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Details

Stereochemistry ACHIRAL
Molecular Formula C21H16ClF3N4O3
Molecular Weight 464.8257
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SORAFENIB

SMILES

CNC(=O)c1cc(ccn1)Oc2ccc(cc2)NC(=Nc3ccc(c(c3)C(F)(F)F)Cl)O

InChI

InChIKey=MLDQJTXFUGDVEO-UHFFFAOYSA-N
InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)

HIDE SMILES / InChI

Description
Curator's Comment:: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/20812347 https://www.ncbi.nlm.nih.gov/pubmed/16757355

Sorafenib (BAY 43-9006), marketed as Nexavar by Bayer, is a drug approved for the treatment of advanced renal cell carcinoma (primary kidney cancer, hepatocellular carcinoma and for the treatment of patients with locally recurrent or metastatic, progressive, differentiated thyroid carcinoma (DTC) that is refractory to radioactive iodine treatment. It has also received "Fast Track" designation by the FDA for the treatment of advanced hepatocellular carcinoma (primary liver cancer), and has since performed well in Phase III trials. Sorafenib was shown to interact with multiple intracellular (CRAF, BRAF and mutant BRAF) and cell surface kinases (KIT, FLT- 3, VEGFR- 2, VEGFR- 3, and PDGFR- ß). Several of these kinases are thought to be involved in angiogenesis. Thus, sorafenib may inhibit tumor growth by a dual mechanism, acting either directly on the tumor (through inhibition of Raf and Kit signaling) and/or on tumor angiogenesis (through inhibition of VEGFR and PDGFR signaling). Sorafenib inhibited tumor growth of the murine renal cell carcinoma, RENCA, and several other human tumor xenografts in athymic mice. A reduction in tumor angiogenesis was seen in some tumor xenograft models.

CNS Activity

Curator's Comment:: Sorafenib effectively crosses the blood-brain barrier and inhibits tumor growth in an orthotopic tumor model of glioblastoma

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
NEXAVAR

Approved Use

NEXAVAR is a kinase inhibitor indicated for the treatment of •Unresectable hepatocellular carcinoma (1.1) •Advanced renal cell carcinoma (1.2) •Locally recurrent or metastatic, progressive, differentiated thyroid carcinoma refractory to radioactive iodine treatment (1.3) 1.1 Hepatocellular Carcinoma NEXAVAR® is indicated for the treatment of patients with unresectable hepatocellular carcinoma (HCC). 1.2 Renal Cell Carcinoma NEXAVAR is indicated for the treatment of patients with advanced renal cell carcinoma (RCC). 1.3 Differentiated Thyroid Carcinoma NEXAVAR is indicated for the treatment of patients with locally recurrent or metastatic, progressive, differentiated thyroid carcinoma (DTC) that is refractory to radioactive iodine treatment.

Launch Date

1.13503686E12
Primary
NEXAVAR

Approved Use

NEXAVAR is a kinase inhibitor indicated for the treatment of •Unresectable hepatocellular carcinoma (1.1) •Advanced renal cell carcinoma (1.2) •Locally recurrent or metastatic, progressive, differentiated thyroid carcinoma refractory to radioactive iodine treatment (1.3) 1.1 Hepatocellular Carcinoma NEXAVAR® is indicated for the treatment of patients with unresectable hepatocellular carcinoma (HCC). 1.2 Renal Cell Carcinoma NEXAVAR is indicated for the treatment of patients with advanced renal cell carcinoma (RCC). 1.3 Differentiated Thyroid Carcinoma NEXAVAR is indicated for the treatment of patients with locally recurrent or metastatic, progressive, differentiated thyroid carcinoma (DTC) that is refractory to radioactive iodine treatment.

