Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H15ClF4N4O3.H2O |
Molecular Weight | 500.831 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.CNC(=O)C1=NC=CC(OC2=CC(F)=C(NC(=O)NC3=CC=C(Cl)C(=C3)C(F)(F)F)C=C2)=C1
InChI
InChIKey=ZOPOQLDXFHBOIH-UHFFFAOYSA-N
InChI=1S/C21H15ClF4N4O3.H2O/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26;/h2-10H,1H3,(H,27,31)(H2,29,30,32);1H2
DescriptionCurator's Comment: description was created based on several sources, including
http://www.news-medical.net/news/20140220/Bayer-enrolls-patients-for-Phase-III-trial-of-Stivarga-(regorafenib)-tablets-in-colorectal-cancer.aspx; http://www.ncbi.nlm.nih.gov/pubmed/?term=21170960
Curator's Comment: description was created based on several sources, including
http://www.news-medical.net/news/20140220/Bayer-enrolls-patients-for-Phase-III-trial-of-Stivarga-(regorafenib)-tablets-in-colorectal-cancer.aspx; http://www.ncbi.nlm.nih.gov/pubmed/?term=21170960
Regorafenib (trade name Stivarga) is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor cell signaling. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model, and inhibition of tumor growth as well as anti-metastatic activity in several mouse xenograft models including some for human colorectal carcinoma. Since 2009 it was studied as a potential treatment option in multiple tumor types. Stivarga is approved by FDA to treat two different tumor types: metastatic colorectal cancer in patients who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy (approved in 2012) and to treat patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor who have been previously treated with imatinib mesylate and sunitinib malate (approved in 2013).
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P04049 Gene ID: 5894.0 Gene Symbol: RAF1 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=21170960 |
2.5 nM [IC50] | ||
Target ID: P07949 Gene ID: 5979.0 Gene Symbol: RET Target Organism: Homo sapiens (Human) |
1.5 nM [IC50] | ||
Target ID: P35968 Gene ID: 3791.0 Gene Symbol: KDR Target Organism: Homo sapiens (Human) |
4.2 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Secondary | STIVARGA Approved UseIndicated for the treatment of patients with: metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy; locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate. Launch Date2012 |
|||
Secondary | STIVARGA Approved UseIndicated for the treatment of patients with: metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy; locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate. Launch Date2012 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2522.2 μg/L EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23553067 |
160 mg 1 times / day steady-state, oral dose: 160 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
REGORAFENIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
33042.8 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23553067 |
160 mg 1 times / day steady-state, oral dose: 160 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
REGORAFENIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
30.4 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23553067 |
160 mg 1 times / day steady-state, oral dose: 160 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
REGORAFENIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.5% |
REGORAFENIB plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: |
Disc. AE: Hepatic failure... AEs leading to discontinuation/dose reduction: Hepatic failure (grade 5, 1.6%) Sources: |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
Disc. AE: General physical health deterioration, Palmar-plantar erythrodysaesth.... AEs leading to discontinuation/dose reduction: General physical health deterioration (4%) Sources: Page: 203085Orig1s000MedR.pdf - p.47Palmar-plantar erythrodysaesth. (1%) Decreased appetite (1%) Pneumonia (1%) Rash (1%) |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
Disc. AE: Palmar-plantar erythrodysaesth., Diarrhea... AEs leading to discontinuation/dose reduction: Palmar-plantar erythrodysaesth. (18.2%) Sources: Page: 203085Orig1s000MedR.pdf - p.48Diarrhea (3.8%) Hypertension (3.2%) Fatigue (2%) Rash (2%) Mucositis (1.2%) Abdominal pain (1%) Asthenia (1%) |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Disc. AE: Palmar-plantar erythrodysaesth., Diarrhea... AEs leading to discontinuation/dose reduction: Palmar-plantar erythrodysaesth. (18.8%) Sources: Page: 203085Orig1s000MedR.pdf - p.49Diarrhea (6.2%) Pyrexia (4.6%) Fatigue (4%) Rash (3.6%) Hyperbilirubinemia (3.6%) Decreased appetite (3%) Asthenia (2.8%) Hypertension (2.6%) Abdominal pain (2.4%) Stomatitis (2.2%) Dyspnea (2%) AST increased (1.8%) Vomiting (1.8%) Thrombocytopenia (1.6%) ALT increased (1.4%) Proteinuria (1.2%) |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
Other AEs: Hemorrhage, Hemorrhage... Other AEs: Hemorrhage (grade 1, 17.4%) Sources: Page: 203085Orig1s000MedR.pdf - p.53Hemorrhage (grade 2, 1.8%) Hemorrhage (grade 3, 1.4%) Hemorrhage (grade 5, 0.8%) |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.54 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.54 |
Other AEs: Palmar-plantar erythrodysaesth., Rash... Other AEs: Palmar-plantar erythrodysaesth. (grade 3, 17%) Sources: Page: 203085Orig1s000MedR.pdf - p.54Rash (grade 3, 5%) |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.57 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.57 |
Other AEs: Pulmonary embolism, Venous thromboembolism... Other AEs: Pulmonary embolism (grade 3, 0.8%) Sources: Page: 203085Orig1s000MedR.pdf - p.57Venous thromboembolism (grade 3, 0.6%) Arterial thromboembolism (grade 3, 1%) |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Other AEs: Decreased appetite, Diarrhea... Other AEs: Decreased appetite (grade 3, 5%) Sources: Page: 203085Orig1s000MedR.pdf - p.59Diarrhea (grade 3, 8%) Mucositis (grade 3, 4%) Weight loss (grade 3, <1%) Infection (grade 3, 9%) Hypertension (grade 3, 8%) Pain (grade 3, 3%) Fever (grade 3, 2%) Rash (grade 3, 6%) Hemorrhage (grade 3, 2%) Headache (grade 3, <1%) Asthenia (grade 3, 15%) |
