U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C22H27ClFN7O4S
Molecular Weight 540.0126
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ENCORAFENIB

SMILES

CC(C)n1cc(-c2ccnc(NC[C@]([H])(C)N=C(O)OC)n2)c(-c3cc(cc(c3F)NS(=O)(=O)C)Cl)n1

InChI

InChIKey=CMJCXYNUCSMDBY-ZDUSSCGKSA-N
InChI=1S/C22H27ClFN7O4S/c1-12(2)31-11-16(17-6-7-25-21(28-17)26-10-13(3)27-22(32)35-4)20(29-31)15-8-14(23)9-18(19(15)24)30-36(5,33)34/h6-9,11-13,30H,10H2,1-5H3,(H,27,32)(H,25,26,28)/t13-/m0/s1

HIDE SMILES / InChI

Molecular Formula C22H27ClFN7O4S
Molecular Weight 540.0126
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23617957 | https://www.drugbank.ca/drugs/DB11718

Encorafenib, also known as BRAFTOVI or LGX818, is an orally available mutated BRaf V600E inhibitor with potential antineoplastic activity, which was developed by Novartis. LGX818 possesses selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E. In the A375 (BRAFV600E) human melanoma cell line LGX818 suppresses phospho-ERK (EC50 = 3 nM) leading to potent inhibition of proliferation (EC50 = 4 nM). No significant activity was observed against a panel of 100 kinases (IC50 > 900 nM) and LGX818 did not inhibit proliferation of > 400 cell lines expressing wild-type BRAF. On June 27, 2018, the Food and Drug Administration approved encorafenib and Binimetinib (BRAFTOVI and MEKTOVI, Array BioPharma Inc.) in combination for patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. Encorafenib and binimetinib target two different kinases in the RAS/RAF/MEK/ERK pathway. Compared with either drug alone, co-administration of encorafenib and binimetinib result in greater anti-proliferative activity in vitro in BRAF mutation-positive cell lines and greater anti-tumor activity with respect to tumor growth inhibition in BRAF V600E mutant human melanoma xenograft studies in mice. In addition to the above, the combination of encorafenib and binimetinib acted to delay the emergence of resistance in BRAF V600E mutant human melanoma xenografts in mice compared with the administration of either drug alone. Encorafenib is in phase III for Metastatic Colorectal Cancer and in phase II for Relapsed or Refractory Multiple Myeloma.

Originator

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
BRAFTOVI

Approved Use

BRAFTOVI is a kinase inhibitor indicated, in combination with binimetinib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. (1, 2.1) Limitations of Use: BRAFTOVI is not indicated for treatment of patients with wild-type BRAF melanoma. (1, 5.2)