Launch Date

1.13503686E12
Primary
NEXAVAR

Approved Use

NEXAVAR is a kinase inhibitor indicated for the treatment of •Unresectable hepatocellular carcinoma (1.1) •Advanced renal cell carcinoma (1.2) •Locally recurrent or metastatic, progressive, differentiated thyroid carcinoma refractory to radioactive iodine treatment (1.3) 1.1 Hepatocellular Carcinoma NEXAVAR® is indicated for the treatment of patients with unresectable hepatocellular carcinoma (HCC). 1.2 Renal Cell Carcinoma NEXAVAR is indicated for the treatment of patients with advanced renal cell carcinoma (RCC). 1.3 Differentiated Thyroid Carcinoma NEXAVAR is indicated for the treatment of patients with locally recurrent or metastatic, progressive, differentiated thyroid carcinoma (DTC) that is refractory to radioactive iodine treatment.

Launch Date

1.13503686E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.43 mg/L
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3.1 μg/mL
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3.8 μg/L
400 mg 2 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
9.4 mg × h/L
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
12.6 μg × h/mL
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
17.9 μg × h/mL
400 mg 2 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
27.1 h
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.31%
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.29%
400 mg 2 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SORAFENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
DLT: Hypertension, Rash...
Other AEs: Dyspnea, Rash...
Dose limiting toxicities:
Hypertension (grade 3, 33%)
Rash (grade 2, 33%)
Rash (grade 3, 67%)
Other AEs:
Dyspnea (grade 3, 33%)
Rash (grade 3, 67%)
Fatigue (grade 1, 67%)
Anorexia (grade 1, 33%)
Nausea (grade 1, 33%)
Pharyngitis (grade 1, 33%)
Dyspnea (grade 3, 33%)
Pruritis (grade 1, 67%)
Sources:
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Other AEs: Ascites, Constipation...
Other AEs:
Ascites (grade 3, 33%)
Constipation (grade 3, 17%)
Obstruction ureter (grade 3, 17%)
Hypoalbuminemia (grade 3, 17%)
Alkaline phosphatase (grade 3, 33%)
Muscle weakness (grade 3, 17%)
Depressed level of consciousness (grade 3, 17%)
Pleural effusion (grade 3, 17%)
Hypoxia (grade 3, 17%)
Pruritis (grade 1, 17%)
Rash (grade 1, 17%)
Hypocalcemia (grade 1, 17%)
Sources:
800 mg 2 times / day multiple, oral
Highest studied dose
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Other AEs: Diarrhea...
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Other AEs: Hand and foot skin reaction, Desquamation...
Other AEs:
Hand and foot skin reaction (10%)
Desquamation (5%)
Fatigue (12.5%)
Hypertension (5%)
Mucositis oral (2.5%)
Alopecia (12.5%)
Dry skin (12.5%)
Nausea (12.5%)
Vomiting (12.5%)
Anorexia (15%)
Weight loss (17.5%)
Hypocalcaemia (12.5%)
Sources:
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Other AEs: Hypertension, Fatigue...
Other AEs:
Hypertension (grade 3, 2%)
Fatigue (grade 3, 2%)
Fever (grade 3, <1%)
Weight loss (grade 3, <1%)
Rash (grade 3, 1%)
Hand and foot skin reaction (grade 3, 5%)
Pruritus (grade 3, <1%)
Flushing (grade 3, <1%)
Diarrhea (grade 3, 2%)
Nausea (grade 3, 1%)
Anorexia (grade 3, 1%)
Constipation (grade 3, 1%)
Vomiting (grade 3, <1%)
Mucositis (grade 3, <1%)
Infection (grade 3, 1%)
Cough (grade 3, <1%)
Dyspnea (grade 3, 2%)
Dyspnea (grade 4, <1%)
Hypertension (grade 4, <1%)
Fatigue (grade 4, <1%)
Lymphopenia (grade 3, 5.1%)
Amylase increased (grade 3, 2.4%)
Hyperglycemia (grade 3, 4.1%)
Hyperkalemia (grade 3, 2.1%)
Lipase increased (grade 3, 3.5%)
Hyponatremia (grade 3, 3.5%)
Hypophosphatemia (grade 3, 1.8%)
Lymphopenia (grade 4, 0.6%)
Amylase increased (grade 4, 0.6%)
Hyperglycemia (grade 4, 0.3%)
Hyperkalemia (grade 4, 0.6%)
Lipase increased (grade 4, 1.8%)
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
100 mg 2 times / day multiple, oral
Highest studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, Median age 60 years
n = 5
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 60 years
Sex: M+F
Population Size: 5
Sources:
DLT: Diarrhea...
Dose limiting toxicities:
Diarrhea (grade 3, 20%)
Sources:
400 mg 2 times / day multiple, oral
MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources:
unhealthy, Median age 60 years
n = 15
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 60 years
Sex: M+F
Population Size: 15
Sources:
Disc. AE: Pancreatitis...
AEs leading to
discontinuation/dose reduction:
