テネリグリプチン
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/09/05 04:18:25」(JST)
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Teneligliptin
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Systematic (IUPAC) name |
{(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl}(1,3-thiazolidin-3-yl)methanone
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Clinical data |
Trade names |
Tenelia |
Legal status |
Legal status |
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Identifiers |
CAS Number |
760937-92-6 |
PubChem |
CID 11949652 |
ChemSpider |
10123963 |
Chemical data |
Formula |
C22H30N6OS |
Molar mass |
426.58 g/mol |
SMILES
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CC1=NN(C(=C1)N2CCN(CC2)[C@H]3C[C@H](NC3)C(=O)N4CCSC4)C5=CC=CC=C5
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InChI
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InChI=1S/C22H30N6OS/c1-17-13-21(28(24-17)18-5-3-2-4-6-18)26-9-7-25(8-10-26)19-14-20(23-15-19)22(29)27-11-12-30-16-27/h2-6,13,19-20,23H,7-12,14-16H2,1H3/t19-,20-/m0/s1
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Key:WGRQANOPCQRCME-PMACEKPBSA-N
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Teneligliptin (INN; trade name Tenelia) is a pharmaceutical drug for the treatment of type 2 diabetes mellitus. It belongs to the class of anti-diabetic drugs known as dipeptidyl peptidase-4 inhibitors or "gliptins".[1]
Contents
- 1 Creation
- 2 Licensing and use
- 3 Pharmacology
- 4 References
Creation
It was created by Mitsubishi Tanabe Pharma and launched in September 2012 by both Mitsubishi Tanabe Pharma and Daiichi Sankyo in Japan.[2]
Licensing and use
Japan/Korea
It is approved for use in Japan, Korea and India. [3]
Pharmacology
Teneligliptin has unique J shaped or anchor locked domain structure because of which it has more potent inhibition of DPP 4 enzyme as compared to Sitagliptin and Vildagliptin.[citation needed]
Teneligliptin significantly controls glycemic parameters[clarification needed] with safety. No dose adjustment is required in renally impaired patients.[4]
References
- ^ Kishimoto, M (2013). "Teneligliptin: A DPP-4 inhibitor for the treatment of type 2 diabetes". Diabetes, metabolic syndrome and obesity : targets and therapy. 6: 187–95. doi:10.2147/DMSO.S35682. PMC 3650886. PMID 23671395.
- ^ http://www.daiichisankyo.com/media_investors/media_relations/press_releases/detail/006054.html
- ^ Joanne Bronson; Amelia Black; T. G. Murali Dhar; Bruce A. Ellsworth; J. Robert Merritt. "Teneligliptin (Antidiabetic), Chapter: To Market, To Market - 2012". Annual Reports in Medicinal Chemistry. 48: 523–524. doi:10.1016/b978-0-12-417150-3.00028-4.
- ^ Biochemical and Biophysical Research Communications, 2013, 434(2), 191-196
Oral anti-diabetic drugs, insulins and insulin analogs, and other drugs used in diabetes (A10)
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Insulin |
Sensitizers |
Biguanides |
- Buformin‡
- Metformin#
- Phenformin‡
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TZDs/"glitazones" (PPAR) |
- Ciglitazone§
- Darglitazone§
- Englitazone§
- Lobeglitazone
- Netoglitazone§
- Pioglitazone
- Rivoglitazone†
- Rosiglitazone
- Troglitazone‡
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Dual PPAR agonists |
- Aleglitazar†
- Muraglitazar§
- Saroglitazar
- Tesaglitazar§
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Secretagogues |
K+ATP |
Sulfonylureas |
- 1st generation: Acetohexamide
- Carbutamide
- Chlorpropamide
- Glycyclamide
- Metahexamide
- Tolazamide
- Tolbutamide
- 2nd generation: Glibenclamide (glyburide)#
- Glibornuride
- Glicaramide
- Gliclazide
- Glimepiride
- Glipizide
- Gliquidone
- Glisoxepide
