vildagliptin

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

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	-0.215		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	4.624		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	2.051	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	2.399	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	78.720	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	76.600	%	High	1
herg	hERG pIC50	4.159	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	1.361	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	3.311	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	77.660	%	High	1
kinase-safety-class	EIF2AK3,GRK2,PDK1,PDK2,PDK4	5
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	2.328		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	3.041		High	1
mppb	Mouse plasma protein binding (% unbound)	84.870		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	4.315		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	84.720	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	1.742	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	89.950	%	High	1
rppb	Rat plasma protein binding (% unbound)	82.750	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	887.156	uM	High	1

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	1164.39	23.42	230	5275	8796	90614146
Lactic acidosis	291.55	23.42	111	5394	50352	90572590
Acute kidney injury	196.23	23.42	159	5346	320228	90302714
Hypoglycaemia	165.64	23.42	82	5423	69766	90553176
Compartment syndrome	145.07	23.42	34	5471	2878	90620064
Euglycaemic diabetic ketoacidosis	93.09	23.42	28	5477	6173	90616769
Diabetes mellitus inadequate control	72.75	23.42	31	5474	18653	90604289
Glycosylated haemoglobin increased	67.89	23.42	28	5477	15534	90607408
Dermatitis bullous	67.84	23.42	25	5480	10291	90612651
Hyperkalaemia	63.79	23.42	43	5462	64921	90558021
Shock	62.86	23.42	32	5473	28746	90594196
Ketoacidosis	61.87	23.42	20	5485	5575	90617367
Hyperglycaemia	60.49	23.42	38	5467	50932	90572010
Drug interaction	55.86	23.42	76	5429	276377	90346565
Crush syndrome	52.81	23.42	10	5495	299	90622643
Sensorimotor disorder	49.34	23.42	11	5494	744	90622198
Altered state of consciousness	49.08	23.42	28	5477	31504	90591438
Renal impairment	47.34	23.42	44	5461	105377	90517565
Diabetic ketoacidosis	47.16	23.42	25	5480	24382	90598560
Acute generalised exanthematous pustulosis	44.45	23.42	20	5485	13683	90609259
Polymyalgia rheumatica	43.89	23.42	15	5490	4962	90617980
Eosinophilia	43.51	23.42	25	5480	28508	90594434
Blood glucose increased	41.31	23.42	39	5466	95207	90527735
Rhabdomyolysis	41.14	23.42	30	5475	51226	90571716
Intentional overdose	39.89	23.42	38	5467	93796	90529146
Cerebral infarction	39.74	23.42	23	5482	26573	90596369
Overdose	39.07	23.42	48	5457	157661	90465281
Diabetic metabolic decompensation	38.93	23.42	11	5494	1946	90620996
Hypomagnesaemia	38.41	23.42	25	5480	35563	90587379
Pancreatitis acute	38.23	23.42	24	5481	32091	90590851
Ischaemic stroke	38.07	23.42	21	5484	22145	90600797
Angioedema	36.95	23.42	31	5474	64845	90558097
Language disorder	35.63	23.42	11	5494	2641	90620301
Thrombocytosis	35.36	23.42	14	5491	6987	90615955
Hyperparathyroidism secondary	35.27	23.42	10	5495	1791	90621151
Capillary leak syndrome	35.17	23.42	11	5494	2756	90620186
Anuria	33.88	23.42	17	5488	14801	90608141
Hyperphosphataemia	32.00	23.42	11	5494	3700	90619242
Urine ketone body present	31.83	23.42	10	5495	2542	90620400
Inflammatory marker increased	31.65	23.42	14	5491	9200	90613742
Hypoparathyroidism	31.10	23.42	8	5497	993	90621949
Bladder sphincter atony	30.45	23.42	6	5499	222	90622720
Blood phosphorus increased	30.37	23.42	11	5494	4307	90618635
Drug reaction with eosinophilia and systemic symptoms	29.80	23.42	23	5482	42735	90580207
Cardiac failure acute	28.20	23.42	14	5491	11915	90611027
Coma	26.37	23.42	27	5478	72605	90550337
Cutaneous lupus erythematosus	25.95	23.42	9	5496	3109	90619833
Haemodynamic instability	25.47	23.42	13	5492	11726	90611216
Hypotension	25.43	23.42	59	5446	325338	90297604
Disseminated intravascular coagulation	25.39	23.42	16	5489	21522	90601420
Subacute cutaneous lupus erythematosus	24.73	23.42	9	5496	3573	90619369
Acquired perforating dermatosis	24.05	23.42	3	5502	3	90622939

