Teneligliptin

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H30N6OS
Molecular Weight	426.578
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=NN(C(=C1)N2CCN(CC2)[C@@H]3CN[C@@H](C3)C(=O)N4CCSC4)C5=CC=CC=C5

InChI

InChIKey=WGRQANOPCQRCME-PMACEKPBSA-N

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

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23671395
Curator's Comment: description was created based on several sources, including https://www.pmda.go.jp/files/000153594.pdf

Teneligliptin is a DPP IV inhibitor which was developed by Mitsubishi Tanabe Pharma and now is used for the treatment of type 2 diabetes mellitus in Asia under the name Tenelia.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dipeptidyl peptidase IV 37 Target ID: CHEMBL284 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23671395	Inhibitor 8504		0.889 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23671395	Primary		Approved 8583	TENELIA Approved Use Type 2 diabetes mellitus. Launch Date 2012

C_max

Value	Dose	Analyte	Population
236.2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=30 \| https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_K102_2.pdf#page=18	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
187.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=30 \| https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_K102_2.pdf#page=18	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
13.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
77.22 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
187.2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
382.4 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
955.77 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2107.83 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
420.67 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
160.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
220.14 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
926.73 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1180.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
176.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
208 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
203.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
191.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
195.8 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=39	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
219 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=39	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
164.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=39	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
185.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=40	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
229.3 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=40	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
247.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=40	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
1861.1 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=30 \| https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_K102_2.pdf#page=18	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1814.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=30 \| https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_K102_2.pdf#page=18	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
298 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
876.9 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2028.9 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3705.1 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7649.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18180.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3613.5 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1057.2 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1514.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5257.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7292.2 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1772.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2234.2 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3090.3 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2833.3 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1843.1 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=39	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2472.9 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=39	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2162.5 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=39	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1548.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=40	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2207.9 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=40	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2418.9 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=40	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
27.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=30 \| https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_K102_2.pdf#page=18	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
28.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=30 \| https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_K102_2.pdf#page=18	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
31.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
25.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
24.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
20.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
24.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
23.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
27.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
25.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
30.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
17.6 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
23.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=33	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
26.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
27.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
36 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
29.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=38	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
18.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=39	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
23.6 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=39	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
22.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=39	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
24.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=40	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
27.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=40	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
30.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=40	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TENELIGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
17.8% OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_A100_2.pdf#page=30 \| https://www.pmda.go.jp/drugs/2012/P201200070/400315000_22400AMX00728_I100_2.pdf#page=35			TENELIGLIPTIN plasma	Homo sapiens

Doses

Dose	Population	Adverse events
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/26212570/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FED Sources: https://pubmed.ncbi.nlm.nih.gov/26212570/	Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (grade 3, 5%) Sources: https://pubmed.ncbi.nlm.nih.gov/26212570/

AEs

AE	Significance	Dose	Population
Vomiting	grade 3, 5% Disc. AE	40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/26212570/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FED Sources: https://pubmed.ncbi.nlm.nih.gov/26212570/

PubMed

Title	Date	PubMed
Comparative Binding Analysis of Dipeptidyl Peptidase IV (DPP-4) with Antidiabetic Drugs - An Ab Initio Fragment Molecular Orbital Study.	2016	27832184
Teneligliptin, a Dipeptidyl Peptidase-4 Inhibitor, Improves Early-Phase Insulin Secretion in Drug-Naïve Patients with Type 2 Diabetes.	2015-09	26224337
Teneligliptin improves glycemic control with the reduction of postprandial insulin requirement in Japanese diabetic patients.	2015	25252844
Add-on treatment with teneligliptin ameliorates glucose fluctuations and improves glycemic control index in Japanese patients with type 2 diabetes on insulin therapy.	2014-12	25144424
Teneligliptin as an initial therapy for newly diagnosed, drug naive subjects with type 2 diabetes.	2014-08	24883155
Efficacy and safety of teneligliptin in combination with pioglitazone in Japanese patients with type 2 diabetes mellitus.	2013-11-27	24843712
Efficacy, safety and dose-response relationship of teneligliptin, a dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes mellitus.	2013-09	23464664
Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes.	2013	23671395
Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.	2012-10-01	22959556

Patents

Sample Use Guides

In Vivo Use Guide

The usual adult dosage is 20 mg of teneligliptin administered orally once daily. If efficacy is insufficient, the dose may be increased up to 40 mg once daily while closely monitoring the clinical course.

Route of Administration: Oral

In Vitro Use Guide

Human umbilical vein endothelial cells were cultured under normal (5 mmol/L) or high glucose level (25 mmol/L) during 21 days, or at high glucose during 14 days followed by 7 days at normal glucose, to reproduce the high-metabolic memory state. At this time, different concentrations of teneligliptin (0.1, 1.0 and 3.0 umol/L) were added to cells. Teneligliptin was shown to protect human umbilical vein endothelial cells from oxidative stress.

Name

Type

Language

MP-513

Preferred Name

English

Teneligliptin

Official Name

English

teneligliptin [INN]

Common Name

English

Teneligliptin [WHO-DD]

Common Name

English

Methanone, [(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]-3-thiazolidinyl-

Systematic Name

English

Teneligliptin [MI]

Common Name

English

[(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]-3-thiazolidinylmethanone

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C98086