Pancreatitis (grade 3, 6.7%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Anorexia grade 1, 33%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Nausea grade 1, 33%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Pharyngitis grade 1, 33%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Fatigue grade 1, 67%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Pruritis grade 1, 67%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Rash grade 2, 33%
DLT, Disc. AE
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Dyspnea grade 3, 33%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Dyspnea grade 3, 33%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Hypertension grade 3, 33%
DLT, Disc. AE
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Rash grade 3, 67%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Rash grade 3, 67%
DLT, Disc. AE
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 3
Sources:
Hypocalcemia grade 1, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Pruritis grade 1, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Rash grade 1, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Constipation grade 3, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Depressed level of consciousness grade 3, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Hypoalbuminemia grade 3, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Hypoxia grade 3, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Muscle weakness grade 3, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Obstruction ureter grade 3, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Pleural effusion grade 3, 17%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Alkaline phosphatase grade 3, 33%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Ascites grade 3, 33%
600 mg 2 times / day multiple, oral
MTD
Dose: 600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 600 mg, 2 times / day
Sources:
unhealthy, Mean age 53.7 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Mean age 53.7 years
Sex: M+F
Population Size: 6
Sources:
Diarrhea 22.5%
800 mg 2 times / day multiple, oral
Highest studied dose
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Hand and foot skin reaction 10%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Alopecia 12.5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Dry skin 12.5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Fatigue 12.5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Hypocalcaemia 12.5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Nausea 12.5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Vomiting 12.5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Anorexia 15%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Weight loss 17.5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Mucositis oral 2.5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Desquamation 5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Hypertension 5%
800 mg 2 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources:
unhealthy, Median age 57 years
n = 20
Health Status: unhealthy
Condition: metastatic renal cell carcinoma
Age Group: Median age 57 years
Sex: M+F
Population Size: 20
Sources:
Anorexia grade 3, 1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Constipation grade 3, 1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Infection grade 3, 1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Nausea grade 3, 1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Rash grade 3, 1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Hypophosphatemia grade 3, 1.8%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Diarrhea grade 3, 2%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Dyspnea grade 3, 2%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Fatigue grade 3, 2%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Hypertension grade 3, 2%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Hyperkalemia grade 3, 2.1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Amylase increased grade 3, 2.4%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Hyponatremia grade 3, 3.5%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Lipase increased grade 3, 3.5%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Hyperglycemia grade 3, 4.1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Hand and foot skin reaction grade 3, 5%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Lymphopenia grade 3, 5.1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Cough grade 3, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Fever