Vildagliptin
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Vildagliptin
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CAS No:
274901-16-5
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Formula:
C17H25N3O2
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Chemical Name:
Vildagliptin
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Synonyms:
2-Pyrrolidinecarbonitrile,1-[2-[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-,(2S)-;2-Pyrrolidinecarbonitrile,1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-,(2S)-;(2S)-1-[2-[(3-Hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-2-pyrrolidinecarbonitrile;Vildagliptin;LAF 237;NVP-LAF 237;Galvus;Equa;DSP 7238;(S)-1-[2-[(3-Hydroxyadamant-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile;(2S)-1-[2-[(3-Hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile;Xiliarx;Jalra;565453-38-5
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Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs
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CAS No:
Description
Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.IC50 Value: 2.3 nM[1]Target: DPP-4in vitro: Vildagliptin is an N-substituted glycyl-2-cyanopyrrolidine (figure 2). It is a potent competitive and reversible inhibitor of human and rodent DPP-4 in vitro, with a median inhibitory concentration (IC50) ~2-3 nmol/L. Importantly, vildagliptin inhibits DPP-4 with high specificity relative to other similar peptidases where its IC50 exceeds 200 mol/L [1].in vivo: Compared to a
A pyrrolidine-carbonitrile derivative and potent inhibitor of DIPEPTIDYL PEPTIDASE 4 that is used in the treatment of TYPE 2 DIABETES MELLITUS.
Vildagliptin Basic Attributes
303.39900
303.40
A10BH02|A10BD08|A - Alimentary tract and metabolism
2933990090
Characteristics
76.36000
1.50308
white crystalline powder
1.27 g/cm3
148-150 °C @ Solvent: Ethyl acetate, Isopropanol
531.3ºC at 760 mmHg
275.1ºC
Safety Information
24/25-26-28-36/37/39
|Danger|H300 (12.5%): Fatal if swallowed [Danger Acute toxicity, oral]|P201, P202, P260, P261, P264, P270, P271, P273, P280, P281, P301+P310, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P308+P313, P310, P312, P314, P321, P322, P330, P332+P313, P362, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 17 companies from 8 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Drug Information
Vildagliptin is indicated as an adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes mellitus:as monotherapy in patients in whom metformin is inappropriate due to contraindications or intolerance.in combination with other medicinal products for the treatment of diabetes, including insulin, when these do not provide adequate glycaemic control|Vildagliptin is indicated as an adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes mellitus:as monotherapy in patients in whom metformin is inappropriate due to contraindications or intolerance.in combination with other medicinal products for the treatment of diabetes, including insulin, when these do not provide adequate glycaemic control (see sections 4.4, 4.5 and 5.1 for available data on different combinations).|Eucreas is indicated as an adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes mellitus:in patients who are inadequately controlled with metformin hydrochloride alone.in patients who are already being treated with the combination of vildagliptin and metformin hydrochloride, as separate tablets.in combination with other medicinal products for the treatment of diabetes, including insulin, when these do not provide adequate glycaemic control|Zomarist is indicated as an adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes mellitus:in patients who are inadequately controlled with metformin hydrochloride alone.in patients who are already being treated with the combination of vildagliptin and metformin hydrochloride, as separate tablets.in combination with other medicinal products for the treatment of diabetes, including insulin, when these do not provide adequate.|Icandra is indicated as an adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes mellitus:in patients who are inadequately controlled with metformin hydrochloride alone.in patients who are already being treated with the combination of vildagliptin and metformin hydrochloride, as separate tablets.in combination with other medicinal products for the treatment of diabetes, including insulin, when these do not provide adequate glycaemic control (see sections 4.4, 4.5 and 5.1 for available data on different combinations).|Treatment of type II diabetes mellitus
Compounds that suppress the degradation of INCRETINS by blocking the action of DIPEPTIDYL-PEPTIDASE IV. This helps to correct the defective INSULIN and GLUCAGON secretion characteristic of TYPE 2 DIABETES MELLITUS by stimulating insulin secretion and suppressing glucagon release. (See all compounds classified as Dipeptidyl-Peptidase IV Inhibitors.)|Substances which lower blood glucose levels. (See all compounds classified as Hypoglycemic Agents.)
(2S)-(((3-hydroxyadamantan-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile
Vildagliptin Use and Manufacturing
Vildagliptin (previously LAF237, trade names Galvus, Zomelis,) is an 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 glucagon release by the alpha cells of the islets of Langerhans in the pancreas.Vildagliptin has been shown to reduce hyperglycemia in type 2 diabetes mellitus.
Human drugs -> Galvus -> EMA Drug Category|Drugs used in diabetes -> Human pharmacotherapeutic group|Human drugs -> Xiliarx -> EMA Drug Category|Human drugs -> Eucreas -> EMA Drug Category|Drugs used in diabetes, Combinations of oral blood glucose lowering drugs -> Human pharmacotherapeutic group|Human drugs -> Zomarist -> EMA Drug Category|Human drugs -> Icandra (previously Vildagliptin / metformin hydrochloride Novartis) -> EMA Drug Category|Human drugs -> Jalra -> EMA Drug Category|Drugs used in diabetes, Dipeptidyl peptidase 4 (DPP-4) inhibitors -> Human pharmacotherapeutic group|Human Drugs -> EU pediatric investigation plans
Computed Properties
Molecular Weight:303.4
XLogP3:0.9
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:3
Exact Mass:303.19467705
Monoisotopic Mass:303.19467705
Topological Polar Surface Area:76.4
Heavy Atom Count:22
Complexity:523
Defined Atom Stereocenter Count:3
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
Drug Function and Efficacy
Selective dipeptidyl peptidase-4 (DPP-4) inhibitors can quickly and completely inhibit DPP-4 activity, increase the content of endogenous incretin GLP-1 and GIP, and regulate insulin and glucagon secretion to lower blood sugar by increasing the sensitivity of β-cells to glucose and increasing the content of endogenous GLP-1.
Registered Holders
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INNOVARE LABS PRIVATE LTD
Active
United States
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MANKIND PHARMA LTD
Active
United States
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OPTIMUS DRUGS PRIVATE LTD
Active
United States
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