Teneligliptin

Teneligliptin
Clinical data
Trade names	Tenelia
ATC code	None;
Legal status
Legal status	Approved in Japan;
Identifiers
	IUPAC name {(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl}(1,3-thiazolidin-3-yl)methanone;
CAS Number	760937-92-6;
PubChem CID	11949652;
ChemSpider	10123963;
UNII	28ZHI4CF9C;
CompTox Dashboard (EPA)	DTXSID30997419 ;
Chemical and physical data
Formula	C22H30N6OS
Molar mass	426.58 g·mol−1
3D model (JSmol)	Interactive image;
	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/Korea/India/Argentina

It is approved for use in Japan, Argentina, Korea and India.[3]

Pharmacology

Teneligliptin has unique J shaped or anchor locked domain structure because of which it has a potent inhibition of DPP 4 enzyme.

Teneligliptin significantly controls glycemic parameters with safety. No dose adjustment is required in renally impaired patients.[4]

gollark: \@everyone

gollark: Go(lang) = bad.

gollark: ``` [...] MIPS is short for Millions of Instructions Per Second. It is a measure for the computation speed of a processor. Like most such measures, it is more often abused than used properly (it is very difficult to justly compare MIPS for different kinds of computers). BogoMips are Linus's own invention. The linux kernel version 0.99.11 (dated 11 July 1993) needed a timing loop (the time is too short and/or needs to be too exact for a non-busy-loop method of waiting), which must be calibrated to the processor speed of the machine. Hence, the kernel measures at boot time how fast a certain kind of busy loop runs on a computer. "Bogo" comes from "bogus", i.e, something which is a fake. Hence, the BogoMips value gives some indication of the processor speed, but it is way too unscientific to be called anything but BogoMips. The reasons (there are two) it is printed during boot-up is that a) it is slightly useful for debugging and for checking that the computer[’]s caches and turbo button work, and b) Linus loves to chuckle when he sees confused people on the news. [...]```I was wondering what BogoMIPS was, and wikipedia had this.

gollark: ```Architecture: x86_64CPU op-mode(s): 32-bit, 64-bitByte Order: Little EndianCPU(s): 8On-line CPU(s) list: 0-7Thread(s) per core: 2Core(s) per socket: 4Socket(s): 1NUMA node(s): 1Vendor ID: GenuineIntelCPU family: 6Model: 42Model name: Intel(R) Xeon(R) CPU E31240 @ 3.30GHzStepping: 7CPU MHz: 1610.407CPU max MHz: 3700.0000CPU min MHz: 1600.0000BogoMIPS: 6587.46Virtualization: VT-xL1d cache: 32KL1i cache: 32KL2 cache: 256KL3 cache: 8192KNUMA node0 CPU(s): 0-7Flags: fpu vme de pse tsc msr pae mce cx8 apic sep mtrr pge mca cmov pat pse36 clflush dts acpi mmx fxsr sse sse2 ss ht tm pbe syscall nx rdtscp lm constant_tsc arch_perfmon pebs bts rep_good nopl xtopology nonstop_tsc cpuid aperfmperf pni pclmulqdq dtes64 monitor ds_cpl vmx smx est tm2 ssse3 cx16 xtpr pdcm pcid sse4_1 sse4_2 x2apic popcnt tsc_deadline_timer aes xsave avx lahf_lm pti tpr_shadow vnmi flexpriority ept vpid xsaveopt dtherm ida arat pln pts```

gollark: I think it's a server thing.

References

Kishimoto M (2013). "Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes". Diabetes, Metabolic Syndrome and Obesity. 6: 187–95. doi:10.2147/DMSO.S35682. PMC 3650886. PMID 23671395.
"TENELIA® 20mg tablets, a Treatment for Type 2 Diabetes Mellitus Approval of Partial Change in Indication to Lift Restrictions in Combination Therapy". Media & Investors. Daiichi Sankyo.
Bronson J, Black A, Dhar TG, Ellsworth BA, Merritt JR (2013). Teneligliptin (Antidiabetic), Chapter: To Market, To Market - 2012. Annual Reports in Medicinal Chemistry. 48. pp. 523–524. doi:10.1016/b978-0-12-417150-3.00028-4. ISBN 9780124171503.
Nabeno M, Akahoshi F, Kishida H, Miyaguchi I, Tanaka Y, Ishii S, Kadowaki T (May 2013). "A comparative study of the binding modes of recently launched dipeptidyl peptidase IV inhibitors in the active site". Biochemical and Biophysical Research Communications. 434 (2): 191–6. doi:10.1016/j.bbrc.2013.03.010. PMID 23501107.

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[1] Kishimoto M (2013). "Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes". Diabetes, Metabolic Syndrome and Obesity. 6: 187–95. doi:10.2147/DMSO.S35682. PMC 3650886. PMID 23671395.

[2] "TENELIA® 20mg tablets, a Treatment for Type 2 Diabetes Mellitus Approval of Partial Change in Indication to Lift Restrictions in Combination Therapy". Media & Investors. Daiichi Sankyo.

[3] Bronson J, Black A, Dhar TG, Ellsworth BA, Merritt JR (2013). Teneligliptin (Antidiabetic), Chapter: To Market, To Market - 2012. Annual Reports in Medicinal Chemistry. 48. pp. 523–524. doi:10.1016/b978-0-12-417150-3.00028-4. ISBN 9780124171503.

[4] Nabeno M, Akahoshi F, Kishida H, Miyaguchi I, Tanaka Y, Ishii S, Kadowaki T (May 2013). "A comparative study of the binding modes of recently launched dipeptidyl peptidase IV inhibitors in the active site". Biochemical and Biophysical Research Communications. 434 (2): 191–6. doi:10.1016/j.bbrc.2013.03.010. PMID 23501107.