grade 3, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Flushing grade 3, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Mucositis grade 3, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Pruritus grade 3, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Vomiting grade 3, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Weight loss grade 3, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Hyperglycemia grade 4, 0.3%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Amylase increased grade 4, 0.6%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Hyperkalemia grade 4, 0.6%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Lymphopenia grade 4, 0.6%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Lipase increased grade 4, 1.8%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Dyspnea grade 4, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Fatigue grade 4, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Hypertension grade 4, <1%
400 mg 2 times / day multiple, oral
Recommended
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
unhealthy, Median age 58 years
n = 384
Health Status: unhealthy
Condition: renal cell carcinoma
Age Group: Median age 58 years
Sex: M+F
Population Size: 384
Sources: Page: 021923_s000_Nexavar_MedR.pdf - p.68-71
Diarrhea grade 3, 20%
DLT
100 mg 2 times / day multiple, oral
Highest studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, Median age 60 years
n = 5
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 60 years
Sex: M+F
Population Size: 5
Sources:
Pancreatitis grade 3, 6.7%
Disc. AE
400 mg 2 times / day multiple, oral
MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: multiple
Dose: 400 mg, 2 times / day
Sources:
unhealthy, Median age 60 years
n = 15
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 60 years
Sex: M+F
Population Size: 15
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
yes [IC50 0.84 uM]
yes [Ki 1.5 uM]
yes [Ki 1.5 uM]
yes [Ki 17 uM]
no (co-administration study)
Comment: Administration of NEXAVAR 400 mg twice daily for 28 days did not alter the exposure of concomitantly administered midazolam (CYP3A4 substrate), dextromethorphan (CYP2D6 substrate), or omeprazole (CYP2C19 substrate).
Page: -
yes [Ki 2.4 uM]
yes [Ki 4.2 uM]
no (co-administration study)
Comment: Administration of NEXAVAR 400 mg twice daily for 28 days did not alter the exposure of concomitantly administered midazolam (CYP3A4 substrate), dextromethorphan (CYP2D6 substrate), or omeprazole (CYP2C19 substrate).
Page: -
yes [Ki 4.9 uM]
no (co-administration study)
Comment: Administration of NEXAVAR 400 mg twice daily for 28 days did not alter the exposure of concomitantly administered midazolam (CYP3A4 substrate), dextromethorphan (CYP2D6 substrate), or omeprazole (CYP2C19 substrate).
Page: -
yes [Ki 6.2 uM]
yes [Ki 7.3 uM]
no (co-administration study)
Comment: The possible effect of sorafenib on a CYP2C9 substrate was assessed indirectly in patients receiving warfarin. The mean changes from baseline in PT-INR were not higher in NEXAVAR patients compared to placebo patients
Page: -
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
no (co-administration study)
Comment: Ketoconazole (400 mg), a potent inhibitor of CYP3 A4, administered once daily for 7 days did not alter the mean AUC of a single oral 50 mg dose of sorafenib in healthy volunteers. There is no clinical information on the effect of CYP3A4 inducers on the pharmacokinetics of sorafenib. Substances that are inducers of CYP3A4 activity are expected to increase metabolism of sorafenib and thus decrease sorafenib concentrations.
Page: -
no
no
no
no
no
no
no
no
no
no
yes [Km 5.8 uM]
yes
yes
yes
unlikely
Comment: The efflux ratio of sorafenib for transport from basolateral —> apical side to transport from the apical —> basolateral side of Caco-2 cells, ranged from 2.9 to 4.7. Given that sorafenib is highly permeable, the degree of efflux is not expected to result in an effect on overall absorption in man.
Page: -
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Therapy targeted at vascular endothelial growth factor in metastatic renal cell carcinoma: biology, clinical results and future development.
2005 Aug
Safety and pharmacokinetics of the dual action Raf kinase and vascular endothelial growth factor receptor inhibitor, BAY 43-9006, in patients with advanced, refractory solid tumors.
2005 Aug 1
Preclinical and clinical development of the oral multikinase inhibitor sorafenib in cancer treatment.
