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vildagliptin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
dipeptidyl aminopeptidase-IV inhibitors	3642	274901-16-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: xiliarx galvus vildagliptin jalra NVP-LAF237 vildagliptin hydrochloride vildagliptin HCl	A pyrrolidine-carbonitrile derivative and potent inhibitor of DIPEPTIDYL PEPTIDASE 4 that is used in the treatment of TYPE 2 DIABETES MELLITUS. Molecular weight: 303.41 Formula: C17H25N3O2 CLOGP: 0.97 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 76.36 ALOGS: -2.24 ROTB: 3

Molecule

Description

Molfile Inchi Smiles

Synonyms:

xiliarx
galvus
vildagliptin
jalra
NVP-LAF237
vildagliptin hydrochloride
vildagliptin HCl

A pyrrolidine-carbonitrile derivative and potent inhibitor of DIPEPTIDYL PEPTIDASE 4 that is used in the treatment of TYPE 2 DIABETES MELLITUS.

Molecular weight: 303.41
Formula: C17H25N3O2
CLOGP: 0.97
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 76.36
ALOGS: -2.24
ROTB: 3

Drug dosage:

Dose	Unit	Route
0.10	g	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	9.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	85 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	60 mg/mL	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	1.67 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.03 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.89 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Sept. 26, 2007	EMA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pemphigoid	1098.77	23.58	217	4266	7127	63477412
Lactic acidosis	239.66	23.58	93	4390	38194	63446345
Acute kidney injury	133.02	23.58	125	4358	263290	63221249
Hypoglycaemia	108.92	23.58	62	4421	60003	63424536
Diabetes mellitus inadequate control	74.58	23.58	31	4452	15095	63469444
Dermatitis bullous	61.49	23.58	23	4460	8485	63476054
Crush syndrome	60.03	23.58	10	4473	119	63484420
Sensorimotor disorder	52.52	23.58	11	4472	475	63484064
Compartment syndrome	48.68	23.58	14	4469	2270	63482269
Hyperkalaemia	48.63	23.58	36	4447	54167	63430372

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pemphigoid	881.43	20.47	215	5214	8451	34943051
Diabetes mellitus inadequate control	80.27	20.47	40	5389	13424	34938078
Hyperglycaemia	65.49	20.47	52	5377	39428	34912074
Cardiac failure	62.81	20.47	74	5355	91174	34860328
Hypoglycaemia	56.48	20.47	55	5374	54585	34896917
Acute kidney injury	53.42	20.47	134	5295	304854	34646648
Cerebral infarction	51.70	20.47	39	5390	27416	34924086
Euglycaemic diabetic ketoacidosis	50.63	20.47	19	5410	3203	34948299
Glycosylated haemoglobin increased	45.77	20.47	26	5403	11334	34940168
Ketonuria	41.39	20.47	11	5418	600	34950902

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pemphigoid	1894.95	18.12	427	9498	14888	79719575
Lactic acidosis	216.75	18.12	125	9800	70234	79664229
Acute kidney injury	171.29	18.12	262	9663	519142	79215321
Hypoglycaemia	147.64	18.12	113	9812	101481	79632982
Diabetes mellitus inadequate control	116.58	18.12	58	9867	24206	79710257
Hyperglycaemia	108.24	18.12	81	9844	70254	79664209
Hyperkalaemia	90.48	18.12	90	9835	114308	79620155
Euglycaemic diabetic ketoacidosis	88.58	18.12	33	9892	6811	79727652
Cerebral infarction	84.87	18.12	59	9866	45617	79688846
Drug interaction	77.72	18.12	164	9761	415019	79319444

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A10BD08	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs
ATC	A10BH02	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Dipeptidyl peptidase 4 (DPP-4) inhibitors
MeSH PA	D054873	Dipeptidyl-Peptidase IV Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D007004	Hypoglycemic Agents
MeSH PA	D011480	Protease Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Diabetes mellitus type 2	indication	44054006	DOID:9352

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.1	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Dipeptidyl peptidase 4	Enzyme	P27487	DPP4_HUMAN	INHIBITOR	Ki	8.52	CHEMBL	DRUG LABEL
Dipeptidyl peptidase 8	Enzyme	Q6V1X1	DPP8_HUMAN		Ki	6.09	CHEMBL
Dipeptidyl peptidase 9	Enzyme	Q86TI2	DPP9_HUMAN		Ki	7.17	CHEMBL
Prolyl endopeptidase FAP	Enzyme	Q12884	SEPR_HUMAN		IC50	5.43	CHEMBL
Dipeptidyl peptidase 9	Unclassified		E1BI31_BOVIN		IC50	6.17	CHEMBL
Dipeptidyl peptidase IV	Unclassified		O31048_PORGN		Ki	7.77	CHEMBL
Prolyl endopeptidase FAP	Enzyme		SEPR_MOUSE		IC50	4.28	CHEMBL

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External reference:

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ID	Source
012358	NDDF
428611002	SNOMEDCT_US
428807006	SNOMEDCT_US
596554	RXNORM
6310	IUPHAR_LIGAND_ID
6918537	PUBCHEM_CID
8399	INN_ID
924914-75-0	SECONDARY_CAS_RN
C1570906	UMLSCUI
CHEBI:135285	CHEBI

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Pharmaceutical products:

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