ANAGLIPTIN

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C19H25N7O2
Molecular Weight	383.4475
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=NN2C=C(C=NC2=C1)C(=O)NCC(C)(C)NCC(=O)N3CCC[C@H]3C#N

InChI

InChIKey=LDXYBEHACFJIEL-HNNXBMFYSA-N

InChI=1S/C19H25N7O2/c1-13-7-16-21-9-14(11-26(16)24-13)18(28)22-12-19(2,3)23-10-17(27)25-6-4-5-15(25)8-20/h7,9,11,15,23H,4-6,10,12H2,1-3H3,(H,22,28)/t15-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C19H25N7O2
Molecular Weight	383.4475
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.kowa-souyaku.co.jp/upload/item/24/35/7-wse_163.doc
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23337530

Anagliptin is a DPP-4 inhibitor developed for the treatment of type 2 diabetes mellitus. The drug was approved in Japan under the name Suiny and now it is being tested in the USA.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dipeptidyl peptidase IV 37 Target ID: CHEMBL284 Sources: http://www.kowa-souyaku.co.jp/upload/item/24/35/7-wse_163.doc	Inhibitor 8504		3.8 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262 Sources: http://www.kowa-souyaku.co.jp/upload/item/24/35/7-wse_163.doc	Primary		Approved 8583	SUINY Approved Use It is usually used for the treatment of type 2 diabetes mellitus.

C_max

Value	Dose	Analyte	Population
499 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=35	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
422 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=35	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
57.7 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
186 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
253 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
624 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1040 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3330 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
266 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
544 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1250 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1280 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=40	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1200 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=40	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2704.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=44	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2522.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=44	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2401 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3349 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2769 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2991 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3396 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3381 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43 \| https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_K105_1.pdf#page=120	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
2200 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=35	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1960 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=35	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
202 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
641 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1040 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2650 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5360 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12600 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1050 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2460 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4900 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4740 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=40	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4890 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=40	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11294 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=44	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9650 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=44	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7582 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
12533 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
13370 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
20446 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
24437 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
21263 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43 \| https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_K105_1.pdf#page=120	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
3.02 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=35	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.05 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=35	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
5.06 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.82 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.51 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.75 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.61 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.59 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=39	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.93 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=40	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.03 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=40	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.99 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=44	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.45 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=44	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9.58 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.17 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6.84 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.25 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.54 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.55 h OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=43 \| https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_K105_1.pdf#page=120	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANAGLIPTIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
51.8% OTHER GOV'T https://www.pmda.go.jp/drugs/2012/P201200123/300297000_22400AMX01387000_A100_1.pdf#page=36			ANAGLIPTIN serum	Homo sapiens

Doses

Dose	Population	Adverse events
200 mg 2 times / day multiple, oral Highest studied dose Dose: 200 mg, 2 times / day Route: oral Route: multiple Dose: 200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25819061/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25819061/	Other AEs: Pharyngitis, Dyspepsia... Other AEs: Pharyngitis (16.13%) Dyspepsia (9.68%) Dizziness (3.23%) Nausea (6.45%) Arthralgia (6.45%) Hypercalcaemia (3.23%) Muscae volitantes (6.45%) Macular oedem (3.23%) Eye abnormality (3.23%) Pruritus (3.23%) Urticaria (3.23%) Dermatitis fungal (3.23%) Upper respiratory tract infection (3.23%) Sputum abnormal (3.23%) Pneumonia (3.23%) Coughing (6.45%) Bronchitis (3.23%) Abscess (3.23%) Hyperuricaemia (3.23%) Hypertriglyceridaemia (3.23%) Hepatic function abnormal (3.23%) Hearing decreased (3.23%) Constipation (3.23%) Abdominal pai (3.23%) Hypoaesthesia (3.23%) Headache (6.45%) Oedema peripheral (3.23%) Granulomatous lesio (3.23%) Sources: https://pubmed.ncbi.nlm.nih.gov/25819061/
400 mg single, oral Highest studied dose Dose: 400 mg Route: oral Route: single Dose: 400 mg Sources: https://professional.diabetes.org/files/Posters/2007/p0482-P.pdf	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://professional.diabetes.org/files/Posters/2007/p0482-P.pdf	Sources: https://professional.diabetes.org/files/Posters/2007/p0482-P.pdf
200 mg 2 times / day multiple, oral Studied dose Dose: 200 mg, 2 times / day Route: oral Route: multiple Dose: 200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23972359/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23972359/	Disc. AE: Angioedema... AEs leading to discontinuation/dose reduction: Angioedema Sources: https://pubmed.ncbi.nlm.nih.gov/23972359/

AEs

PubMed

Title	Date	PubMed
Anti-inflammatory role of DPP-4 inhibitors in a nondiabetic model of glomerular injury.	2015-04-15	25656369
Additive effects of miglitol and anagliptin on insulin-treated type 2 diabetes mellitus: a case study.	2015-02	25511640
A randomized, placebo-controlled, double-blind, phase 3 trial to evaluate the efficacy and safety of anagliptin in drug-naïve patients with type 2 diabetes.	2015	25819061
High-fat diet feeding significantly attenuates anagliptin-induced regeneration of islets of Langerhans in streptozotocin-induced diabetic mice.	2015	26097511
Pharmacokinetics and metabolism of [14C]anagliptin, a novel dipeptidyl peptidase-4 inhibitor, in humans.	2013-05	23075005
Anagliptin, a DPP-4 inhibitor, suppresses proliferation of vascular smooth muscles and monocyte inflammatory reaction and attenuates atherosclerosis in male apo E-deficient mice.	2013-03	23337530
Inhibition of postprandial hyperglycemia by either an insulin-dependent or -independent drug reduces the expression of genes related to inflammation in peripheral leukocytes of OLETF rats.	2013	24200798
Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor.	2011-12-01	22019046

Patents

Sample Use Guides

In Vivo Use Guide

In general, for adults, take 1 tablet (100mg of anagliptin) at a time, twice a day, in the morning and in the evening. If the effect is insufficient, a dose may be increased up to 2 tablets (200mg) at a time, adequately monitoring the condition.

Route of Administration: Oral

In Vitro Use Guide

Rat aortic smooth muscle cells were incubated with 100 uM of anagliptin and its effect on cells prolifiration was studied. Anagliptin suppressed the proliferation by inhibiting ERK phosphorylation.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:59:40 GMT 2025` Edited by `admin` on `Mon Mar 31 18:59:40 GMT 2025`
Record UNII	K726J96838
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ANAGLIPTIN

Official Name

English

CWP-403

Preferred Name

English

Anagliptin [WHO-DD]

Common Name

English

ANAGLIPTIN [JAN]

Common Name

English

anagliptin [INN]

Common Name

English

N-(2-((2-((2S)-2-CYANOPYRROLIDIN-1-YL)-2-OXOETHYL)AMINO)-2-METHYLPROPYL)-2-METHYLPYRAZOLO(1,5-A)PYRIMIDINE-6-CARBOXAMIDE

Systematic Name

English

SK-0403

Code

English

SUINY

Brand Name

English

ANAGLIPTIN [MI]

Common Name

English

PYRAZOLO(1,5-A)PYRIMIDINE-6-CARBOXAMIDE, N-(2-((2-((2S)-2-CYANO-1-PYRROLIDINYL)-2-OXOETHYL)AMINO)-2-METHYLPROPYL)-2-METHYL-

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C98086