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Details

Stereochemistry ABSOLUTE
Molecular Formula C16H15F6N5O
Molecular Weight 407.3136
Optical Activity ( - )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SITAGLIPTIN

SMILES

N[C@@H](CC(=O)N1CCN2C(C1)=NN=C2C(F)(F)F)CC3=C(F)C=C(F)C(F)=C3

InChI

InChIKey=MFFMDFFZMYYVKS-SECBINFHSA-N
InChI=1S/C16H15F6N5O/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22/h4,6,9H,1-3,5,7,23H2/t9-/m1/s1

HIDE SMILES / InChI
Molecular Formula C16H15F6N5O
Molecular Weight 407.3136
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23745054 https://www.ncbi.nlm.nih.gov/pubmed/17580730

Sitagliptin (MK-0431), chemically (2R)-4-Oxo-4-[3- (trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifl uorophenyl)butan-2-amine has a very high selectivity towards DPP-4, with an IC(50) of 18 nM. There is no affinity towards other DDP enzymes (DPP- 8 and DPP-9). It has been approved for the treatment of type 2 diabetes in the USA and Europe and is registered by the name Januvia (Merck Pharmaceuticals, Whitehouse Station, NJ, USA). In healthy volunteers and in patients with type 2 diabetes of different ethnic background, the tolerability of different doses given once or twice daily is good. The drug works to competitively inhibit a protein/enzyme, dipeptidyl peptidase 4 (DPP-4), that results in an increased amount of active incretins (GLP-1 and GIP), reduced amount of release of glucagon (diminishes its release) and increased release of insulin. Sitagliptin is an incretin enhancer and the first marketed medication belonging to the gliptin class. In fact, no published literature exists regarding incidence or severity of hypoglycemia when sitagliptin is used off-label in combined with insulin therapy. However, is recommended to use methods to avoid hypoglycemia when using this off-label combination. Approximately 79% of sitagliptin is excreted unchanged in the urine with metabolism being a minor pathway of elimination. Elimination of sitagliptin occurs primarily via renal excretion and involves active tubular secretion. Sitagliptin is a substrate for human organic anion transporter-3 (hOAT-3), which may be involved in the renal elimination of sitagliptin

Originator

Merck
236
Curator's Comment: # Merck in 1999

Approval Year

2006
191
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8228
 18.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8360
JANUVIA

Approved Use

JANUVIA is a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. (1.1) Important Limitations of Use: •JANUVIA should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. (1.2) •JANUVIA has not been studied in patients with a history of pancreatitis. (1.2, 5.1) 1.1 Monotherapy and Combination Therapy JANUVIA® is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. [See Clinical Studies (14).

Launch Date

1.16095674E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
950 nM
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022044s046lbl.pdf
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SITAGLIPTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
8.52 μM × h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022044s046lbl.pdf
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SITAGLIPTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
12.4 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022044s046lbl.pdf
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SITAGLIPTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
62%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022044s046lbl.pdf
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SITAGLIPTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
200 mg single, oral
Highest studied dose
Dose: 200 mg
Route: oral
Route: single
Dose: 200 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/30346099
unhealthy, 14.8 years
n = 8
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 14.8 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/30346099
Other AEs: Vomiting...
Other AEs:
Vomiting (12.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/30346099
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021995lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/19602719
healthy, 18-45 years
n = 77
Health Status: healthy
Age Group: 18-45 years
Sex: M+F
Population Size: 77
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021995lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/19602719
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021995lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/19602719
1700 mg single, oral
Overdose
Dose: 1700 mg
Route: oral
Route: single
Dose: 1700 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/22277726/
unknown, 86 years
Health Status: unknown
Age Group: 86 years
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/22277726/
Sources:
https://pubmed.ncbi.nlm.nih.gov/22277726/
AEs

AEs

AESignificanceDosePopulation
Vomiting 12.5%
200 mg single, oral
Highest studied dose
Dose: 200 mg
Route: oral
Route: single
Dose: 200 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/30346099
unhealthy, 14.8 years
n = 8
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 14.8 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/30346099
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1709

