Vildagliptin hydrochloride

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C17H25N3O2.ClH
Molecular Weight	339.86
Optical Activity	( - )
Defined Stereocenters	1 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.OC12CC3CC(C1)CC(C3)(C2)NCC(=O)N4CCC[C@H]4C#N

InChI

InChIKey=RZUUYWHYKBKAGN-DNSMMRBLSA-N

InChI=1S/C17H25N3O2.ClH/c18-9-14-2-1-3-20(14)15(21)10-19-16-5-12-4-13(6-16)8-17(22,7-12)11-16;/h12-14,19,22H,1-8,10-11H2;1H/t12?,13?,14-,16?,17?;/m0./s1

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

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

Molecular Formula	C17H25N3O2
Molecular Weight	303.3993
Charge	0
Count

Stereochemistry	MIXED
Additional Stereochemistry	No
Defined Stereocenters	1 / 3
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000771/WC500020327.pdf
Curator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB04876

Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucaon release by the alpha cells of the islets of Langerhans in the pancreas. It is currently in clinical trials in the U.S. and has been shown to reduce hyperglycemia in type 2 diabetes mellitus. While the drug is still not approved for use in the US, it was approved in Feb 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions. Vildagliptin is marketed under the trade names Galvus, Zomelis.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dipeptidyl peptidase IV 37 Target ID: CHEMBL284 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000771/WC500020327.pdf	Inhibitor 8504		62.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000771/WC500020327.pdf	Primary		Approved 8583	Galvus Approved Use Vildagliptin is indicated in the treatment of type 2 diabetes mellitus in adults Launch Date 2007

C_max

Value	Dose	Analyte	Population
162 ng/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
272 ng/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
671 ng/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1959 ng/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2860 ng/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
524 ng/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	50 mg 2 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
415 ng/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	50 mg 2 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
538 ng/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
431 ng/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
675 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
497 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
512 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
632 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
545 ng × h/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1139 ng × h/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2968 ng × h/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6857 ng × h/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
13420 ng × h/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1480 ng × h/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	50 mg 2 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1490 ng × h/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	50 mg 2 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2500 ng × h/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2215 ng × h/mL EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
2567 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2076 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2411 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3322 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
1.54 h EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.77 h EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.1 h EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2 h EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.29 h EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=36	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.78 h EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	50 mg 2 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.41 h EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	50 mg 2 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.1 h EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.9 h EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=37	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED
2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2010/P201000008/30024200_22200AMX00233_A100_5.pdf#page=50 \| https://pubmed.ncbi.nlm.nih.gov/17486328/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VILDAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
90.7% EXPERIMENT https://www.info.pmda.go.jp/go/interview/1/300242_3969011F1020_1_EQA_1F.pdf#page=40			VILDAGLIPTIN plasma	Homo sapiens

Doses

Dose	Population	Adverse events
400 mg 1 times / day multiple, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/21609207/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/21609207/	Sources: https://pubmed.ncbi.nlm.nih.gov/21609207/
100 mg 1 times / day multiple, oral Recommended Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17373638/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17373638/	Sources: https://pubmed.ncbi.nlm.nih.gov/17373638/