Launch Date

1.53005759E12
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
5153 ng/mL
450 mg 1 times / day steady-state, oral
dose: 450 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered: CETUXIMAB
ENCORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1050 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENCORAFENIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
16946 ng × h/mL
450 mg 1 times / day steady-state, oral
dose: 450 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered: CETUXIMAB
ENCORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3940 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENCORAFENIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3 h
450 mg 1 times / day steady-state, oral
dose: 450 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered: CETUXIMAB
ENCORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6.11 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENCORAFENIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
6.77%
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENCORAFENIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 26-79 years
n = 15
Health Status: unhealthy
Age Group: 26-79 years
Sex: M+F
Population Size: 15
Sources:
DLT: Myalgia, Arthralgia...
Dose limiting toxicities:
Myalgia (33.3%)
Arthralgia (26.7%)
Fatigue (20%)
Asthenia (13.3%)
VIIth nerve paralysis (6.7%)
Insomnia (6.7%)
Sources:
700 mg 1 times / day multiple, oral
Highest studied dose
Dose: 700 mg, 1 times / day
Route: oral
Route: multiple
Dose: 700 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 2
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 2
Sources:
DLT: Diarrhea, Headache...
Disc. AE: Headache...
Dose limiting toxicities:
Diarrhea (1 patient)
Headache (1 patient)
Rash (1 patient)
Asthenia (1 patient)
Insomnia (1 patient)
AEs leading to
discontinuation/dose reduction:
Headache (1.9%)
Sources:
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 25
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 25
Sources:
Disc. AE: Palmar-plantar erythrodysesthesia syndrome...
AEs leading to
discontinuation/dose reduction:
Palmar-plantar erythrodysesthesia syndrome (3.7%)
Sources:
300 mg 1 times / day multiple, oral
RP2D
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 5
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 5
Sources:
DLT: Neuralgia...
Disc. AE: Neuralgia...
Dose limiting toxicities:
Neuralgia (1 patient)
AEs leading to
discontinuation/dose reduction:
Neuralgia (1.9%)
Sources:
100 mg 1 times / day multiple, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 9
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 9
Sources:
DLT: Palmar-plantar erythrodysesthesia syndrome...
Disc. AE: Palmar-plantar erythrodysesthesia syndrome...
Dose limiting toxicities:
Palmar-plantar erythrodysesthesia syndrome (1 patient)
AEs leading to
discontinuation/dose reduction:
Palmar-plantar erythrodysesthesia syndrome (3.7%)
Sources:
100 mg 2 times / day multiple, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 4
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 4
Sources:
DLT: Facial paresis, Confusional state...
Dose limiting toxicities:
Facial paresis (1 patient)
Confusional state (1 patient)
Sources:
150 mg 2 times / day multiple, oral
Dose: 150 mg, 2 times / day
Route: oral
Route: multiple
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 3
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 3
Sources:
DLT: Musculoskeletal pain, Neck pain...
Dose limiting toxicities:
Musculoskeletal pain (1 patient)
Neck pain (1 patient)
Neuralgia (1 patient)
Sources:
550 mg 1 times / day multiple, oral
Dose: 550 mg, 1 times / day
Route: oral
Route: multiple
Dose: 550 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 4
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 4
Sources:
DLT: Fatigue...
Disc. AE: Hyperkeratosis...
Dose limiting toxicities:
Fatigue (1 patient)
AEs leading to
discontinuation/dose reduction:
Hyperkeratosis (1.9%)
Sources:
300 mg 1 times / day multiple, oral
RP2D
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
unhealthy, 61.0 years (range: 43–79 years)
n = 9
Health Status: unhealthy
Age Group: 61.0 years (range: 43–79 years)
Sex: M+F
Population Size: 9
Sources:
DLT: Pancreatitis acute, Insomnia...
Dose limiting toxicities:
Pancreatitis acute (1 patient)
Insomnia (1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Asthenia 13.3%
DLT
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 26-79 years
n = 15
Health Status: unhealthy
Age Group: 26-79 years
Sex: M+F
Population Size: 15
Sources:
Fatigue 20%
DLT
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 26-79 years
n = 15
Health Status: unhealthy
Age Group: 26-79 years
Sex: M+F
Population Size: 15
Sources:
Arthralgia 26.7%
DLT
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 26-79 years
n = 15
Health Status: unhealthy
Age Group: 26-79 years
Sex: M+F
Population Size: 15
Sources:
Myalgia 33.3%
DLT
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 26-79 years
n = 15
Health Status: unhealthy
Age Group: 26-79 years
Sex: M+F
Population Size: 15
Sources:
Insomnia 6.7%
DLT
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 26-79 years
n = 15
Health Status: unhealthy
Age Group: 26-79 years
Sex: M+F
Population Size: 15
Sources:
VIIth nerve paralysis 6.7%
DLT
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 26-79 years
n = 15
Health Status: unhealthy
Age Group: 26-79 years
Sex: M+F
Population Size: 15
Sources:
Asthenia 1 patient
DLT
700 mg 1 times / day multiple, oral
Highest studied dose
Dose: 700 mg, 1 times / day
Route: oral
Route: multiple
Dose: 700 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 2
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 2
Sources:
Diarrhea 1 patient
DLT
700 mg 1 times / day multiple, oral
Highest studied dose
Dose: 700 mg, 1 times / day
Route: oral
Route: multiple
Dose: 700 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 2
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 2
Sources:
Headache 1 patient
DLT
700 mg 1 times / day multiple, oral
Highest studied dose
Dose: 700 mg, 1 times / day
Route: oral
Route: multiple
Dose: 700 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 2
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 2
Sources:
Insomnia 1 patient
DLT
700 mg 1 times / day multiple, oral
Highest studied dose
Dose: 700 mg, 1 times / day
Route: oral
Route: multiple
Dose: 700 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 2
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 2
Sources:
Rash 1 patient
DLT
700 mg 1 times / day multiple, oral
Highest studied dose
Dose: 700 mg, 1 times / day
Route: oral
Route: multiple
Dose: 700 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 2
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 2
Sources:
Headache 1.9%
Disc. AE
700 mg 1 times / day multiple, oral
Highest studied dose
Dose: 700 mg, 1 times / day
Route: oral
Route: multiple
Dose: 700 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 2
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 2
Sources:
Palmar-plantar erythrodysesthesia syndrome 3.7%
Disc. AE
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 25
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 25
Sources:
Neuralgia 1 patient
DLT
300 mg 1 times / day multiple, oral
RP2D
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 5
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 5
Sources:
Neuralgia 1.9%
Disc. AE
300 mg 1 times / day multiple, oral
RP2D
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 5
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 5
Sources:
Palmar-plantar erythrodysesthesia syndrome 1 patient
DLT
100 mg 1 times / day multiple, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 9
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 9
Sources:
Palmar-plantar erythrodysesthesia syndrome 3.7%
Disc. AE
100 mg 1 times / day multiple, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 9
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 9
Sources:
Confusional state 1 patient
DLT
100 mg 2 times / day multiple, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 4
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 4
Sources:
Facial paresis 1 patient
DLT
100 mg 2 times / day multiple, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 4
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 4
Sources:
Musculoskeletal pain 1 patient
DLT
150 mg 2 times / day multiple, oral
Dose: 150 mg, 2 times / day
Route: oral
Route: multiple
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 3
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 3
Sources:
Neck pain 1 patient
DLT
150 mg 2 times / day multiple, oral
Dose: 150 mg, 2 times / day
Route: oral
Route: multiple
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 3
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 3
Sources:
Neuralgia 1 patient
DLT
150 mg 2 times / day multiple, oral
Dose: 150 mg, 2 times / day
Route: oral
Route: multiple
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 3
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 3
Sources:
Fatigue 1 patient
DLT
550 mg 1 times / day multiple, oral
Dose: 550 mg, 1 times / day
Route: oral
Route: multiple
Dose: 550 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 4
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 4
Sources:
Hyperkeratosis 1.9%
Disc. AE
550 mg 1 times / day multiple, oral
Dose: 550 mg, 1 times / day
Route: oral
Route: multiple
Dose: 550 mg, 1 times / day
Sources:
unhealthy, 51.0 years (range: 33–70 years)
n = 4
Health Status: unhealthy
Age Group: 51.0 years (range: 33–70 years)
Sex: M+F
Population Size: 4
Sources:
Insomnia 1 patient
DLT
300 mg 1 times / day multiple, oral
RP2D
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
unhealthy, 61.0 years (range: 43–79 years)
n = 9
Health Status: unhealthy
Age Group: 61.0 years (range: 43–79 years)
Sex: M+F
Population Size: 9
Sources:
Pancreatitis acute 1 patient
DLT
300 mg 1 times / day multiple, oral
RP2D
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
unhealthy, 61.0 years (range: 43–79 years)
n = 9
Health Status: unhealthy
Age Group: 61.0 years (range: 43–79 years)
Sex: M+F
Population Size: 9
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >50 uM]
yes [EC50 3.8 uM]
yes [IC50 0.92 uM]
yes [IC50 1 uM]
yes [IC50 10 uM]
yes [IC50 12.7 uM]
yes [IC50 2.05 uM]
yes [IC50 22 uM]
yes [IC50 25 uM]
yes [IC50 30 uM]
yes [IC50 4 uM]
yes [IC50 4.2 uM]
yes [IC50 5 uM]
yes [IC50 5.35 uM]
yes [IC50 6.16 uM]
yes [IC50 8 uM]
yes [IC50 >100 uM]
yes [IC50 >100 uM]
yes [IC50 >100 uM]
yes [IC50 >50 uM]
yes
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
yes
yes
yes
yes
yes (co-administration study)
Comment: Coadministration of repeat doses of posaconazole (a strong CYP3A4 inhibitor) with a single dose encorafenib 50 mg increased encorafenib AUC by 2.8-fold (90% CI: 2.5, 3.2) and Cmax by 1.7-fold (90% CI: 1.5, 1.8) as compared with encorafenib administered alone.
Page: 69.0
Tox targets
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Personalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapies.
2016 Apr 1
Cutaneous toxicity of a new BRAF inhibitor, LGX818 (encorafenib).
2017 Jan-Feb
Patents

Sample Use Guides

Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to the initiation of BRAFTOVI. (2.1) The recommended dose is 450 mg orally once daily in combination with binimetinib. Take BRAFTOVI with or without food.
Route of Administration: Oral
In Vitro Use Guide
Sources: DOI: 10.1158/1538-7445 DOI: 10.1158/1538-7445 Retrived from http://cancerres.aacrjournals.org/content/72/8_Supplement/3790
In the A375 (BRAFV600E) human melanoma cell line LGX818 (ENCORAFENIB) suppresses phospho-ERK (EC50 = 3 nM) leading to potent inhibition of proliferation (EC50 = 4 nM). No significant activity was observed against a panel of 100 kinases (IC50 > 900 nM) and LGX818 did not inhibit proliferation of > 400 cell lines expressing wild-type BRAF.
Substance Class Chemical
Created
by admin
on Sat Jun 26 14:55:07 UTC 2021
Edited
by admin
on Sat Jun 26 14:55:07 UTC 2021
Record UNII
8L7891MRB6
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ENCORAFENIB
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
LGX-818
Common Name English
ENCORAFENIB [USAN]
Common Name English
ENCORAFENIB [MI]
Common Name English
BRAFTOVI
Brand Name English
ENCORAFENIB [INN]
Common Name English
LGX818
Common Name English
NVP-LGX818
Code English
ENCORAFENIB [ORANGE BOOK]
Common Name English
ENCORAFENIB [WHO-DD]
Common Name English
NVP-LGX-818-NXA
Code English
CARBAMIC ACID, N-((1S)-2-((4-(3-(5-CHLORO-2-FLUORO-3-((METHYLSULFONYL)AMINO)PHENYL)-1-(1-METHYLETHYL)-1H-PYRAZOL-4-YL)-2-PYRIMIDINYL)AMINO)-1-METHYLETHYL)-, METHYL ESTER
Common Name English
NVP-LGX818-NXA
Code English
METHYL N-((2S)-1-((4-(3-(5-CHLORO-2-FLUORO-3-(METHANESULFONAMIDO)PHENYL)(-1-(PROPAN-2-YL)-1H-PYRAZOL-4-YL(PYRIMIDIN-2-YL)AMINO)PROPAN-2-YL)CARBAMATE
Systematic Name English
Classification Tree Code System Code
WHO-ATC L01XE46
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
FDA ORPHAN DRUG 411413
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
FDA ORPHAN DRUG 411613
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
NCI_THESAURUS C61074
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
Code System Code Type Description
EPA CompTox
1269440-17-6
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
NCI_THESAURUS
C98283
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
FDA UNII
8L7891MRB6
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
EVMPD
SUB177218
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
ChEMBL
CHEMBL3301612
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
LACTMED
Encorafenib
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
RXCUI
2049106
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
DRUG BANK
DB11718
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
INN
9816
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
CAS
1269440-17-6
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
DRUG CENTRAL
5289
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
MERCK INDEX
M12077
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
PUBCHEM
50922675
Created by admin on Sat Jun 26 14:55:08 UTC 2021 , Edited by admin on Sat Jun 26 14:55:08 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> INHIBITOR
IC50
METABOLIC ENZYME -> INHIBITOR
IC50
METABOLIC ENZYME -> INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
IC50
EXCRETED UNCHANGED
Following a single 100 mg oral dose of 14C-encorafenib, 47% of the administered dose (1.8% as unchanged) was recovered in the urine.
URINE
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TRANSPORTER -> INHIBITOR
IC50
TARGET -> INHIBITOR
IC50
METABOLIC ENZYME -> INHIBITOR
IC50
METABOLIC ENZYME -> INDUCER
IC50
METABOLIC ENZYME -> INHIBITOR
IC50
METABOLIC ENZYME -> INDUCER
IC50
METABOLIC ENZYME -> SUBSTRATE
MINOR
TARGET -> INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
IC50
EXCRETED UNCHANGED
Following a single 100 mg oral dose of 14C-encorafenib, 39% of the administered dose (5% as unchanged) was recovered in the feces.
FECAL
METABOLIC ENZYME -> INHIBITOR
IC50
BINDER->LIGAND
Encorafenib is 86% bound to human plasma proteins and binding is not concentrationdependent
METABOLIC ENZYME -> INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
IC50
METABOLIC ENZYME -> INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
MINOR
TRANSPORTER -> INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> INDUCER
IC50
TRANSPORTER -> INHIBITOR
IC50
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC DOSE

Biological Half-life PHARMACOKINETIC DOSE

Tmax PHARMACOKINETIC DOSE