inducer
768

inhibitor
1579
inhibitor
1752
inhibitor
1837
inhibitor
1599

OverviewOther

Other InhibitorOther SubstrateOther Inducer
OCT transporters
13

CYP
110

P-gp
1437

OAT3
636

CYP1A2
1509

CYP2B6
799

CYP2C8
901

CYP2C19
1463
CYP2C8
688

OAT3
333

P-gp
1527

OAT1
320

PEPT1
48

OCT2
348

OAT4
76
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1673
 no [IC50 >100 uM]
CYP2B6
985
 no [IC50 >100 uM]
CYP2C19
1537
 no [IC50 >100 uM]
CYP2C8
955
 no [IC50 >100 uM]
CYP2C9
1803
 no [IC50 >100 uM]
CYP2D6
1875
 no [IC50 >100 uM]
CYP3A4
1909
 no [IC50 >100 uM]
no (co-administration study)
Comment: results indicated that sitagliptin was not a time-dependent inhibitor of CYP3A4; sitagliptin did not meaningfully alter the pharmacokinetics of simvastatin.
Page: 15, 30
CYP
146
 no
CYP3A4
1909
 no
OAT3
638
 no
OCT transporters
13
 no
P-gp
1626
 no
no (co-administration study)
Comment: sitagliptin had no inhibitory effect on the P-gp mediated transport of digoxin, verapmil, ritonavir, adn vinblastine
Page: 15.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
OAT4
76
 inconclusive
OAT1
320
 no
OCT2
348
 no
PEPT1
48
 no
CYP2C8
688
 yes
CYP3A4
1709
 yes
OAT3
333
 yes
P-gp
1527
 yes
yes (co-administration study)
Comment: cyclosporin A significantly inhibited P-gp transport of sitagliptin
Page: 4, 15
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1632
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:40237
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:40237
ChemicalBook
CB01449778
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB01449778
MolPort
MolPort-003-666-756
https://www.molport.com/shop/molecule-link/MolPort-003-666-756
ZINC
ZINC000001489478
http://zinc15.docking.org/substances/ZINC000001489478
eMolecules
6755163
https://www.emolecules.com/cgi-bin/more?vid=6755163
PubMed

PubMed

TitleDatePubMed
MK-431 (Merck).
2005 Apr
New therapeutic strategies for the treatment of type 2 diabetes mellitus based on incretins.
2005 Summer
The development of a stable, coated pellet formulation of a water-sensitive drug, a case study: development of a stable core formulation.
2006
Dipeptidyl peptidase IV (DPP IV) inhibitors: A newly emerging drug class for the treatment of type 2 diabetes.
2006 Dec
Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone.
2006 Dec
First-in-class diabetes drug approved.
2006 Dec 1
Sitagliptin: a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
2006 Jul-Aug
[Dipeptidylpeptidase IV inhibitors and dual action PPAR-agonists].
2006 Mar
Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus.
2006 Nov
Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing pioglitazone therapy in patients with type 2 diabetes: a 24-week, multicenter, randomized, double-blind, placebo-controlled, parallel-group study.
2006 Oct
Oral agents for type 2 diabetes reduce HbA1c, are weight neutral.
2006 Sep
Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
2007
[Glucagon-like peptide-1 (GLP-1), new target for the treatment of type 2 diabetes].
2007 Apr
Characterization of two cyclic metabolites of sitagliptin.
2007 Apr
Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C]sitagliptin in humans.
2007 Apr
[Incretin enhancers, incretin mimetics: from therapeutic concept to clinical application].
2007 Apr 1
Antihyperglycaemic therapy in elderly patients with type 2 diabetes: potential role of incretin mimetics and DPP-4 inhibitors.
2007 Aug
Incretins: a new treatment option for type 2 diabetes?
2007 Feb
Effect of a single cyclosporine dose on the single-dose pharmacokinetics of sitagliptin (MK-0431), a dipeptidyl peptidase-4 inhibitor, in healthy male subjects.
2007 Feb
Finding new treatments for diabetes--how many, how fast... how good?
2007 Feb 1
Efficacy and tolerability of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy over 12 weeks in patients with type 2 diabetes.
2007 Jan
Effect of renal insufficiency on the pharmacokinetics of sitagliptin, a dipeptidyl peptidase-4 inhibitor.
2007 Jul
Dipeptidyl peptidase 4 (DPP-4) inhibitors and their role in Type 2 diabetes management.
2007 Jul-Aug
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
2007 Jun 15
New treatments for diabetes.
2007 May 24
Absolute bioavailability of sitagliptin, an oral dipeptidyl peptidase-4 inhibitor, in healthy volunteers.
2007 Sep
Sensitive liquid chromatography tandem mass spectrometry method for the quantification of sitagliptin, a DPP-4 inhibitor, in human plasma using liquid-liquid extraction.
2008 Feb
Efficacy and safety of sitagliptin monotherapy in Japanese patients with type 2 diabetes.
2008 Feb
Dipeptidyl peptidase IV inhibitors and diabetes therapy.
2008 Jan 1
Patents

Patents

07495123
9
08183373
9
08309724
9
08329696
9
08389724
9
08476437
9
20030100563
9
20040167133
9
20050032804
9
JP2010155857A
9
JP2010527621A
9
JP2011509922A
11
JP2011510067A
55
JP2011510954A
142
JP2011529945A
20
JP2012500190A
21

