BELVARAFENIB

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

Structure Search

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

Molecular Formula	C23H16ClFN6OS
Molecular Weight	478.929
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

C_max

Value	Dose	Analyte	Population
552.7 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
806.7 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
601.8 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
899.8 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1213.1 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1592.3 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	900 mg 2 times / day multiple, oral dose: 900 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1790 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1300 mg 2 times / day multiple, oral dose: 1300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1438.8 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1600 mg 2 times / day multiple, oral dose: 1600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1115 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
1986.7 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
2524 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
3213.8 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
5695 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
6094.3 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	900 mg 2 times / day multiple, oral dose: 900 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
7325 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1300 mg 2 times / day multiple, oral dose: 1300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
2362.5 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1600 mg 2 times / day multiple, oral dose: 1600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

AUC

Value	Dose	Analyte	Population
26992.9 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
51512.2 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
37767.7 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
78336.7 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
169243.6 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
177316.6 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	900 mg 2 times / day multiple, oral dose: 900 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
223040.9 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1300 mg 2 times / day multiple, oral dose: 1300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
142290.4 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1600 mg 2 times / day multiple, oral dose: 1600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
88753.7 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
349410.1 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
239193.5 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
206835.1 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
507018 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
322397.4 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	900 mg 2 times / day multiple, oral dose: 900 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
625324.6 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1300 mg 2 times / day multiple, oral dose: 1300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
138758.7 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1600 mg 2 times / day multiple, oral dose: 1600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
127000 ng × h/mL OTHER https://investors.kinnate.com/static-files/cd6f5996-ca49-40fc-8241-209d76882173	450 mg 2 times / day steady-state, oral dose: 450 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
51.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
55.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
57.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
70.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
86.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
84.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	900 mg 2 times / day multiple, oral dose: 900 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
77.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1300 mg 2 times / day multiple, oral dose: 1300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
61.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1600 mg 2 times / day multiple, oral dose: 1600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
70.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
106.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
69.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
41.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
52.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
32.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	900 mg 2 times / day multiple, oral dose: 900 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
66.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1300 mg 2 times / day multiple, oral dose: 1300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
42.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33953400/	1600 mg 2 times / day multiple, oral dose: 1600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.11% OTHER https://investors.kinnate.com/static-files/cd6f5996-ca49-40fc-8241-209d76882173	450 mg 2 times / day steady-state, oral dose: 450 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BELVARAFENIB plasma	Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Substance Class	Chemical Created by `admin` on `Tue Apr 01 23:30:59 GMT 2025` Edited by `admin` on `Tue Apr 01 23:30:59 GMT 2025`
Record UNII	31M3WLJ3KG
Record Status	`Validated (UNII)`
Record Version

Download

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

Code System Code Type Description

CAS

1446113-23-0