BELVARAFENIB

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C23H16ClFN6OS
Molecular Weight	478.929
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC1=C(NC(=O)C2=CSC3=C2N=CN=C3N)C4=CC=NC(NC5=CC=CC(Cl)=C5F)=C4C=C1

InChI

InChIKey=KVCQTKNUUQOELD-UHFFFAOYSA-N

InChI=1S/C23H16ClFN6OS/c1-11-5-6-13-12(7-8-27-22(13)30-16-4-2-3-15(24)17(16)25)18(11)31-23(32)14-9-33-20-19(14)28-10-29-21(20)26/h2-10H,1H3,(H,27,30)(H,31,32)(H2,26,28,29)

HIDE SMILES / InChI

Approval Year

C_max

Value	Dose	Analyte	Population
552.7 μg/L	50 mg single, oral	BELVARAFENIB plasma	Homo sapiens
806.7 μg/L	100 mg single, oral	BELVARAFENIB plasma	Homo sapiens
601.8 μg/L	200 mg single, oral	BELVARAFENIB plasma	Homo sapiens
899.8 μg/L	400 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
1213.1 μg/L	600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
1592.3 μg/L	900 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
1790 μg/L	1300 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
1438.8 μg/L	1600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
1115 μg/L	50 mg 1 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
1986.7 μg/L	100 mg 1 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
2524 μg/L	200 mg 1 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
3213.8 μg/L	400 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
5695 μg/L	600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
6094.3 μg/L	900 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
7325 μg/L	1300 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
2362.5 μg/L	1600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
26992.9 μg × h/L	50 mg single, oral	BELVARAFENIB plasma	Homo sapiens
51512.2 μg × h/L	100 mg single, oral	BELVARAFENIB plasma	Homo sapiens
37767.7 μg × h/L	200 mg single, oral	BELVARAFENIB plasma	Homo sapiens
78336.7 μg × h/L	400 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
169243.6 μg × h/L	600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
177316.6 μg × h/L	900 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
223040.9 μg × h/L	1300 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
142290.4 μg × h/L	1600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
88753.7 μg × h/L	50 mg 1 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
349410.1 μg × h/L	100 mg 1 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
239193.5 μg × h/L	200 mg 1 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
206835.1 μg × h/L	400 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
507018 μg × h/L	600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
322397.4 μg × h/L	900 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
625324.6 μg × h/L	1300 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
138758.7 μg × h/L	1600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
127000 ng × h/mL	450 mg 2 times / day steady-state, oral	BELVARAFENIB plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
51.6 h	50 mg single, oral	BELVARAFENIB plasma	Homo sapiens
55.3 h	100 mg single, oral	BELVARAFENIB plasma	Homo sapiens
57.7 h	200 mg single, oral	BELVARAFENIB plasma	Homo sapiens
70.7 h	400 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
86.6 h	600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
84.3 h	900 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
77.9 h	1300 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
61.8 h	1600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
70.7 h	50 mg 1 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
106.1 h	100 mg 1 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
69.8 h	200 mg 1 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
41.2 h	400 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
52.3 h	600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
32.3 h	900 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
66.4 h	1300 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens
42.7 h	1600 mg 2 times / day multiple, oral	BELVARAFENIB plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.11%	450 mg 2 times / day steady-state, oral		BELVARAFENIB plasma	Homo sapiens

Show entries

Name

Type

Language

4-AMINO-N-(1-((3-CHLORO-2-FLUOROPHENYL)AMINO)-6-METHYLISOQUINOLIN-5-YL)THIENO(3,2-D)PYRIMIDINE-7-CARBOXAMIDE

Preferred Name

English

BELVARAFENIB

Official Name

English

belvarafenib [INN]

Common Name

English

THIENO(3,2-D)PYRIMIDINE-7-CARBOXAMIDE, 4-AMINO-N-(1-((3-CHLORO-2-FLUOROPHENYL)AMINO)-6-METHYL-5-ISOQUINOLINYL)-

Systematic Name

English

Belvarafenib [WHO-DD]

Common Name

English

Showing 1 to 5 of 5 entries

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Show entries

Code System

Code

Type

Description

CAS

1446113-23-0

PRIMARY

NCI_THESAURUS

C121646

PRIMARY

FDA UNII

31M3WLJ3KG

PRIMARY

PUBCHEM

89655386

PRIMARY

USAN

FG-177

PRIMARY

Showing 1 to 5 of 7 entries

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ACTIVE MOIETY


					31M3WLJ3KG

BELVARAFENIB

SMILES

InChI

Approval Year

Cmax

AUC

T1/2

Funbound

C_max

T_1/2

F_unbound