PubMed

Title	Date	PubMed
The effect of age, gender, and body mass index on the pharmacokinetics and pharmacodynamics of vildagliptin in healthy volunteers.	2008-03	17961192
Effects of the dipeptidyl peptidase-IV inhibitor vildagliptin on incretin hormones, islet function, and postprandial glycemia in subjects with impaired glucose tolerance.	2008-01	17947341
Characterization of the influence of vildagliptin on model-assessed -cell function in patients with type 2 diabetes and mild hyperglycemia.	2008-01	17925336
The dipeptidyl peptidase-4 inhibitor vildagliptin improves beta-cell function and insulin sensitivity in subjects with impaired fasting glucose.	2008-01	17909087
Evaluation of the potential for steady-state pharmacokinetic interaction between vildagliptin and simvastatin in healthy subjects.	2007-12	17931461
Management of type 2 diabetes in treatment-naive elderly patients: benefits and risks of vildagliptin monotherapy.	2007-12	17878242
Incretin receptors for glucagon-like peptide 1 and glucose-dependent insulinotropic polypeptide are essential for the sustained metabolic actions of vildagliptin in mice.	2007-12	17717280
The dipeptidyl peptidase 4 inhibitor vildagliptin does not accentuate glibenclamide-induced hypoglycemia but reduces glucose-induced glucagon-like peptide 1 and gastric inhibitory polypeptide secretion.	2007-11	17698900
DPP-4 inhibition improves glucose tolerance and increases insulin and GLP-1 responses to gastric glucose in association with normalized islet topography in mice with beta-cell-specific overexpression of human islet amyloid polypeptide.	2007-10-04	17482289
Dipeptidyl peptidase 4 (DPP-4) inhibitors and their role in Type 2 diabetes management.	2007-09-13	17848846
Vildagliptin was effective as add-on therapy in type 2 diabetes inadequately controlled with metformin monotherapy.	2007-09-04	17764138
The DPP-4 inhibitor vildagliptin: robust glycaemic control in type 2 diabetes and beyond.	2007-09	17877545
Incretin-based treatment of type 2 diabetes: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors.	2007-09	17877544
Dose proportionality and the effect of food on vildagliptin, a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers.	2007-09	17656620
Comparison between vildagliptin and metformin to sustain reductions in HbA(1c) over 1 year in drug-naïve patients with Type 2 diabetes.	2007-09	17509069
Evaluation of pharmacokinetic interactions between vildagliptin and digoxin in healthy volunteers.	2007-08	17660482
Dipeptidyl peptidase IV inhibitors and the incretin system in type 2 diabetes mellitus.	2007-08	17655515
Dipeptidyl peptidase 4 inhibition and vildagliptin therapy for type 2 diabetes.	2007-08	17593276
Antihyperglycaemic therapy in elderly patients with type 2 diabetes: potential role of incretin mimetics and DPP-4 inhibitors.	2007-08	17593275
Antidiabetic medications in overweight/obese patients with type 2 diabetes: drawbacks of current drugs and potential advantages of incretin-based treatment on body weight.	2007-08	17593274
Does addition of vildagliptin to metformin monotherapy improve glycemic control in patients with type 2 diabetes mellitus?	2007-08	17549095
Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis.	2007-07-11	17622601
A review of the effects of antihyperglycaemic agents on body weight: the potential of incretin targeted therapies.	2007-07	17559747
[New concepts in the treatment of type 2 diabetes].	2007-07	17541529
The influence of hepatic impairment on the pharmacokinetics of the dipeptidyl peptidase IV (DPP-4) inhibitor vildagliptin.	2007-07	17486328
Vildagliptin: a novel oral therapy for type 2 diabetes mellitus.	2007-06	17563048
Which patients are candidates for dipeptidyl peptidase IV inhibitors?	2007-06	17563046
Addition of vildagliptin to insulin improves glycaemic control in type 2 diabetes.	2007-06	17387446
Dipeptidyl peptidase-4 inhibitors: clinical data and clinical implications.	2007-06	17337494
New treatments for diabetes.	2007-05-24	17522409
Vildagliptin was noninferior to rosiglitazone for glycemic control in type 2 diabetes but caused less weight gain.	2007-05-04	17474683
Effect of the novel oral dipeptidyl peptidase IV inhibitor vildagliptin on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects.	2007-05	17519080
The role of vildagliptin in the management of type 2 diabetes mellitus.	2007-05	17456545
Pharmacodynamics of vildagliptin in patients with type 2 diabetes during OGTT.	2007-05	17442688
Effects of dipeptidyl peptidase-4 inhibition on gastrointestinal function, meal appearance, and glucose metabolism in type 2 diabetes.	2007-05	17303799
[Incretin enhancers, incretin mimetics: from therapeutic concept to clinical application].	2007-04-01	17383951
Dipeptidyl peptidase-4 inhibitors and the management of type 2 diabetes mellitus.	2007-04	17940427
[Glucagon-like peptide-1 (GLP-1), new target for the treatment of type 2 diabetes].	2007-04	17566392
Gateways to clinical trials.	2007-04	17520107
Inhibition of DPP-4: a new therapeutic approach for the treatment of type 2 diabetes.	2007-04	17407649
beta-cell failure in diabetes and preservation by clinical treatment.	2007-04	17353295
Gateways to clinical trials.	2007-03-09	17344945
Vildagliptin in drug-naïve patients with type 2 diabetes: a 24-week, double-blind, randomized, placebo-controlled, multiple-dose study.	2007-03	17373638
Efficacy and tolerability of initial combination therapy with vildagliptin and pioglitazone compared with component monotherapy in patients with type 2 diabetes.	2007-03	17300593
Incretins: a new treatment option for type 2 diabetes?	2007-02	17379930
The absolute oral bioavailability and population-based pharmacokinetic modelling of a novel dipeptidylpeptidase-IV inhibitor, vildagliptin, in healthy volunteers.	2007	17713976
Pharmacokinetics and pharmacodynamics of vildagliptin in patients with type 2 diabetes mellitus.	2007	17596103
Review of sitagliptin phosphate: a novel treatment for type 2 diabetes.	2007	17580730
11 Years of cyanopyrrolidines as DPP-IV inhibitors.	2007	17352679
New therapeutic strategies for the treatment of type 2 diabetes mellitus based on incretins.	2005	17491680

Patents

Sample Use Guides

In Vivo Use Guide

When used as monotherapy, in combination with metformin, in combination with thiazolidinedione, in combination with metformin and a sulphonylurea, or in combination with insulin (with or without metformin), the recommended daily dose of vildagliptin is 100 mg, administered as one dose of 50 mg in the morning and one dose of 50 mg in the evening. When used in dual combination with a sulphonylurea, the recommended dose of vildagliptin is 50 mg once daily administered in the morning. In this patient population, vildagliptin 100 mg daily was no more effective than vildagliptin 50 mg once daily.

Route of Administration: Oral

In Vitro Use Guide

Vildagliptin inhibited rat plasma DPP-IV activity in vitro with an IC(50) value of 2.12 nmol/l

Substance Class	Chemical Created by `admin` on `Wed Apr 02 13:19:37 GMT 2025` Edited by `admin` on `Wed Apr 02 13:19:37 GMT 2025`
Record UNII	9KND64V2AA
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

Vildagliptin hydrochloride [WHO-DD]

Preferred Name

English

Vildagliptin hydrochloride

Common Name

English

2-Pyrrolidinecarbonitrile, 1-[2-[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-, hydrochloride (1:1), (2S)-

Systematic Name

English

(2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile hydrochloride

Systematic Name

English

Code System Code Type Description

PUBCHEM

16070539

Created by admin on Wed Apr 02 13:19:37 GMT 2025 , Edited by admin on Wed Apr 02 13:19:37 GMT 2025

PRIMARY

CAS

924914-75-0

Created by admin on Wed Apr 02 13:19:37 GMT 2025 , Edited by admin on Wed Apr 02 13:19:37 GMT 2025

PRIMARY

SMS_ID

300000037391

Created by admin on Wed Apr 02 13:19:37 GMT 2025 , Edited by admin on Wed Apr 02 13:19:37 GMT 2025

PRIMARY

FDA UNII

9KND64V2AA

Created by admin on Wed Apr 02 13:19:37 GMT 2025 , Edited by admin on Wed Apr 02 13:19:37 GMT 2025

PRIMARY

Related Record Type Details


					I6B4B2U96P

Vildagliptin

PARENT -> SALT/SOLVATE

Amount:

Details

SMILES

InChI

DescriptionSources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000771/WC500020327.pdfCurator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB04876

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

PubMed

Patents

Sample Use Guides

Description
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000771/WC500020327.pdf
Curator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB04876

C_max

T_1/2

F_unbound