2005 Dec
Sorafenib: scientific rationales for single-agent and combination therapy in clear-cell renal cell carcinoma.
2005 Dec
Role of tyrosine kinase inhibitors in cancer therapy.
2005 Dec
Cutaneous side-effects of kinase inhibitors and blocking antibodies.
2005 Jul
Gateways to clinical trials.
2005 Jun
Gateways to clinical trials.
2005 Nov
Update on angiogenesis inhibitors.
2005 Nov
Phase I study to determine the safety and pharmacokinetics of the novel Raf kinase and VEGFR inhibitor BAY 43-9006, administered for 28 days on/7 days off in patients with advanced, refractory solid tumors.
2005 Oct
The role of Mcl-1 downregulation in the proapoptotic activity of the multikinase inhibitor BAY 43-9006.
2005 Oct 20
Apoptosis induced by the kinase inhibitor BAY 43-9006 in human leukemia cells involves down-regulation of Mcl-1 through inhibition of translation.
2005 Oct 21
Results of a phase I trial of sorafenib (BAY 43-9006) in combination with oxaliplatin in patients with refractory solid tumors, including colorectal cancer.
2005 Sep
Spinal cord metastasis of a non-neurofibromatosis type-1 malignant peripheral nerve sheath tumor: an unusual manifestation of a rare tumor.
2005 Sep
Promising systemic therapy for renal cell carcinoma.
2005 Sep
Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.
2006
The role of adjuvant therapy in non-metastatic RCC.
2006 Apr
What's new in pancreatic cancer treatment pipeline?
2006 Apr
Molecular targets in melanoma from angiogenesis to apoptosis.
2006 Apr 1
Chemotherapy and targeted therapy combinations in advanced melanoma.
2006 Apr 1
Emerging role of tyrosine kinase inhibitors in the treatment of advanced renal cell cancer: a review.
2006 Aug
Sorafenib is a potent inhibitor of FIP1L1-PDGFRalpha and the imatinib-resistant FIP1L1-PDGFRalpha T674I mutant.
2006 Aug 15
Drug approval triggers debate on future direction for cancer treatments.
2006 Feb
[Progress in therapeutic strategy for renal cell carcinoma].
2006 Feb
The Raf inhibitor BAY 43-9006 (Sorafenib) induces caspase-independent apoptosis in melanoma cells.
2006 Feb 1
[Therapy strategies for advanced renal cell carcinoma].
2006 Jan
Phase I trial of sorafenib and gemcitabine in advanced solid tumors with an expanded cohort in advanced pancreatic cancer.
2006 Jan 1
Targeting Raf-kinase: molecular rationales and translational issues.
2006 Jun
Comparative integromics on VEGF family members.
2006 Jun
Phase II placebo-controlled randomized discontinuation trial of sorafenib in patients with metastatic renal cell carcinoma.
2006 Jun 1
Sorafenib: recent update on activity as a single agent and in combination with interferon-alpha2 in patients with advanced-stage renal cell carcinoma.
2006 Mar
Molecule of the month. Sorafenib.
2006 Mar
Multi-target inhibitors in non-small cell lung cancer (NSCLC).
2006 Mar
VEGF-targeted therapy in renal cell carcinoma: active drugs and active choices.
2006 Mar
Sorafenib.
2006 Mar
Pooled safety analysis of BAY 43-9006 (sorafenib) monotherapy in patients with advanced solid tumours: Is rash associated with treatment outcome?
2006 Mar
BRAF is a therapeutic target in aggressive thyroid carcinoma.
2006 Mar 1
BAY 43-9006 inhibition of oncogenic RET mutants.
2006 Mar 1
Targeted therapy for metastatic renal cell carcinoma.
2006 Mar 13
Mechanisms of hypertension associated with BAY 43-9006.
2006 Mar 20
Treatment for advanced kidney cancer.
2006 Mar-Apr
New drugs: abatacept, sorafenib, and nelarabine.
2006 Mar-Apr
Targeted therapy for cytokine-refractory metastatic renal cell carcinoma, and treatment in the community.
2006 May
Emerging efficacy endpoints for targeted therapies in advanced renal cell carcinoma.
2006 May
Results of a Phase I trial of sorafenib (BAY 43-9006) in combination with doxorubicin in patients with refractory solid tumors.
2006 May
Pharmacodynamic monitoring of BAY 43-9006 (Sorafenib) in phase I clinical trials involving solid tumor and AML/MDS patients, using flow cytometry to monitor activation of the ERK pathway in peripheral blood cells.
2006 May
Lack of effect of ketoconazole-mediated CYP3A inhibition on sorafenib clinical pharmacokinetics.
2006 May
The place of VEGF inhibition in the current management of renal cell carcinoma.
2006 May 8
Isolation and characterization of dominant and recessive IL-3-independent hematopoietic transformants.
2006 Oct 26
Sorafenib is efficacious and tolerated in combination with cytotoxic or cytostatic agents in preclinical models of human non-small cell lung carcinoma.
2007 Feb
Patents

