Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H30N6O2 |
Molecular Weight | 446.5447 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC(=CC(OC)=C1)N(CCNC(C)C)C2=CC=C3N=CC(=NC3=C2)C4=CN(C)N=C4
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
Molecular Formula | C25H30N6O2 |
Molecular Weight | 446.5447 |
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3650 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788 |
1.2 nM [IC50] | ||
Target ID: CHEMBL4142 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788 |
2.5 nM [IC50] | ||
Target ID: CHEMBL2742 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788 |
3.0 nM [IC50] | ||
Target ID: CHEMBL3973 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788 |
5.7 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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 n = 7 Health Status: unhealthy Condition: Cancer Age Group: 62.7 years Sex: M+F Population Size: 7 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 n = 3 Health Status: unhealthy Condition: Cancer Age Group: 65.7 years Sex: M+F Population Size: 3 Sources: |
Other AEs: Hyperphosphatemia... |
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 n = 13 Health Status: unhealthy Condition: solid tumors Age Group: adult Sex: unknown Population Size: 13 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: Page: 84 |
unhealthy, adult n = 7 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 7 Sources: Page: 84 |
|
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
Disc. AE: Acute myocardial infarction, Eye disorders... Other AEs: Hyperphosphatemia, Stomatitis... AEs leading to discontinuation/dose reduction: Acute myocardial infarction (grade 5, 1%) Other AEs:Eye disorders (6%) Hyperphosphatemia (24%) Sources: Page: 6.1Stomatitis (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%) |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
Other AEs: Stomatitis, Diarrhea... Other AEs: Stomatitis (all grades, 56%) Sources: Page: Table 3Diarrhea (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%) |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
Other AEs: Hemoglobin decreased, Platelets decreased... Other AEs: Hemoglobin decreased (grade 3-4, 3%) Sources: Page: Table 4Platelets 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 n = 7 Health Status: unhealthy Condition: Cancer Age Group: 62.7 years Sex: M+F Population Size: 7 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 n = 3 Health Status: unhealthy Condition: Cancer Age Group: 65.7 years Sex: M+F Population Size: 3 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 n = 13 Health Status: unhealthy Condition: solid tumors Age Group: adult Sex: unknown Population Size: 13 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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: 6.1 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: 6.1 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 3 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 3 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
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: Page: Table 4 |
unhealthy, adult n = 87 Health Status: unhealthy Condition: urothelial carcinoma Age Group: adult Sex: unknown Population Size: 87 Sources: Page: Table 4 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: (label) 14 |
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
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 82, 95, 96 |
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%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 82, 95, 96 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 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%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 82, 95, 96 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212018Orig1s000MultidisciplineR.pdf#page=96 Page: 95, 96 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Oncogenic Characterization and Pharmacologic Sensitivity of Activating Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations to the Selective FGFR Inhibitor Erdafitinib. | 2017 Aug |
|
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
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02699606
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28341788
Erdafitinib (JNJ-42756493) effectively inhibited pFGFR1, pFGFR3 and pFGFR4
at 100nM in NCI-H1581, KMS-11 and MDA-MB-453 cells, respectively, and pFGFR2 at 30nM in SNU-16 cells. Inhibition of FGFR auto-phosphorylation was consistent with its antiproliferative IC50s in these cell lines (2.6, 0.40, 102.4, and 129.2 nM, for NCI-H1581, SNU-16, KMS-11 and MDA-MB-453, respectively)
Substance Class |
Chemical
Created
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on
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Record UNII |
890E37NHMV
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Record Status |
Validated (UNII)
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NCI_THESAURUS |
C1967
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NCI_THESAURUS |
C129825
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C103273
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1346242-81-6
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Erdafitinib
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m12171
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DTXSID001027936
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890E37NHMV
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CHEMBL3545376
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DB12147
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890E37NHMV
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DE-47
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1620332-47-9
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100000177214
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67462786
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Erdafitinib
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
IC50
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EXCRETED UNCHANGED |
URINE
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TARGET -> INHIBITOR |
IC50
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BINDER->LIGAND |
primarily to alpha-1-acid glycoprotein.
BINDING
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TARGET -> INHIBITOR |
IC50
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TRANSPORTER -> INHIBITOR |
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TRANSPORTER -> SUBSTRATE |
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EXCRETED UNCHANGED |
FECAL
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METABOLIC ENZYME -> SUBSTRATE |
CYP3A4 in the total clearance of erdafitinib is estimated to be 20%.
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METABOLIC ENZYME -> SUBSTRATE |
Contribution of CYP2C9 to the total clearance of erdafitinib is estimated to be 39%
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TARGET -> INHIBITOR |
IC50
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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