- Glyclopyramide
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Meglitinides/"glinides" |
- Mitiglinide
- Nateglinide
- Repaglinide
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GLP-1 agonists |
- Albiglutide†
- Dulaglutide
- Exenatide
- Liraglutide
- Lixisenatide
- Semaglutide†
- Taspoglutide†
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DPP-4 inhibitors/"gliptins" |
- Alogliptin
- Anagliptin
- Gemigliptin
- Linagliptin
- Omarigliptin
- Saxagliptin
- Sitagliptin
- Teneligliptin
- Vildagliptin
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Free fatty acid receptor 1 (GPR40) |
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Analogs/other insulins |
- fast-acting (Insulin aspart
- Insulin glulisine
- Insulin lispro)
- short-acting (Regular insulin)
- long-acting (Insulin detemir
- Insulin glargine
- NPH insulin)
- ultra-long-acting (Insulin degludec)
- inhalable (Exubera‡
- Afrezza)
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Other |
Aldose reductase inhibitors |
- Epalrestat
- Fidarestat§
- Ranirestat†
- Tolrestat‡
- Zenarestat§
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Alpha-glucosidase inhibitors |
- Acarbose
- Miglitol
- Voglibose
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Amylin analog |
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Sodium glucose transporter (SGLT2) inhibitors |
- Canagliflozin
- Dapagliflozin
- Empagliflozin
- Remogliflozin§
- Sergliflozin§
- Tofogliflozin†
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Other |
- Benfluorex‡
- Bromocriptine
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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English Journal
- Teneligliptin Prevents Cardiomyocyte Hypertrophy, Fibrosis, and Development of Hypertensive Heart Failure in Dahl Salt-Sensitive Rats.
- Yamamoto M1, Ishizu T2, Seo Y1, Suto Y3, Sai S1, Xu D1, Murakoshi N1, Kimura T4, Kawakami Y4, Aonuma K1.
- Journal of cardiac failure.J Card Fail.2017 Sep 6. pii: S1071-9164(17)31163-6. doi: 10.1016/j.cardfail.2017.09.001. [Epub ahead of print]
- PMID 28888840
- A validated UHPLC-QTOF-MS method for quantification of metformin and teneligliptin in rat plasma: Application to pharmacokinetic interaction study.
- Paul D1, Allakonda L1, Satheeshkumar N2.
- Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2017 Sep 5;143:1-8. doi: 10.1016/j.jpba.2017.05.026. Epub 2017 May 15.
- PMID 28544884
- Network meta-analysis of liraglutide versus dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes in Japanese patients.
- Ayers D1, Kanters S1,2, Goldgrub R1, Hughes M1, Kato R3, Kragh N4.
- Current medical research and opinion.Curr Med Res Opin.2017 Sep;33(9):1653-1661. doi: 10.1080/03007995.2017.1345730. Epub 2017 Jul 19.
- PMID 28635331
Japanese Journal
- Teneligliptin improves glycemic control with the reduction of postprandial insulin requirement in Japanese diabetic patients
- Retraction: 糖尿病血液透析患者に対する新規DPP-4阻害薬テネリグリプチンの有用性
- Teneligliptin improves glycemic control with the reduction of postprandial insulin requirement in Japanese diabetic patients
Related Links
- ChemicalBook あなたのためにTeneligliptin(760937-92-6)の化学的性質を提供して、融点、価格、蒸気圧、沸点、毒性、比重、沸点、密度、分子式、分子量、物理的な性質、毒性 税関のコードなどの情報、同時にあなたは更にTeneligliptin ...
- Online Database of Chemicals from Around the World Search | Submit | Advertising | chemBlink >> Chemical Listing >> T >> Teneligliptin Share this page: Teneligliptin List of Suppliers
Related Pictures
★リンクテーブル★
[★]
- 英
- teneligliptin
- 化
- テネリグリプチン臭化水素酸塩水和物 teneligliptin hydrobromide hydrate
- 商
- テネリア Tenelia、カナリア配合(カナグリフロジンとの合剤)
- 関
- 糖尿病用剤。ジペプチジルペプチダーゼ4阻害薬
- 規格20mg錠(直径7.1mm,厚さ3.1mm)、40mg錠(直径8.6mm,厚さ4.5mm)
- 粉砕可能(遮光で50日間保存可能、苦みあり)