Firmonertinib

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C28H31F3N8O2
Molecular Weight	568.5933
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C)CCN(C)C1=NC(OCC(F)(F)F)=C(NC2=NC=CC(=N2)C3=CN(C)C4=C3C=CC=C4)C=C1NC(=O)C=C

InChI

InChIKey=GHKOONMJXNWOIW-UHFFFAOYSA-N

InChI=1S/C28H31F3N8O2/c1-6-24(40)33-21-15-22(26(41-17-28(29,30)31)36-25(21)38(4)14-13-37(2)3)35-27-32-12-11-20(34-27)19-16-39(5)23-10-8-7-9-18(19)23/h6-12,15-16H,1,13-14,17H2,2-5H3,(H,33,40)(H,32,34,35)

HIDE SMILES / InChI

Approval Year

C_max

Value	Dose	Analyte	Population
7.37 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
20 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
34.3 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
80.4 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
110 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
17.4 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
33.7 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
61.2 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	80 mg 1 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
92.3 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	160 mg 1 times / day steady-state, oral dose: 160 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
120 ng/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
25.4 ng/mL CLINICAL TRIAL https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7757978/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
39.6 ng/mL CLINICAL TRIAL https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7757978/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

AUC

Value	Dose	Analyte	Population
99.5 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
276 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
473 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1060 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1610 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
316 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
585 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1050 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	80 mg 1 times / day steady-state, oral dose: 80 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1640 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	160 mg 1 times / day steady-state, oral dose: 160 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2020 ng × h/mL CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S1556086420300319#appsec1	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ALFLUTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
843 ng × h/mL CLINICAL TRIAL https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7757978/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1110 ng × h/mL CLINICAL TRIAL https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7757978/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	ALFLUTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

T_1/2

Value	Dose	Co-administered	Analyte	Population
34.9 h CLINICAL TRIAL https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7757978/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:		ALFLUTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
34.1 h CLINICAL TRIAL https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7757978/	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:		ALFLUTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

F_unbound

Value	Dose	Co-administered	Analyte	Population
5% EXPERIMENT https://www.nature.com/articles/s41401-021-00667-8	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:		ALFLUTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Name

Type

Language

Firmonertinib

Official Name

English

ALFLUTINIB

Preferred Name

English

AST-2818

Code

English

AST2818

Code

English

Furmonertinib [WHO-DD]

Common Name

English

FIRMONERTINIB [USAN]

Common Name

English

N-[2-{[2-(dimethylamino)ethyl](methyl)amino}-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}-6-(2,2,2-trifluoroethoxy)pyridin-3-yl]prop-2-enamide

Systematic Name

English

N-[2-[[2-(Dimethylamino)ethyl]methylamino]-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]-6-(2,2,2-trifluoroethoxy)-3-pyridinyl]-2-propenamide

Systematic Name

English

firmonertinib [INN]

Common Name

English

FURMONERTINIB

Common Name

English

2-Propenamide, N-[2-[[2-(dimethylamino)ethyl]methylamino]-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]-6-(2,2,2-trifluoroethoxy)-3-pyridinyl]-

Systematic Name

English

Code System Code Type Description

PUBCHEM

118861389