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Details

Stereochemistry ACHIRAL
Molecular Formula C25H30N6O2
Molecular Weight 446.5456
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ERDAFITINIB

SMILES

CC(C)NCCN(c1ccc2c(c1)nc(cn2)-c3cnn(C)c3)c4cc(cc(c4)OC)OC

InChI

InChIKey=OLAHOMJCDNXHFI-UHFFFAOYSA-N
InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3

HIDE SMILES / InChI

Molecular Formula C25H30N6O2
Molecular Weight 446.5456
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. It was discovered in collaboration with Janssen Pharmaceutica, N.V. from a partnership which commenced in June 2008. Astex’s FGFr inhibitor program originated from a collaboration initiated in 2005 with the Cancer Research UK Drug Discovery Group at the Newcastle Cancer Centre (Newcastle University UK), and Cancer Research Technology Limited. JNJ42756493 is currently being evaluated by Janssen in Phase 2 clinical trials in patients with urothelial cancer, advanced hepatocellular carcinoma, advanced non-small lung cancer, esophageal cancer or cholangiocarcinoma. JNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). In vitro, the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival. It is also in phase I trials for the treatment of advanced refractory solid tumors or advanced refractory hematologic cancer.

Approval Year

TargetsConditions
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1399 ng/mL
8 mg 1 times / day steady-state, oral
dose: 8 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ERDAFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
29268 ng × h/mL
8 mg 1 times / day steady-state, oral
dose: 8 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ERDAFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
59 h
8 mg 1 times / day steady-state, oral
dose: 8 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ERDAFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.2%
8 mg 1 times / day steady-state, oral
dose: 8 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ERDAFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
12 mg 1 times / day multiple, oral
Highest studied dose
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, 62.7 years
Health Status: unhealthy
Age Group: 62.7 years
Sex: M+F
Sources:
DLT: Retinal pigment epithelium atrophy...
Dose limiting toxicities:
Retinal pigment epithelium atrophy (grade 2, 1 patient)
Sources:
10 mg 1 times / day multiple, oral
RP2D
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
unhealthy, 65.7 years
Health Status: unhealthy
Age Group: 65.7 years
Sex: M+F
Sources:
Other AEs: Hyperphosphatemia...
Other AEs:
Hyperphosphatemia (3 patients)
Sources:
12 mg 1 times / day multiple, oral
Highest studied dose
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
DLT: Alanine aminotransferase increase...
Dose limiting toxicities:
Alanine aminotransferase increase (grade 3, 1 patient)
Sources:
12 mg 1 times / day steady, oral
Highest studied dose
Dose: 12 mg, 1 times / day
Route: oral
Route: steady
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Disc. AE: Acute myocardial infarction, Eye disorders...
Other AEs: Hyperphosphatemia, Stomatitis...
AEs leading to
discontinuation/dose reduction:
Acute myocardial infarction (grade 5, 1%)
Eye disorders (6%)
Other AEs:
Hyperphosphatemia (24%)
Stomatitis (17%)
Eye disorders (17%)
Palmar-plantar erythrodysaesthesia syndrome (8%)
Eye disorders (23%)
Stomatitis (15%)
Hyperphosphatemia (7%)
Palmar-plantar erythrodysaesthesia syndrome (7%)
Paronychia (7%)
Nail dystrophy (6%)
Sources:
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Other AEs: Hemoglobin decreased, Platelets decreased...
Other AEs:
Hemoglobin decreased (grade 3-4, 3%)
Platelets decreased (grade 3-4, 1%)
Neutrophil count decreased (grade 3-4, 2%)
Phosphate increased (grade 3-4, 1%)
Creatinine increased (grade 3-4, 5%)
Sodium decreased (grade 3-4, 16%)
Alanine aminotransferase increased (grade 3-4, 1%)
Alkaline phosphatase increased (grade 3-4, 1%)
Magnesium decreased (grade 3-4, 1%)
Phosphate decreased (grade 3-4, 9%)
Calcium increased (grade 3-4, 3%)
Sources:
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Other AEs: Stomatitis, Diarrhea...
Other AEs:
Stomatitis (all grades, 56%)
Diarrhea (all grades, 47%)
Dry mouth (all grades, 45%)
Constipation (all grades, 28%)
Abdominal pain (all grades, 23%)
Nausea (all grades, 21%)
Vomiting (all grades, 13%)
Decreased appetite (all grades, 38%)
Fatigue (all grades, 54%)
Pyrexia (all grades, 14%)
Onycholysis (all grades, 41%)
Dry skin (all grades, 34%)
Palmar-plantar erythrodysaesth. (all grades, 26%)
Alopecia (all grades, 26%)
Nail discoloration (all grades, 11%)
Dry eye (all grades, 28%)
Vision blurred (all grades, 17%)
Lacrimation increased (all grades, 10%)
Dysgeusia (all grades, 37%)
Paronychia (all grades, 17%)
Urinary tract infection (all grades, 17%)
Conjunctivitis (all grades, 11%)
Oropharyngeal pain (all grades, 11%)
Dyspnea (all grades, 10%)
Hematuria (all grades, 11%)
Musculoskeletal pain (all grades, 20%)
Arthralgia (all grades, 11%)
Weight decreased (all grades, 16%)
Stomatitis (grade 3-4, 9%)
Diarrhea (grade 3-4, 2%)
Constipation (grade 3-4, 1%)
Abdominal pain (grade 3-4, 2%)
Nausea (grade 3-4, 1%)
Vomiting (grade 3-4, 2%)
Fatigue (grade 3-4, 10%)
Pyrexia (grade 3-4, 1%)
Onycholysis (grade 3-4, 10%)
Palmar-plantar erythrodysaesth. (grade 3-4, 6%)
Dry eye (grade 3-4, 6%)
Dysgeusia (grade 3-4, 1%)
Paronychia (grade 3-4, 3%)
Urinary tract infection (grade 3-4, 6%)
Oropharyngeal pain (grade 3-4, 1%)
Dyspnea (grade 3-4, 2%)
Hematuria (grade 3-4, 2%)
Gastrointestinal disorders (all grades, 94%)
Metabolism and nutrition disorders (all grades, 90%)
Skin and subcutaneous tissue disorders (all grades, 75%)
Eye disorders (all grades, 62%)
Nervous system disorders (all grades, 57%)
Infections and infestations (all grades, 56%)
Respiratory, thoracic and mediastinal disorders (all grades, 40%)
Renal and urinary disorders (all grades, 38%)
Musculoskeletal and connective tissue disorders (all grades, 31%)
Gastrointestinal disorders (grade 3-4, 24%)
Metabolism and nutrition disorders (grade 3-4, 16%)
Skin and subcutaneous tissue disorders (grade 3-4, 16%)
Eye disorders (grade 3-4, 11%)
Nervous system disorders (grade 3-4, 5%)
Infections and infestations (grade 3-4, 20%)
Respiratory, thoracic and mediastinal disorders (grade 3-4, 7%)
Renal and urinary disorders (grade 3-4, 10%)
Hemoglobin decreased (all grades, 35%)
Platelets decreased (all grades, 19%)
Leukocyte count decreased (all grades, 17%)
Neutrophil count decreased (all grades, 10%)
Phosphate increased (all grades, 76%)
Creatinine increased (all grades, 52%)
Sodium decreased (all grades, 40%)
Alanine aminotransferase increased (all grades, 41%)
Alkaline phosphatase increased (all grades, 41%)
Albumin decreased (all grades, 37%)
Aspartate aminotransferase increased (all grades, 30%)
Magnesium decreased (all grades, 30%)
Phosphate decreased (all grades, 24%)
Calcium increased (all grades, 22%)
Potassium increased (all grades, 16%)
Fasting blood glucose increased (all grades, 10%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Retinal pigment epithelium atrophy grade 2, 1 patient
DLT, Disc. AE
12 mg 1 times / day multiple, oral
Highest studied dose
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, 62.7 years
Health Status: unhealthy
Age Group: 62.7 years
Sex: M+F
Sources:
Hyperphosphatemia 3 patients
10 mg 1 times / day multiple, oral
RP2D
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
unhealthy, 65.7 years
Health Status: unhealthy
Age Group: 65.7 years
Sex: M+F
Sources:
Alanine aminotransferase increase grade 3, 1 patient
DLT
12 mg 1 times / day multiple, oral
Highest studied dose
Dose: 12 mg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Stomatitis 15%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Eye disorders 17%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Stomatitis 17%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Eye disorders 23%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Hyperphosphatemia 24%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Nail dystrophy 6%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Eye disorders 6%
Disc. AE
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Hyperphosphatemia 7%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Palmar-plantar erythrodysaesthesia syndrome 7%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Paronychia 7%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Palmar-plantar erythrodysaesthesia syndrome 8%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Acute myocardial infarction grade 5, 1%
Disc. AE
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Alanine aminotransferase increased grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Alkaline phosphatase increased grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Magnesium decreased grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Phosphate increased grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Platelets decreased grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Sodium decreased grade 3-4, 16%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Neutrophil count decreased grade 3-4, 2%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Calcium increased grade 3-4, 3%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Hemoglobin decreased grade 3-4, 3%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Creatinine increased grade 3-4, 5%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Phosphate decreased grade 3-4, 9%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Dyspnea all grades, 10%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Fasting blood glucose increased all grades, 10%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Lacrimation increased all grades, 10%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Neutrophil count decreased all grades, 10%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Arthralgia all grades, 11%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Conjunctivitis all grades, 11%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Hematuria all grades, 11%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Nail discoloration all grades, 11%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Oropharyngeal pain all grades, 11%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Vomiting all grades, 13%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Pyrexia all grades, 14%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Potassium increased all grades, 16%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Weight decreased all grades, 16%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Leukocyte count decreased all grades, 17%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Paronychia all grades, 17%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Urinary tract infection all grades, 17%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Vision blurred all grades, 17%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Platelets decreased all grades, 19%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Musculoskeletal pain all grades, 20%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Nausea all grades, 21%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Calcium increased all grades, 22%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Abdominal pain all grades, 23%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Phosphate decreased all grades, 24%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Alopecia all grades, 26%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Palmar-plantar erythrodysaesth. all grades, 26%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Constipation all grades, 28%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Dry eye all grades, 28%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Aspartate aminotransferase increased all grades, 30%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Magnesium decreased all grades, 30%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Musculoskeletal and connective tissue disorders all grades, 31%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Dry skin all grades, 34%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Hemoglobin decreased all grades, 35%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Albumin decreased all grades, 37%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Dysgeusia all grades, 37%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Decreased appetite all grades, 38%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Renal and urinary disorders all grades, 38%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Respiratory, thoracic and mediastinal disorders all grades, 40%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Sodium decreased all grades, 40%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Alanine aminotransferase increased all grades, 41%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Alkaline phosphatase increased all grades, 41%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Onycholysis all grades, 41%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Dry mouth all grades, 45%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Diarrhea all grades, 47%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Creatinine increased all grades, 52%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Fatigue all grades, 54%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Infections and infestations all grades, 56%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Stomatitis all grades, 56%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Nervous system disorders all grades, 57%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Eye disorders all grades, 62%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Skin and subcutaneous tissue disorders all grades, 75%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Phosphate increased all grades, 76%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Metabolism and nutrition disorders all grades, 90%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Gastrointestinal disorders all grades, 94%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Constipation grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Dysgeusia grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Nausea grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Oropharyngeal pain grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Pyrexia grade 3-4, 1%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Fatigue grade 3-4, 10%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Onycholysis grade 3-4, 10%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Renal and urinary disorders grade 3-4, 10%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Eye disorders grade 3-4, 11%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Metabolism and nutrition disorders grade 3-4, 16%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Skin and subcutaneous tissue disorders grade 3-4, 16%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Abdominal pain grade 3-4, 2%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Diarrhea grade 3-4, 2%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Dyspnea grade 3-4, 2%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Hematuria grade 3-4, 2%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Vomiting grade 3-4, 2%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Infections and infestations grade 3-4, 20%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Gastrointestinal disorders grade 3-4, 24%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Paronychia grade 3-4, 3%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Nervous system disorders grade 3-4, 5%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Dry eye grade 3-4, 6%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Palmar-plantar erythrodysaesth. grade 3-4, 6%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Urinary tract infection grade 3-4, 6%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Respiratory, thoracic and mediastinal disorders grade 3-4, 7%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Stomatitis grade 3-4, 9%
8 mg 1 times / day steady, oral
Recommended
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Overview

