
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
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
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
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

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. [Article]
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]
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]
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]
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]
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]
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]
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]

External Links

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

FDA label

Download (492 KB)

MSDS

Download (479 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	Completed	Basic Science	Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Coronary Artery Disease (CAD) / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Diabetes Mellitus	1
4	Completed	Treatment	Diabetes Mellitus, Noninsulin Dependent	1
4	Completed	Treatment	Diabetes Mellitus, Noninsulin Dependent / Heart Failure	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Tablet, film coated, extended release	Oral
Tablet	Oral
Tablet, film coated, extended release	Oral	1000 mg
Tablet, film coated, extended release	Oral	500 mg
Tablet, extended release	Oral
Tablet, coated	Oral
Tablet	Oral
Tablet	Oral	2.5 mg
Tablet	Oral	2.500 mg
Tablet	Oral	5 mg
Tablet, film coated	Oral
Tablet, film coated	Oral	2.5 mg/1
Tablet, film coated	Oral	5 mg/1
Tablet, film coated	Oral	2.5 mg
Tablet, film coated	Oral	5 mg
Tablet, coated	Oral	2.5 mg
Tablet, film coated	Oral
Tablet, coated	Oral	5 mg

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US6395767	No	2002-05-28	2021-02-16
USRE44186	No	2013-04-30	2023-07-31
US7951400	No	2011-05-31	2028-11-30
US8628799	No	2014-01-14	2025-07-13
US8501698	Yes	2013-08-06	2027-12-20
US6414126	No	2002-07-02	2020-10-04
US6515117	Yes	2003-02-04	2026-04-04
US6936590	No	2005-08-30	2020-10-04
US9198925	No	2015-12-01	2020-10-04
US7919598	No	2011-04-05	2029-12-16
US8361972	Yes	2013-01-29	2028-09-21
US8716251	No	2014-05-06	2028-03-21
US8221786	No	2012-07-17	2028-03-21
US9339472	No	2016-05-17	2025-07-13
US9616028	No	2017-04-11	2030-11-12

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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-0ue9-9810000000-9ea6dee5e5df7feeccf4
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-014i-0029000000-a6e092a1c43df8a60005
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-03di-0009000000-cc06168ea0c6191b5171
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-001r-0922000000-352f7caed3706d51359c
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-03di-0559000000-c1fd99c43d89a3cdf931
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-001l-9800000000-ac78e4041a28a6c22583
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-01ox-7891000000-b02c5522e9dbffe947ac
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å²)	Source type	Source
[M-H]-	179.7796122	predicted	DarkChem Lite v0.1.0
[M-H]-	179.8603122	predicted	DarkChem Lite v0.1.0
[M-H]-	167.64781	predicted	DeepCCS 1.0 (2019)
[M+H]+	180.7809122	predicted	DarkChem Lite v0.1.0
[M+H]+	180.7848122	predicted	DarkChem Lite v0.1.0
[M+H]+	170.04338	predicted	DeepCCS 1.0 (2019)
[M+Na]+	179.9080122	predicted	DarkChem Lite v0.1.0
[M+Na]+	175.95592	predicted	DeepCCS 1.0 (2019)

Targets

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Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	3	N/A	N/A	A30381
IC 50 (nM)	3.4	N/A	N/A	A29631
IC 50 (nM)	0.6	N/A	N/A	A29636
IC 50 (nM)	3.37	N/A	N/A	A29639
Ki (nM)	0.6	N/A	N/A	A30612 / A30380 / A29630

Details1. 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

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]
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

Details1. Cytochrome P450 3A5

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. [Article]
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]
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]

Details2. Cytochrome P450 3A4

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. [Article]
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]
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

Details1. Multidrug resistance-associated protein 1

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. [Article]

Details2. Solute carrier organic anion transporter family member 4C1

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. [Article]

Details3. Solute carrier family 22 member 8

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. [Article]

Drug created at March 19, 2008 16:24 / Updated at February 20, 2024 23:55

Saxagliptin

Identification

Structure for Saxagliptin (DB06335)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

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Clinical Trials

Pharmacoeconomics

Properties

Spectra

Collision Cross Sections (CCS)

Targets

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Enzymes

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Transporters

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