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	975.41	19.64	247	6432	11220	42603436
Diabetes mellitus inadequate control	95.14	19.64	47	6632	15343	42599313
Hypoglycaemia	88.54	19.64	74	6605	59780	42554876
Cardiac failure	75.14	19.64	88	6591	106768	42507888
Hyperglycaemia	70.50	19.64	58	6621	45801	42568855
Glycosylated haemoglobin increased	66.85	19.64	35	6644	12889	42601767
Lactic acidosis	62.87	19.64	54	6625	45207	42569449
Cerebral infarction	62.17	19.64	46	6633	31123	42583533
Acute kidney injury	53.83	19.64	152	6527	367185	42247471
Pancreatic carcinoma	49.88	19.64	26	6653	9480	42605176
Euglycaemic diabetic ketoacidosis	49.56	19.64	22	6657	5638	42609018
Ketonuria	40.38	19.64	11	6668	653	42614003
Drug interaction	38.52	19.64	110	6569	266889	42347767
Interstitial lung disease	35.40	19.64	52	6627	78410	42536246
Diabetic ketoacidosis	33.73	19.64	28	6651	22339	42592317
Eosinophilia	33.48	19.64	33	6646	32866	42581790
Ketoacidosis	32.03	19.64	16	6663	5336	42609320
Hyperkalaemia	31.60	19.64	50	6629	80408	42534248
Polycythaemia	31.12	19.64	13	6666	2873	42611783
MELAS syndrome	30.47	19.64	6	6673	82	42614574
Bone marrow oedema	28.78	19.64	9	6670	868	42613788
Hyperinsulinaemia	28.52	19.64	6	6673	116	42614540
Orbital oedema	26.13	19.64	6	6673	176	42614480
Intercepted medication error	24.35	19.64	7	6672	506	42614150
Agnosia	23.55	19.64	5	6674	101	42614555
Toxicity to various agents	23.21	19.64	4	6675	229132	42385524
Renal impairment	22.67	19.64	52	6627	110176	42504480
Altered state of consciousness	22.02	19.64	25	6654	29234	42585422
Blister	21.56	19.64	24	6655	27466	42587190
Heart rate abnormal	20.56	19.64	9	6670	2230	42612426
Fatigue	20.40	19.64	23	6656	435618	42179038
Dermatitis bullous	20.34	19.64	14	6665	8442	42606214
Toxic skin eruption	20.31	19.64	17	6662	13713	42600943
Blister rupture	20.20	19.64	5	6674	203	42614453
Urinary tract candidiasis	19.94	19.64	6	6673	509	42614147
Food intolerance	19.69	19.64	8	6671	1648	42613008

