SAXAGLIPTIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C18H25N3O2.H2O
Molecular Weight	333.4253
Optical Activity	UNSPECIFIED
Defined Stereocenters	4 / 6
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.N[C@H](C(=O)N1[C@H]2C[C@H]2C[C@H]1C#N)C34CC5CC(CC(O)(C5)C3)C4

InChI

InChIKey=AFNTWHMDBNQQPX-NHKADLRUSA-N

InChI=1S/C18H25N3O2.H2O/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;1H2/t10?,11?,12-,13+,14+,15-,17?,18?;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C18H25N3O2
Molecular Weight	315.41
Charge	0
Count

Stereochemistry	MIXED
Additional Stereochemistry	No
Defined Stereocenters	4 / 6
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	H2O
Molecular Weight	18.0153
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.drugbank.ca/drugs/DB06335
Curator's Comment: Description was created based on several sources, including https://www.drugs.com/monograph/saxagliptin-hydrochloride.html

Saxagliptin 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. 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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dipeptidyl peptidase IV 37 Target ID: CHEMBL284 Sources: http://www.drugbank.ca/drugs/DB06335 \| https://www.ncbi.nlm.nih.gov/pubmed/18223196	Inhibitor 8504		30.3 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262 Sources: https://www.drugs.com/monograph/saxagliptin-hydrochloride.html	Primary		Approved 8583	Onglyza Approved Use Diabetes mellitus, type 2: As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (noninsulin dependent, NIDDM) as monotherapy or in combination therapy. Launch Date 2009

C_max

Value	Dose	Co-administered	Analyte	Population
24 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		SAXAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
78 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		SAXAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.5 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		SAXAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
100% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		SAXAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
10 mg 1 times / day steady, oral Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19650754/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/19650754/	Disc. AE: Adverse event... AEs leading to discontinuation/dose reduction: Adverse event (5.1%) Sources: https://pubmed.ncbi.nlm.nih.gov/19650754/
2.5 mg 1 times / day steady, oral Recommended Dose: 2.5 mg, 1 times / day Route: oral Route: steady Dose: 2.5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	Disc. AE: Lymphopenia, Rash... AEs leading to discontinuation/dose reduction: Lymphopenia (0.1%) Rash (0.2%) Blood creatinine increased (0.3%) Blood creatine phosphokinase increased (0.1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf
5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	Disc. AE: Lymphopenia, Rash... AEs leading to discontinuation/dose reduction: Lymphopenia (0.5%) Rash (0.3%) Blood creatine phosphokinase increased (0.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf

AEs

AE	Significance	Dose	Population
Adverse event	5.1% Disc. AE	10 mg 1 times / day steady, oral Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: steady Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19650754/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/19650754/
Blood creatine phosphokinase increased	0.1% Disc. AE	2.5 mg 1 times / day steady, oral Recommended Dose: 2.5 mg, 1 times / day Route: oral Route: steady Dose: 2.5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf
Lymphopenia	0.1% Disc. AE	2.5 mg 1 times / day steady, oral Recommended Dose: 2.5 mg, 1 times / day Route: oral Route: steady Dose: 2.5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf
Rash	0.2% Disc. AE	2.5 mg 1 times / day steady, oral Recommended Dose: 2.5 mg, 1 times / day Route: oral Route: steady Dose: 2.5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf
Blood creatinine increased	0.3% Disc. AE	2.5 mg 1 times / day steady, oral Recommended Dose: 2.5 mg, 1 times / day Route: oral Route: steady Dose: 2.5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf
Blood creatine phosphokinase increased	0.2% Disc. AE	5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf
Rash	0.3% Disc. AE	5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf
Lymphopenia	0.5% Disc. AE	5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087	inhibitor 2438 inducer 440	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2A6 879 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 CYP2E1 1060 CYP3A4/5 296 P-gp 1741 OCT2 779	CYP3A4/5 91 CYP1A2 1197 CYP2C19 1119 P-gp 2052 OATP1B1 503 OATP1B3 435 OCT1 393 OCT2 434 OAT1 395 OAT3 391 PEPT1 60 PEPT2 37	CYP3A4/5 133 CYP1A2 832 CYP2B6 669 P-gp 301

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	inconclusive
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
CYP3A4/5 357	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf#page=17 Page: 17.0	no	no (co-administration study) Comment: administration with simvastatin did not alter PK of metformin; administration with diltiazem increased the plasma Cmax of diltiazem by 16%, AUC of diltiazem was unchagned Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf#page=17 Page: 17.0
CYP3A4/5 357	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf#page=17 Page: 17.0	no	no (co-administration study) Comment: administration with simvastatin did not alter PK of metformin; administration with diltiazem increased the plasma Cmax of diltiazem by 16%, AUC of diltiazem was unchanged; administration with ketoconazole decreased Cmax and AUC of ketoconazole by 16% and 13%, respectively; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf#page=17 Page: 17.0
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf#page=16 Page: 16.0	no	no (co-administration study) Comment: administration with metformin did not alter PK of metformin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022350lbl.pdf#page=16 Page: 16.0
P-gp 1932	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no	no (co-administration study) Comment: administered with digoxin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no	no (co-administration study) Comment: administered with digoxin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no	unlikely (co-administration study) Comment: no concentration and time-dependent inhibtion; administration with pioglitazone increased the plasma Cmax of glyburide by 14%, AUC was unchanged. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no	unlikely (co-administration study) Comment: no concentration and time-dependent inhibtion; administration with glyburide increased the plasma Cmax of glyburide by 16%, AUC was unchanged. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4/5 91	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=38 Page: 38,42	major	yes (co-administration study) Comment: ketoconazole increased the Cmax for saxagliptin by 62% and the AUC by 2.5-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=38 Page: 38,42
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=38 Page: 38.0	minor
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=38 Page: 38.0	minor
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=38 Page: 38.0	minor
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=40 Page: 40.0	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=40 Page: 40.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=40 Page: 40.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=40 Page: 40.0	no
PEPT1 60	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=40 Page: 40.0	no
PEPT2 37	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=40 Page: 40.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0	yes	no (co-administration study) Comment: administration with digoxin did not alter PK of saxagliptin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_ClinPharmR_P1.pdf#page=39 Page: 39.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022350s000_PharmR_P5.pdf#page=31 Page: 31.0

Sourcing

Vendor/Aggregator	ID	URL
Achemo Scientific Limited	AC-73827	http://www.achemo.com/search/?Keyword=361442-04-8
Achemtek	0101-002229	http://www.achemtek.com/361442-04-8
Achemtek	0102-022621	http://www.achemtek.com/361442-04-8
Acorn PharmaTech	ACN-031557	http://www.acornpharmatech.com/
Adooq BioScience	Saxagliptin - BMS-477118	http://www.adooq.com/saxagliptin-bms-477118.html
Ambeed	A354223	https://www.ambeed.com/products/361442-04-8.html
Ambinter	Amb17620035	http://www.ambinter.com/reference/17620035
Aurora Fine Chemicals LLC	A24.090.433	http://online.aurorafinechemicals.com/info?ID=A24.090.433
Aurum Pharmatech LLC	Q-4418	http://www.Aurumpharmatech.com/Product/ProductDetails/Q_4418
AvaChem Scientific	2771	http://www.avachem.com/productSearch.asp?2771
BioCrick	BCC3934	http://www.biocrick.com/Saxagliptin-BCC3934.html
BLD Pharm	BD162102	http://www.bldpharm.com/products/361442-04-8.html
Chem Scene	CS-0650	http://www.chemscene.com/361442-04-8.html
ChemMol	30112400	http://www.chemmol.com/chemmol/30112400.html
ChemMol	44014170	http://www.chemmol.com/chemmol/44014170.html
Chemspace	CSSB00015193110	https://chem-space.com/CSSB00015193110
CSNpharm	CSN12346	https://www.csnpharm.com/products/saxagliptin.html
DC Chemicals	DC8875	http://www.dcchemicals.com/product_show-Saxagliptin.html
Enamine	Z2235802036	https://www.enaminestore.com/catalog/Z2235802036
eNovation Chemicals	D541352	https://www.enovationchem.com/ProductDetails.asp?ProductID=D541352
eNovation Chemicals	Y0973983	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0973983
iChemical	EBD1390	http://www.ichemical.com/products/361442-04-8.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network	LN01295323	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01295323
LGC Standards	MM3377.01	https://www.lgcstandards.com/US/en/p/MM3377.01
Matrix Scientific	122721	https://www.matrixscientific.com/122721.html
MedChem Express	HY-10285	https://www.medchemexpress.com/Saxagliptin.html
Parkway Scientific	WU-553	http://www.parkwayscientific.com/searchproduct.php?txt_search=WU-553
Selleck Chemicals	S1540	http://www.selleckchem.com/products/Saxagliptin(Onglyza).html
Smolecule	S639894	https://www.smolecule.com/products/s639894
THE BioTek	bt-345214	https://www.thebiotek.com/product/others/bt-345214
VladaChem	VL281619-10MG	https://www.vladachem.com/product.php?products=361442-04-8
Yuhao Chemical	CJ2102	http://www.chemyuhao.com/361442-04-8.html

PubMed

Title	Date	PubMed
Antihyperglycemic effects of ASP8497 in streptozotocin-nicotinamide induced diabetic rats: comparison with other dipeptidyl peptidase-IV inhibitors.	2008-12-03	19904014
(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors.	2008-04	18223196

Patents

Sample Use Guides

In Vivo Use Guide

Diabetes Mellitus Monotherapy Oral 2.5 or 5 mg once daily.1 Higher dosages (e.g., 10 mg once daily) did not provide additional benefit in clinical trials and are not recommended by manufacturer.

Route of Administration: Oral

In Vitro Use Guide

Saxagliptin inhibited rat plasma DPP-IV activity in vitro with an IC(50) value of 2.00 nmol/l

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:18:12 GMT 2025` Edited by `admin` on `Mon Mar 31 18:18:12 GMT 2025`
Record UNII	9GB927LAJW
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SAXAGLIPTIN

Official Name

English

SAXAGLIPTIN MONOHYDRATE

Preferred Name

English

BMS-477118-11

Code

English

SAXAGLIPTIN HYDRATE

Common Name

English

SAXAGLIPTIN [USAN]

Common Name

English

(1S,3S,5S)-2-((2S)-AMINO(3-HYDROXYTRICYCLO(3.3.1.1(SUP 3,7))DEC-1-YL)ACETYL)2-AZABICYCLO(3.1.0)HEXANE-3-CARBONITRILE MONOHYDRATE

Systematic Name

English

QTERNMET COMPONENT SAXAGLIPTIN

Brand Name

English

SAXAGLIPTIN MONOHYDRATE [MI]

Common Name

English

SAXAGLIPTIN [MART.]

Common Name

English

Saxagliptin monohydrate [WHO-DD]

Common Name

English

NSC-760407

Code

English

SAXAGLIPTIN [VANDF]

Common Name

English

SAXAGLIPTIN HYDRATE [JAN]

Common Name

English

2-AZABICYCLO(3.1.0)HEXANE-3-CARBONITRILE, 2-((2S)-2-AMINO-2-(3-HYDROXYTRICYCLO(3.3.1.1(SUP 3,7))DEC-1-YL)ACETYL)-, HYDRATE (1:1), (1S,3S,5S)-

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C98086