Sample Use Guides

In Vivo Use Guide
100 mg once daily. It can be taken with or without food.
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment: Sitagliptin therapy enhances circulating angiogenic cell numbers, angiogenesis and blood flow in the critical limb ischemia area.
Adipose tissue from adult-male Fischer 344 rats were cultured in endothelial progenitor cell culture medium for 14 d with (25 μmol/L) or without sitagliptin.
Substance Class Chemical
Created
by admin
on Thu Jul 06 22:29:43 UTC 2023
Edited
by admin
on Thu Jul 06 22:29:43 UTC 2023
Record UNII
QFP0P1DV7Z
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SITAGLIPTIN
EMA EPAR   HSDB   INN   MI   VANDF   WHO-DD  
INN   USAN  
Official Name English
(2R)-4-OXO-4-(3-(TRIFLUOROMETHYL)-5,6-DIHYDRO(1,2,4)TRIAZOLO(4,3-A)PYRAZIN-7(8H)-YL)-1-(2,4,5-TRIFLUOROPHENYL)BUTAN-2-AMINE
Systematic Name English
sitagliptin [INN]
Common Name English
SITAGLIPTIN [EMA EPAR]
Common Name English
SITAGLIPTIN [HSDB]
Common Name English
SITAGLIPTIN [USAN]
Common Name English
SITAGLIPTIN [MI]
Common Name English
Sitagliptin [WHO-DD]
Common Name English
LEZ-763
Code English
1,2,4-TRIAZOLO(4,3-A)PYRAZINE-7(8H)-PROPANAMINE, 5,6-DIHYDRO-.GAMMA.-OXO-3-(TRIFLUOROMETHYL)-.ALPHA.-((2,4,5-TRIFLUOROPHENYL)METHYL)-, (.ALPHA.R)-
Common Name English
LEZ763
Code English
SITAGLIPTIN [VANDF]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C98086
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
WHO-VATC QA10BD12
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
WHO-VATC QA10BH51
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
NDF-RT N0000175913
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
WHO-ATC A10BH51
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
WHO-ATC A10BD07
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
NDF-RT N0000175912
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
WHO-ATC A10BD24
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
LIVERTOX NBK548083
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
WHO-ATC A10BH01
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
WHO-VATC QA10BD07
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
WHO-VATC QA10BH01
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
WHO-ATC A10BD12
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
Code System Code Type Description
CAS
486460-32-6
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
FDA UNII
QFP0P1DV7Z
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
SMS_ID
100000091875
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
NCI_THESAURUS
C73838
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
EPA CompTox
DTXSID70197572
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
INN
8692
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
LACTMED
Sitagliptin
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
HSDB
7516
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
ChEMBL
CHEMBL1422
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
EVMPD
SUB25227
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
PUBCHEM
4369359
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
MESH
C496398
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
RXCUI
593411
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY RxNorm
WIKIPEDIA
SITAGLIPTIN
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
IUPHAR
6286
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
USAN
JK-166
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
DRUG BANK
DB01261
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
MERCK INDEX
M9960
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY Merck Index
DAILYMED
QFP0P1DV7Z
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
DRUG CENTRAL
2448
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
CHEBI
40237
Created by admin on Thu Jul 06 22:29:45 UTC 2023 , Edited by admin on Thu Jul 06 22:29:45 UTC 2023
PRIMARY
Related Record Type Details
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Structure of SITAGLIPTIN
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
DIPEPTIDYL PEPTIDASE 4 MEMBRANE FORM
TARGET -> INHIBITOR
Structure of SITAGLIPTIN L-MALATE
SALT/SOLVATE -> PARENT
Structure of SITAGLIPTIN PHOSPHATE
SALT/SOLVATE -> PARENT
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
OAT-3
TRANSPORTER -> INHIBITOR
Structure of SITAGLIPTIN PHOSPHATE ANHYDROUS
SALT/SOLVATE -> PARENT
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
Structure of SITAGLIPTIN HYDROCHLORIDE
SALT/SOLVATE -> PARENT
Structure of SITAGLIPTIN SULFATE
SALT/SOLVATE -> PARENT
Structure of SITAGLIPTIN TARTRATE HEMIHYDRATE
SALT/SOLVATE -> PARENT
Structure of SITAGLIPTIN HYDROCHLORIDE MONOHYDRATE
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of .BETA.-D-GLUCOPYRANURONIC ACID, 1-(N-((1R)-3-(5,6-DIHYDRO-3-(TRIFLUOROMETHYL)-1,2,4-TRIAZOLO(4,3-A)PYRAZIN-7(8H)-YL)-3-OXO-1-((2,4,5-TRIFLUOROPHENYL)METHYL)PROPYL)CARBAMATE)
METABOLITE -> PARENT
MINOR
PLASMA
Structure of (10R,11AR)-5,6,9,10,11,11A-HEXAHYDRO-3-(TRIFLUOROMETHYL)-10-((2,4,5-TRIFLUOROPHENYL)METHYL)-8H-1,2,4-TRIAZOLO(3',4':3,4)PYRAZINO(1,2-A)PYRIMIDIN-8-ONE
METABOLITE -> PARENT
MINOR
PLASMA
Structure of (10R,11AS)-5,6,9,10,11,11A-HEXAHYDRO-3-(TRIFLUOROMETHYL)-10-((2,4,5-TRIFLUOROPHENYL)METHYL)-8H-1,2,4-TRIAZOLO(3',4':3,4)PYRAZINO(1,2-A)PYRIMIDIN-8-ONE
METABOLITE -> PARENT
MINOR
PLASMA
Structure of SITAGLIPTIN N-SULFATE
METABOLITE -> PARENT
MINOR
PLASMA
Related Record Type Details
Structure of SITAGLIPTIN
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC ORAL ADMINISTRATION

SINGLE DOSE

Volume of Distribution PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

SINGLE DOSE

Tmax PHARMACOKINETIC DOSE

ORAL ADMINISTRATION

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