OverviewOther

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
likely
no
no
no
no
no
no
weak
yes
yes
likely (co-administration study)
Comment: Time-dependent inhibitor, Concomitant CYP3A substrates with narrow therapeutic index should be avoided.; Erdafitinib mean ratios (90% CI) for Cmax and AUCinf were 105% (86.7, 127) and 134% (109, 164), respectively, when co-administered with itraconazole (a strong CYP3A4 inhibitor and P-gp inhibitor) relative to erdafitinib alone.
Page: 97, (label) 14
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: Concomitant fluconazole (moderate CYP2C9/moderate CYP3A inhibitor, 400 mg QD for 11 days) increased erdafitinib (4 mg single dose on Day 5) AUC by 48% and Cmax by 21% (fasted, healthy subjects with CYP2C9*1/*1, *1/*2 genotypes). The contribution of CYP2C9 in the total clearance of erdafitinib isestimated to be 39%.
Page: 82, 95, 96
major
yes (co-administration study)
Comment: Concomitant itraconazole (strong CYP3A/P-gp inhibitor, 200 mg QD for 11 days) increased erdafitinib (4 mg single dose on Day 5) AUC by 34% but did not significantly change Cmax (5%)(fasted, healthy subjects with CYP2C9*1/*1, *1/*2 genotypes). The contribution of CYP3A in the total clearance of erdafitinib is estimated to be 20%.
Page: 82, 95, 96
yes
yes (co-administration study)
Comment: Concomitant itraconazole (strong CYP3A/P-gp inhibitor, 200 mg QD for 11 days) increased erdafitinib (4 mg single dose on Day 5) AUC by 34% but did not significantly change Cmax (5%)(fasted, healthy subjects with CYP2C9*1/*1, *1/*2 genotypes). The contribution of CYP3A in the total clearance of erdafitinib is estimated to be 20%. Erdafinitib dosse should be separated by >/= 6 h befor or after administration of P-gp substrates with narrow therapeutic index.
Page: 95, 96
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
RACK1 forms a complex with FGFR1 and PKM2, and stimulates the growth and migration of squamous lung cancer cells.
2017 Nov
Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors.
2018 Jun
Patents

Patents

Sample Use Guides

Cancer patients will receive a 8 milligram (mg) starting dose once daily with option to up-titrate to 9 mg on a 28-day cycle.
Route of Administration: Oral
Erdafitinib (JNJ-42756493) effectively inhibited pFGFR1, pFGFR3 and pFGFR4
Substance Class Chemical
Created
by admin
on Sat Jun 26 06:36:01 UTC 2021
Edited
by admin
on Sat Jun 26 06:36:01 UTC 2021
Record UNII
890E37NHMV
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ERDAFITINIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
PAN-FGFR TYROSINE KINASE INHIBITOR JNJ-42756493
Common Name English
BALVERSA
Brand Name English
ERDAFITINIB [ORANGE BOOK]
Common Name English
ERDAFITINIB [INN]
Common Name English
ERDAFITINIB [USAN]
Common Name English
JNJ-42756493
Code English
ERDAFITINIB [WHO-DD]
Common Name English
1,2-ETHANEDIAMINE, N1-(3,5-DIMETHOXYPHENYL)-N2-(1-METHYLETHYL)-N1-(3-(1-METHYL-1H-PYRAZOL-4-YL)-6-QUINOXALINYL)-
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C1967
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C103273
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
DRUG CENTRAL
5327
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
CAS
1346242-81-6
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
INN
10147
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
ChEMBL
CHEMBL3545376
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
DRUG BANK
DB12147
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
FDA UNII
890E37NHMV
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
RXCUI
2123125
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
CAS
1620332-47-9
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
NO STRUCTURE GIVEN
PUBCHEM
67462786
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
LACTMED
Erdafitinib
Created by admin on Sat Jun 26 06:36:01 UTC 2021 , Edited by admin on Sat Jun 26 06:36:01 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
IC50
EXCRETED UNCHANGED
URINE
TARGET -> INHIBITOR
IC50
BINDER->LIGAND
primarily to alpha-1-acid glycoprotein.
BINDING
TARGET -> INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
EXCRETED UNCHANGED
FECAL
METABOLIC ENZYME -> SUBSTRATE
CYP3A4 in the total clearance of erdafitinib is estimated to be 20%.
METABOLIC ENZYME -> SUBSTRATE
Contribution of CYP2C9 to the total clearance of erdafitinib is estimated to be 39%
TARGET -> INHIBITOR
IC50
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC