Nerigliatin

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H20N6O4
Molecular Weight	432.432
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C)C(=O)C1=NC=C(OC2=CC(=CC3=C2C=C(C)O3)C(=O)NC4=NC=C(C)N=C4)C=N1

InChI

InChIKey=MASKQITXHVYVFL-UHFFFAOYSA-N

InChI=1S/C22H20N6O4/c1-12-8-24-19(11-23-12)27-21(29)14-6-17-16(5-13(2)31-17)18(7-14)32-15-9-25-20(26-10-15)22(30)28(3)4/h5-11H,1-4H3,(H,24,27,29)

HIDE SMILES / InChI

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Glucokinase 2 Target ID: P35557 Gene ID: 2645.0 Gene Symbol: GCK Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/23831135 \| https://adisinsight.springer.com/drugs/800031713 \| https://newdrugapprovals.org/tag/pf-04937319/	Activator 1447		0.19 µM [EC50]

C_max

Value	Dose	Analyte	Population
38.22 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
69.49 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
119.4 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
245.4 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
449.3 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
57.73 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
122.3 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED
234.1 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
421.5 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
970.6 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
51.09 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
79.3 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	30 mg 1 times / day steady-state, oral dose: 30 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
171.3 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
251.5 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
555.9 ng/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
407 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
867.7 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
1456 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2749 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6034 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
458 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
928.7 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	30 mg 1 times / day steady-state, oral dose: 30 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
1889 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3167 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7446 ng × h/mL CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
6.563 h CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6.884 h CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	30 mg 1 times / day steady-state, oral dose: 30 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
6.348 h CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6.96 h CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.479 h CLINICAL TRIAL https://classic.clinicaltrials.gov/ct2/show/results/NCT01272804	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PF-04937319 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
31% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25142735/	single, unknown		PF-04937319 plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Name

Type

Language

PF-04937319

Preferred Name

English

Nerigliatin

Common Name

English

2-Pyrimidinecarboxamide, N,N-dimethyl-5-[[2-methyl-6-[[(5-methyl-2-pyrazinyl)amino]carbonyl]-4-benzofuranyl]oxy]-

Systematic Name

English

nerigliatin [INN]

Common Name

English

N,N-Dimethyl-5-[[2-methyl-6-[[(5-methyl-2-pyrazinyl)amino]carbonyl]-4-benzofuranyl]oxy]-2-pyrimidinecarboxamide

Systematic Name

English

Code System Code Type Description

DRUG BANK

DB15009