Sample Use Guides

The recommended daily dose of NEXAVAR (tosylate salt of sorafenib) is 400 mg (2 x 200 mg tablets) taken twice daily, without food (at least 1 hour before or 2 hours after eating). Treatment should continue until the patient is no longer clinically benefiting from therapy or until unacceptable toxicity occurs. 432 433 434 435 436 437 438 439 Management of suspected adverse drug reactions may require temporary interruption and/or dose reduction of NEXAVAR therapy. When dose reduction is necessary, the NEXAVAR dose may be reduced to 400 mg once daily. If additional dose reduction is required, NEXAVAR may be reduced to a single 400 mg dose every other day
Route of Administration: Oral
Patient-derived glioblastoma cells with low concentrations of sorafenib caused a dramatic dose dependent inhibition of proliferation (IC(50), 1.5 microM) and induction of apoptosis and autophagy. Sorafenib inhibited phosphorylation of signal transducer and activator of transcription 3 (Stat3) and expression of cyclins, D and E. In contrast, AKT was not modulated by sorafenib
Name Type Language
SORAFENIB
EMA EPAR   INN   MART.   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
SORAFENIB [USAN]
Common Name English
SORAFENIB [MART.]
Common Name English
SORAFENIB [EMA EPAR]
Common Name English
SORAFENIB [WHO-DD]
Common Name English
2-PYRIDINECARBOXAMIDE, 4-(4-((((4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL)AMINO)CARBONYL)AMINO)PHENOXY)-N-METHYL-
Systematic Name English
BAY 43-9006
Code English
SORAFENIB [MI]
Common Name English
4-(4-(3-(4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL)UREIDO)PHENOXY)-N(SUP 2)-METHYLPYRIDINE-2-CARBOXAMIDE
Systematic Name English
SORAFENIB [VANDF]
Common Name English
BAY-43-9006
Code English
SORAFENIB [INN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
WHO-VATC QL01XE05
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
NCI_THESAURUS C1742
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
WHO-ATC L01XE05
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
NDF-RT N0000175076
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
FDA ORPHAN DRUG 220206
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
FDA ORPHAN DRUG 185204
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
EMA ASSESSMENT REPORTS NEXAVAR (AUTHORIZED: CARCINOMA, HEPATOCELLULAR, CARINOMA, RENAL CELL)
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
FDA ORPHAN DRUG 675918
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
FDA ORPHAN DRUG 320310
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
LIVERTOX 894
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
FDA ORPHAN DRUG 229206
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
NCI_THESAURUS C1404
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
Code System Code Type Description
INN
8234
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
RXCUI
495881
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY RxNorm
LACTMED
Sorafenib
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
NCI_THESAURUS
C61948
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
MESH
C471405
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
PUBCHEM
216239
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
EPA CompTox
284461-73-0
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
WIKIPEDIA
SORAFENIB
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
ChEMBL
CHEMBL1336
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
HSDB
8173
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
IUPHAR
5711
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
DRUG BANK
DB00398
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
DRUG CENTRAL
2459
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
FDA UNII
9ZOQ3TZI87
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
MERCK INDEX
M10116
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY Merck Index
CAS
284461-73-0
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY
EVMPD
SUB23139
Created by admin on Sat Jun 26 08:06:26 UTC 2021 , Edited by admin on Sat Jun 26 08:06:26 UTC 2021
PRIMARY