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	2074.41	17.71	471	11705	19236	110557887
Lactic acidosis	294.07	17.71	161	12015	92650	110484473
Hypoglycaemia	237.90	17.71	152	12024	115952	110461171
Acute kidney injury	225.34	17.71	311	11865	635119	109942004
Hyperglycaemia	132.42	17.71	94	12082	84996	110492127
Euglycaemic diabetic ketoacidosis	130.99	17.71	49	12127	11574	110565549
Diabetes mellitus inadequate control	129.61	17.71	64	12112	29711	110547412
Glycosylated haemoglobin increased	106.47	17.71	52	12124	23567	110553556
Cerebral infarction	106.35	17.71	68	12108	51770	110525353
Hyperkalaemia	99.61	17.71	97	12079	135699	110441424
Drug interaction	93.72	17.71	184	11992	499999	110077124
Compartment syndrome	85.61	17.71	30	12146	5880	110571243
Ketoacidosis	83.49	17.71	34	12142	10053	110567070
Diabetic ketoacidosis	78.49	17.71	52	12124	42006	110535117
Dermatitis bullous	77.23	17.71	38	12138	17491	110559632
Eosinophilia	76.52	17.71	58	12118	57878	110519245
Cardiac failure	70.84	17.71	95	12081	187531	110389592
Renal impairment	65.98	17.71	92	12084	188353	110388770
Altered state of consciousness	65.94	17.71	53	12123	57573	110519550
Interstitial lung disease	57.93	17.71	74	12102	139260	110437863
Pancreatic carcinoma	50.34	17.71	27	12149	14845	110562278
Polycythaemia	48.88	17.71	17	12159	3258	110573865
Polymyalgia rheumatica	47.51	17.71	20	12156	6422	110570701
Blood glucose increased	45.32	17.71	64	12112	132432	110444691
Crush syndrome	44.43	17.71	10	12166	385	110576738
Thrombocytosis	41.17	17.71	21	12155	10423	110566700
Acetonaemia	40.87	17.71	10	12166	555	110576568
Ketonuria	40.13	17.71	12	12164	1423	110575700
Pain	39.03	17.71	29	12147	954926	109622197
Urine ketone body present	38.94	17.71	15	12161	3831	110573292
Sensorimotor disorder	38.04	17.71	11	12165	1161	110575962
Rhabdomyolysis	38.02	17.71	56	12120	120345	110456778
Joint swelling	37.48	17.71	3	12173	442842	110134281
Blister rupture	37.44	17.71	10	12166	788	110576335
Shock	36.87	17.71	37	12139	53551	110523572
Cardiac failure acute	36.04	17.71	26	12150	24052	110553071
Diabetic metabolic decompensation	35.26	17.71	14	12162	3875	110573248
Fatigue	34.92	17.71	50	12126	1215908	109361215
Pancreatitis acute	33.25	17.71	37	12139	60237	110516886
Hypomagnesaemia	33.21	17.71	37	12139	60333	110516790
Toxic skin eruption	32.94	17.71	26	12150	27489	110549634
Inflammatory marker increased	32.21	17.71	20	12156	14449	110562674
Anaemia	29.67	17.71	129	12047	546957	110030166
Diabetes mellitus	29.62	17.71	45	12131	99336	110477787
Hypersensitivity	28.62	17.71	5	12171	403993	110173130
Metabolic acidosis	28.10	17.71	44	12132	99700	110477423
Cardiac failure chronic	28.01	17.71	18	12158	13793	110563330
Drug hypersensitivity	27.41	17.71	8	12168	454082	110123041
Hypoglycaemic coma	27.40	17.71	13	12163	5520	110571603
Bladder sphincter atony	26.65	17.71	6	12170	231	110576892
Arthralgia	26.61	17.71	28	12148	779604	109797519
Ischaemic stroke	25.68	17.71	27	12149	41236	110535887
Swelling	25.63	17.71	4	12172	351037	110226086
Hyperinsulinaemia	25.51	17.71	6	12170	281	110576842
Language disorder	25.28	17.71	11	12165	3827	110573296
Intentional overdose	25.01	17.71	49	12127	132452	110444671
Acute generalised exanthematous pustulosis	24.93	17.71	20	12156	21644	110555479
Alopecia	24.79	17.71	5	12171	364748	110212375
MELAS syndrome	24.70	17.71	6	12170	323	110576800
Infusion related reaction	24.35	17.71	6	12170	381156	110195967
Contraindication to medical treatment	23.96	17.71	8	12168	1355	110575768
Bone marrow oedema	23.96	17.71	9	12167	2147	110574976
Hyperparathyroidism secondary	23.51	17.71	10	12166	3294	110573829
Hypoparathyroidism	23.06	17.71	8	12168	1522	110575601
Diabetic nephropathy	22.93	17.71	10	12166	3498	110573625
Drug reaction with eosinophilia and systemic symptoms	22.82	17.71	36	12140	82059	110495064
Capillary leak syndrome	22.69	17.71	11	12165	4897	110572226
Anal incontinence	22.60	17.71	19	12157	21945	110555178
Orbital oedema	21.94	17.71	6	12170	517	110576606
Hepatic function abnormal	21.90	17.71	37	12139	89258	110487865
Tachypnoea	21.41	17.71	24	12152	39371	110537752
Cholangitis acute	21.31	17.71	8	12168	1905	110575218
Erythema multiforme	21.19	17.71	18	12158	21079	110556044
Blood triglycerides increased	21.19	17.71	19	12157	23907	110553216
Urinary tract candidiasis	20.93	17.71	7	12169	1192	110575931
Musculoskeletal stiffness	20.85	17.71	3	12173	279819	110297304
Acquired perforating dermatosis	20.73	17.71	3	12173	7	110577116
Agnosia	20.34	17.71	5	12171	283	110576840
Abdominal discomfort	20.26	17.71	9	12167	393849	110183274
Drug ineffective	19.97	17.71	93	12083	1520447	109056676
Neutrophilia	19.82	17.71	13	12163	10316	110566807
Cutaneous lupus erythematosus	19.78	17.71	9	12167	3479	110573644
Angina pectoris	19.69	17.71	29	12147	62266	110514857
Idiopathic pulmonary fibrosis	19.54	17.71	10	12166	4994	110572129
Thyroglobulin increased	19.44	17.71	4	12172	100	110577023
Headache	19.22	17.71	43	12133	882334	109694789
Dehydration	19.20	17.71	71	12105	279440	110297683
Glycosuria	18.84	17.71	8	12168	2622	110574501
Nephrotic syndrome	18.59	17.71	14	12162	13817	110563306
Rheumatoid arthritis	18.59	17.71	5	12171	299608	110277515
Wheezing	18.42	17.71	3	12173	255227	110321896
Maternal exposure during pregnancy	18.38	17.71	3	12173	254880	110322243
Ketosis	18.33	17.71	7	12169	1747	110575376
Peripheral swelling	18.16	17.71	11	12165	404023	110173100

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vildagliptin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

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	D004791	Enzyme Inhibitors
MeSH PA	D007004	Hypoglycemic Agents
MeSH PA	D011480	Protease Inhibitors
MeSH PA	D054873	Dipeptidyl-Peptidase IV Inhibitors
CHEBI has role	CHEBI:35469	antidepressant
CHEBI has role	CHEBI:35526	hypoglycemic agent
CHEBI has role	CHEBI:35610	antineoplastic agent

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
Prolyl endopeptidase FAP	Enzyme	Q12884	SEPR_HUMAN		IC50	5.43	CHEMBL
Dipeptidyl peptidase 8	Enzyme	Q6V1X1	DPP8_HUMAN		Ki	6.09	CHEMBL
Dipeptidyl peptidase 9	Enzyme	Q86TI2	DPP9_HUMAN		Ki	7.17	CHEMBL
Dipeptidyl peptidase 4	Enzyme		DPP4_MOUSE		IC50	7.58	CHEMBL
Dipeptidyl peptidase 9	Enzyme		E1BI31_BOVIN		IC50	6.17	CHEMBL
Dipeptidyl peptidase IV	Enzyme		O31048_PORGN		Ki	7.77	CHEMBL
Prolyl endopeptidase FAP	Enzyme		SEPR_MOUSE		IC50	4.28	CHEMBL

ID	Source
D07080	KEGG_DRUG
C1570906	UMLSCUI
CHEBI:135285	CHEBI
CHEMBL142703	ChEMBL_ID
DB04876	DRUGBANK_ID
D000077597	MESH_DESCRIPTOR_UI
6918537	PUBCHEM_CID
6310	IUPHAR_LIGAND_ID
8399	INN_ID
I6B4B2U96P	UNII
596554	RXNORM
012358	NDDF
428611002	SNOMEDCT_US
428807006	SNOMEDCT_US
LF7	PDB_CHEM_ID
924914-75-0	SECONDARY_CAS_RN
I6B4B2U96P	INXIGHT DRUGS