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

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	MOL RATIO 1 MOL RATIO (average)

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

Description

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	Inhibitor 8,456		3.8 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262	Primary		Approved 8,548	SUINY

C_max

Value	Dose	Analyte	Population
499 ng/mL	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
422 ng/mL	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
57.7 ng/mL	10 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
186 ng/mL	25 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
253 ng/mL	50 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
624 ng/mL	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
1040 ng/mL	200 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
3330 ng/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
266 ng/mL	50 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
544 ng/mL	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
1250 ng/mL	200 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
1280 ng/mL	200 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
1200 ng/mL	200 mg 2 times / day multiple, oral	ANAGLIPTIN plasma	Homo sapiens
2704.5 ng/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
2522.9 ng/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
2401 ng/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
3349 ng/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
2769 ng/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
2991 ng/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
3396 ng/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
3381 ng/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
2200 ng × h/mL	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
1960 ng × h/mL	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
202 ng × h/mL	10 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
641 ng × h/mL	25 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
1040 ng × h/mL	50 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
2650 ng × h/mL	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
5360 ng × h/mL	200 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
12600 ng × h/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
1050 ng × h/mL	50 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
2460 ng × h/mL	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
4900 ng × h/mL	200 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
4740 ng × h/mL	200 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
4890 ng × h/mL	200 mg 2 times / day multiple, oral	ANAGLIPTIN plasma	Homo sapiens
11294 ng × h/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
9650 ng × h/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
7582 ng × h/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
12533 ng × h/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
13370 ng × h/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
20446 ng × h/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
24437 ng × h/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
21263 ng × h/mL	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
3.02 h	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
4.05 h	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
5.06 h	10 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
4.82 h	25 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
6.51 h	50 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
6.2 h	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
5.75 h	200 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
6 h	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
7.61 h	50 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
9.9 h	100 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
6.59 h	200 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
7.93 h	200 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
7.03 h	200 mg 2 times / day multiple, oral	ANAGLIPTIN plasma	Homo sapiens
5.99 h	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
8.45 h	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
9.58 h	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
7.17 h	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
6.84 h	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
7.25 h	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
8.54 h	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens
8.55 h	400 mg single, oral	ANAGLIPTIN plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
51.8%			ANAGLIPTIN serum	Homo sapiens

Doses

Show entries

Dose	Population	Adverse events
200 mg 2 times / day multiple, oral Highest studied dose	unhealthy, ADULT	Other AEs: Pharyngitis, Dyspepsia...
400 mg single, oral Highest studied dose	healthy, ADULT
200 mg 2 times / day multiple, oral Studied dose	unhealthy, ADULT	Disc. AE: Angioedema...

Showing 1 to 3 of 3 entries

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AEs

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AE	Significance	Dose	Population
Pharyngitis	16.13%	200 mg 2 times / day multiple, oral Highest studied dose	unhealthy, ADULT
Abdominal pai	3.23%	200 mg 2 times / day multiple, oral Highest studied dose	unhealthy, ADULT
Abscess	3.23%	200 mg 2 times / day multiple, oral Highest studied dose	unhealthy, ADULT
Bronchitis	3.23%	200 mg 2 times / day multiple, oral Highest studied dose	unhealthy, ADULT
Constipation	3.23%	200 mg 2 times / day multiple, oral Highest studied dose	unhealthy, ADULT

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PubMed

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Title	Date	PubMed
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 Dec 1	22019046
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
Additive effects of miglitol and anagliptin on insulin-treated type 2 diabetes mellitus: a case study.	2015 Feb	25511640

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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
Record UNII	K726J96838
Record Status	`Validated (UNII)`
Record Version

Show entries

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

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Classification Tree

Code System

Code

Enzyme Inhibitor

NCI_THESAURUS

C98086

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Code System

Code

Type

Description

EPA CompTox

DTXSID401045689

PRIMARY

EVMPD

SUB93457

PRIMARY

WIKIPEDIA

Anagliptin

PRIMARY

DRUG BANK

DB12417

PRIMARY

PUBCHEM

44513473

PRIMARY

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Related Record

Type

Details


					K726J96838

ANAGLIPTIN

ACTIVE MOIETY

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SMILES

InChI

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Funbound

Doses

AEs

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound