Vildagliptin

JFDA label: Viltin 50mg

Mechanism of Action

Inhibitor of Dipeptidyl peptidase 4 — Dipeptidyl peptidase IV inhibitor

Target	Action	Gene / class
Dipeptidyl peptidase 4 efficacy	INHIBITOR	DPP4

Indications

Approved

• Diabetes Mellitus — diabetes mellitus
• Diabetes Mellitus, Type 2 — type 2 diabetes mellitus

Off-label

• Breast Neoplasms
• Diabetes Mellitus, Type 1
• Diabetes, Gestational
• Glucose Intolerance
• Prediabetic State

Class profile

mechanismClass	DPP-4 inhibitor
insulinSecretagogue	0
weightEffect	Neutral
hypoglycemiaRisk	None
renalContraindicated	0
cardioProtective	0
renalProtective	0
source	ADA-EASD2023/Maruthur2016

Monitoring

Efficacy	HbA1c every 3 months initially, then every 6–12 months when stable; fasting and post-prandial blood glucose; patient-reported hypoglycaemia episodes
Toxicity	Hypoglycaemia symptoms; eGFR for renally-cleared agents; weight; blood pressure
Clinical pearl	Individualise HbA1c targets based on patient age, comorbidities, and hypoglycaemia risk. Targets of < 7% are appropriate for most patients but < 8% may be safer in frail elderly.
Counseling	Monitor blood glucose regularly. Know how to recognise and treat hypoglycaemia. Keep carbohydrate snacks available.

Chemistry & Properties

Formula	C17H25N3O2
Molecular weight	303.41 g/mol
IUPAC name	(2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
CAS	274901-16-5
PubChem CID	6918537
InChIKey	SYOKIDBDQMKNDQ-XWTIBIIYSA-N
logP	1.17 (XLogP 0.9)
Polar surface area	76.36 Ų
H-bond acceptors / donors	4 / 2
Drug-likeness (QED)	0.82
Lipinski violations	0

SMILES

N#C[C@@H]1CCCN1C(=O)CNC12CC3CC(CC(O)(C3)C1)C2

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability	10.0%
Half-life	1.037 h
Volume of distribution	0.981 L/kg
Protein binding	2.3%
BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP2C19	Substrate	—

Receptor binding (top 4)

Target	Action	Affinity
dipeptidyl peptidase 4 (DPP4)	Inhibitor	pIC50 8.0
dipeptidyl peptidase 4 (DPP4)	Inhibitor	pKi 7.8
dipeptidyl peptidase 9 (DPP9)	Inhibitor	pIC50 6.6
dipeptidyl peptidase 8 (DPP8)	Inhibitor	pIC50 5.7

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)MDR1 (Substrate)P-gp (Substrate)

Registered Products (33)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
VILGLAV	Tablet Vildagliptin 50.000 mg	10 tab	Omicron Pharma	5.090
Viltin	Tablet 50 mg	28 tab pack varies	Pharma International Company/ Jordan	6.520
vildasolin	Tablet 50 mg mg TAB	28 tab	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	6.520
GLEPTAL	Tablet 50 mg	30 tab pack varies	Al-Taqqadom Pharmaceutical Industries	6.980
Glavio	Tablet 50.00 mg	30 tab	United Pharmaceutical	6.980
Glunorm	Tablet 50 mg	30 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	6.980
Iylus	Tablet 50 mg	30 tab pack varies	Savvy Pharma	6.980
VildaRAM	Tablet 50 mg	30 tab pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	6.980
Iylumet	Tablet 1000 mg, 50 mg	30 tab pack varies	Savvy Pharma	7.120
Iylumet	Tablet 500 mg, 50 mg	30 tab pack varies	Savvy Pharma	7.120
Iylumet	Tablet 850 mg, 50 mg	30 tab pack varies	SAVVY PHARMA/JORDAN	7.120
Viltin-Met	Tablet 1000 mg, 50.0 mg	30 tab pack varies	Pharma International Company/ Jordan	7.120
Viltin-Met	Tablet 850.000 mg, 50.00 mg	30 tab pack varies	Pharma International Company/ Jordan	7.120
Galvus	Tablet 50 mg	28 tab	The Jordan Drugstore Co	8.630
Iylus	Tablet 50 mg	60 tab pack varies	Savvy Pharma	11.550
Gleptal Plus	Tablet 850 mg, 50 mg	60 tab	AL-TAQADDOM PHARMACEUTICAL INDUSTRIES/JORDAN	11.830
Gleptal Plus	Tablet 1000 mg, 50 mg	60 tab	AL-TAQADDOM PHARMACEUTICAL INDUSTRIES/JORDAN	11.830
Glunorm	Tablet 50 mg	60 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	12.940
GLEPTAL	Tablet 50 mg	60 tab pack varies	Al-Taqqadom Pharmaceutical Industries	13.260
Viltin	Tablet 50 mg	60 tab pack varies	Pharma International Company/ Jordan	13.270
Glunorm M 50/1000mg F.C Tablet	Film-Coated Tablet 1000 mg, 50 mg	60 tab	Dar Al Dawa Development and Investment Co Ltd/Jordan	13.570
Glunorm M 50/850 mg F.C Tab	Film-Coated Tablet 850 mg, 50 mg	60 tab	Dar Al Dawa Development and Investment Co Ltd/Jordan	13.570
Iylumet	Tablet 500 mg, 50 mg	60 tab pack varies	Savvy Pharma	13.570
Iylumet	Tablet 850 mg, 50 mg	60 tab pack varies	SAVVY PHARMA/JORDAN	13.570
Iylumet	Tablet 1000 mg, 50 mg	60 tab pack varies	Savvy Pharma	13.570
Viltin-Met	Tablet 850.000 mg, 50.00 mg	60 tab pack varies	Pharma International Company/ Jordan	13.570
Viltin-Met	Tablet 1000 mg, 50.0 mg	60 tab pack varies	Pharma International Company/ Jordan	13.570
Galvus Met 850mg/50mg	Tablet 850 mg, 50 mg	60 tab	The Jordan Drugstore Co	16.700
Galvus Met 1000mg/50mg	Tablet 1000 mg, 50 mg	60 tab	The Jordan Drugstore Co	16.700
Galvus met 50/500 F.C tab	Film-Coated Tablet 500 mg, 50 mg	60 tab	The Jordan Drugstore Co	17.620
Viltin	Tablet 50 mg	500 tab pack varies	Pharma International Company/ Jordan	101.200
GLEPTAL	Tablet 50 mg	1000 tab pack varies	Al-Taqqadom Pharmaceutical Industries	197.770
VildaRAM	Tablet 50 mg	1000 tab pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	197.770