Teneligliptin

Teneligliptin
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
Clinical data
Trade names	Tenelia
Legal status	Approved in Japan
Identifiers
CAS Number	760937-92-6
PubChem	CID 11949652
ChemSpider	10123963
Chemical data
Formula	C₂₂H₃₀N₆OS
Molar mass	426.58 g/mol
SMILES CC1=NN(C(=C1)N2CCN(CC2)[C@H]3C[C@H](NC3)C(=O)N4CCSC4)C5=CC=CC=C5
InChI 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 Key:WGRQANOPCQRCME-PMACEKPBSA-N

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]

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

It is approved for use in Japan 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.

Teneligliptin significantly controls glycemic parameters 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, and J. Robert Merritt. "Teneligliptin (Antidiabetic)". Annual Reports in Medicinal Chemistry 48: 523–524. doi:10.1016/b978-0-12-417150-3.00028-4. |chapter= ignored (help)
↑ 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)

Insulin

Sensitizers

Biguanides	Metformin^# Buformin<sp>‡ Phenformin^‡

TZDs/"glitazones" (PPAR)	Ciglitazone^§ Darglitazone^§ Englitazone^§ Lobeglitazone Netoglitazone^§ Pioglitazone Rivoglitazone^† Rosiglitazone Troglitazone^‡

Dual PPAR agonists	Aleglitazar^† Muraglitazar^§ Saroglitazar Tesaglitazar^§

Secretagogues

K+ ATP

Sulfonylureas	1st generation: Acetohexamide Carbutamide Chlorpropamide Metahexamide Tolbutamide Tolazamide 2nd generation: Glibenclamide (Glyburide)^# Glibornuride Glicetanile Gliclazide Gliflumide Glipizide Gliquidone Glisoxepide Glyclopyramide Glimepiride

Meglitinides/"glinides"	Nateglinide Repaglinide Mitiglinide

GLP-1 agonists

DPP-4 inhibitors

GPR40 Free fatty acid receptor 1

Fasiglifam^†

Analogs/other insulins

fast-acting (Insulin lispro
Insulin aspart
Insulin glulisine)
short-acting (Regular insulin)
long-acting (Insulin glargine
Insulin detemir
NPH insulin)
ultra-long-acting (Insulin degludec^†)
inhalable Exubera^‡
Afrezza

Other

Aldose reductase inhibitors	Epalrestat Fidarestat^§ Ranirestat^† Tolrestat^‡ Zenarestat^§

Alpha-glucosidase inhibitors	Acarbose Miglitol Voglibose

Amylin analog	Pramlintide

Sodium glucose transporter (SGLT2) inhibitors	Canagliflozin Dapagliflozin Empagliflozin Remogliflozin^§ Sergliflozin^§ Tofogliflozin^†

Other	Benfluorex^‡ Bromocriptine

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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