リナグリプチン
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/08/02 17:00:14」(JST)
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Linagliptin
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| Systematic (IUPAC) name |
|
8-[(3R)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3- methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
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| Clinical data |
| Trade names |
Tradjenta, Trajenta |
| AHFS/Drugs.com |
Consumer Drug Information |
| MedlinePlus |
a611036 |
| License data |
- EU EMA: Trajenta
- US FDA: Linagliptin
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Pregnancy
category |
- US: B (No risk in non-human studies)
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Routes of
administration |
Oral |
| Legal status |
| Legal status |
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| Pharmacokinetic data |
| Bioavailability |
30% oral |
| Protein binding |
75% to 99% in plasma |
| Identifiers |
| CAS Number |
668270-12-0 Y |
| ATC code |
A10BH05 (WHO) |
| PubChem |
CID 10096344 |
| IUPHAR/BPS |
6318 |
| ChemSpider |
8271879 N |
| UNII |
3X29ZEJ4R2 Y |
| KEGG |
D09566 Y |
| ChEMBL |
CHEMBL237500 N |
| Chemical data |
| Formula |
C25H28N8O2 |
| Molar mass |
472.54 g/mol |
SMILES
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CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
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InChI
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InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1 N
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Key:LTXREWYXXSTFRX-QGZVFWFLSA-N N
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| NY (what is this?) (verify) |
Linagliptin (BI-1356, trade names Tradjenta (US), Trajenta (worldwide)) is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes.
Linagliptin (once-daily) was approved by the U.S. Food and Drug Administration (FDA) on 2 May 2011 for treatment of type II diabetes.[1] It is being marketed by Boehringer Ingelheim and Lilly.
Contents
- 1 Medical uses
- 2 Side effects
- 3 Mechanism of action
- 4 See also
- 5 References
- 6 External links
Medical uses
Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.[2]
Side effects
They may cause severe joint pain.[3]
Mechanism of action
See also
References
- H. Spreitzer (September 1, 2008). "Neue Wirkstoffe - BI-1356". Österreichische Apothekerzeitung (in German) (18/2008): 918.
- Wang, Y, Serradell, N, Rosa, E, Castaner, R (2008). "BI-1356". Drugs of the Future 33 (6): 473–477. doi:10.1358/dof.2008.033.06.1215244.
- ^ "FDA Approves Type 2 Diabetes Drug from Boehringer Ingelheim and Lilly". 3 May 2011.
- ^ "Four Phase III Trials Confirm Benefits of BI’s Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010.
- ^ "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". FDA. 2015-08-28. Retrieved 1 September 2015.
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Oral anti-diabetic drugs, insulins and insulin analogs, and other drugs used in diabetes (A10)
|
|
| Insulin |
| Sensitizers |
| Biguanides |
- Buformin‡
- Metformin#
- Phenformin‡
|
|
| 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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|
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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
|
|
| Meglitinides/"glinides" |
- Mitiglinide
- Nateglinide
- Repaglinide
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|
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| GLP-1 agonists |
- Albiglutide†
- Dulaglutide
- Exenatide
- Liraglutide
- Lixisenatide
- Semaglutide†
- Taspoglutide†
|
|
| 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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|
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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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|
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-
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
External links
|
Wikimedia Commons has media related to Linagliptin. |
- Tradjenta official website (United States)
- Trajenta (Australia)
- Trajenta (Canada)
- Trajenta (European Union)
- Trajenta (India)
UpToDate Contents
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English Journal
- Dipeptidyl peptidase-4 inhibitor use in patients with type 2 diabetes and cardiovascular disease or risk factors.
- Ryan G1.
- Postgraduate medicine.Postgrad Med.2015 Oct 5:1-13. [Epub ahead of print]
- OBJECTIVES: Management of cardiovascular (CV) risk is an essential aspect of diabetes care, and acceptable CV risk is a requirement for antidiabetes medications. Dipeptidyl peptidase-4 (DPP-4) inhibitors effectively reduce glycated hemoglobin, with a low risk of hypoglycemia and weight gain. The pur
- PMID 26436470
- Synthesis, Biological Evaluation and Molecular Docking of (R)-2-((8-(3-aminopiperidin-1-yl)-3-methyl-7-(3-methylbut-2-en-1-yl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-1-yl)methyl)benzonitrile as Dipeptidyl Peptidase IV Inhibitors.
- Ran Y1, Pei H1, Shao M1, Chen L1.
- Chemical biology & drug design.Chem Biol Drug Des.2015 Oct 1. doi: 10.1111/cbdd.12663. [Epub ahead of print]
- Type 2 diabetes (T2D) is classified as a major metabolic disorder, which has affected approximately 194 million people worldwide. DPP-IV inhibitors as a new therapy have shown several advantages over traditional anti-diabetic drugs. Based on the similar binding modes of Alogliptin and Linagliptin, m
- PMID 26426933
- Clinical pharmacology of dipeptidyl peptidase 4 inhibitors indicated for the treatment of type 2 diabetes mellitus.
- Chen XW1, He ZX2, Zhou ZW3, Yang T4, Zhang X5, Yang YX6, Duan W7, Zhou SF2,3.
- Clinical and experimental pharmacology & physiology.Clin Exp Pharmacol Physiol.2015 Oct;42(10):999-1024. doi: 10.1111/1440-1681.12455.
- Dipeptidyl peptidase-4 (DPP-4) inhibitors are a class of oral antidiabetic drugs that improve glycaemic control without causing weight gain or increasing hypoglycaemic risk in patients with type 2 diabetes mellitus (T2DM). The eight available DPP-4 inhibitors, including alogliptin, anagliptin, gemig
- PMID 26173919
Japanese Journal
- DPP-4阻害薬リナグリプチン(トラゼンタ^【○!R】)の薬理学的特性および臨床成績
- 大村 剛史,林 直之,Jeffrey Encinas
- 日本薬理學雜誌 = Folia pharmacologica Japonica 139(4), 174-183, 2012-04-01
- リナグリプチン（トラゼンタ®）は，ジペプチジルペプチダーゼ-4（DPP-4）に対して選択性が高く，長時間持続性の強力なDPP-4阻害薬である．In vitro試験において，リナグリプチンは競合的であり，かつ可逆的にヒトDPP-4を阻害する．DPP-4を高発現させたCaCo-2細胞抽出物中の膜結合型DPP-4に対して阻害作用（IC50=1 nM）を示し，ヒトの血漿中においても同様の阻害活性（IC50 …
- NAID 10030572578
- 新薬レビュー Linagliptin(リナグリプチン) : トラゼンタ錠 日本ベーリンガーインゲルハイム 日本イーライリリー
Related Pictures
★リンクテーブル★
[★]
- 英
- linagliptin
- 商
- トラゼンタ
- 関
- 糖尿病用剤
- トラゼンタ(日本ベーリンガーインゲルハイム、日本イーライリリー)は胆汁排泄型であるため、腎機能による減量は不要らしいが。