220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Other AEs: Dysphonia, Dry mouth... Other AEs: Dysphonia Sources: Dry mouth Decreased appetite Voice alteration (75%) Hand and foot skin reaction (58%) Mucositis (67%) Diarrhea (58%) Hypertension (42%) Fatigue (58%) Anorexia (42%) Rash (25%) Alopecia (25%) Voice alteration (grade 3, 8%) Hand and foot skin reaction (grade 3, 42%) Diarrhea (grade 3, 8%) Hypertension (grade 3, 25%) Fatigue (grade 3, 8%) Rash (grade 3, 8%) |
160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Other AEs: Voice alteration, Hand and foot skin reaction... Other AEs: Voice alteration (42%) Sources: Hand and foot skin reaction (67%) Mucositis (25%) Diarrhea (50%) Hypertension (50%) Fatigue (17%) Anorexia (50%) Rash (50%) Alopecia (33%) Hand and foot skin reaction (grade 3, 25%) Mucositis (grade 3, 8%) Diarrhea (grade 3, 17%) Hypertension (grade 3, 17%) Anorexia (grade 3, 8%) Rash (grade 3, 8%) |
120 mg 1 times / day multiple, oral Studied dose Dose: 120 mg, 1 times / day Route: oral Route: multiple Dose: 120 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 8 Sources: |
DLT: Infection, Hand and foot skin reaction... Dose limiting toxicities: Infection (25%) Sources: Hand and foot skin reaction (13%) |
160 mg 1 times / day multiple, oral Studied dose Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
DLT: Allergic reaction, Vomiting... Dose limiting toxicities: Allergic reaction (8%) Sources: Vomiting (8%) |
220 mg 1 times / day multiple, oral Studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
DLT: Hand and foot skin reaction, Pruritic rash... Dose limiting toxicities: Hand and foot skin reaction (17%) Sources: Pruritic rash (8%) Abdominal pain (8%) Asthma bronchial (8%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Hepatic failure | grade 5, 1.6% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: |
Decreased appetite | 1% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
Palmar-plantar erythrodysaesth. | 1% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
Pneumonia | 1% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
Rash | 1% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
General physical health deterioration | 4% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.47 |
Abdominal pain | 1% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
Asthenia | 1% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
Mucositis | 1.2% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
Palmar-plantar erythrodysaesth. | 18.2% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
Fatigue | 2% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
Rash | 2% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
Hypertension | 3.2% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
Diarrhea | 3.8% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.48 |
Proteinuria | 1.2% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
ALT increased | 1.4% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Thrombocytopenia | 1.6% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
AST increased | 1.8% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Vomiting | 1.8% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Palmar-plantar erythrodysaesth. | 18.8% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Dyspnea | 2% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Stomatitis | 2.2% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Abdominal pain | 2.4% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Hypertension | 2.6% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Asthenia | 2.8% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Decreased appetite | 3% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Hyperbilirubinemia | 3.6% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Rash | 3.6% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Fatigue | 4% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Pyrexia | 4.6% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Diarrhea | 6.2% Disc. AE |
160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.49 |
Hemorrhage | grade 1, 17.4% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
Hemorrhage | grade 2, 1.8% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
Hemorrhage | grade 3, 1.4% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
Hemorrhage | grade 5, 0.8% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.53 |
Palmar-plantar erythrodysaesth. | grade 3, 17% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.54 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.54 |
Rash | grade 3, 5% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.54 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.54 |
Venous thromboembolism | grade 3, 0.6% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.57 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.57 |
Pulmonary embolism | grade 3, 0.8% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.57 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.57 |
Arterial thromboembolism | grade 3, 1% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.57 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.57 |
Asthenia | grade 3, 15% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Fever | grade 3, 2% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Hemorrhage | grade 3, 2% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Pain | grade 3, 3% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Mucositis | grade 3, 4% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Decreased appetite | grade 3, 5% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Rash | grade 3, 6% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Diarrhea | grade 3, 8% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Hypertension | grade 3, 8% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Infection | grade 3, 9% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Headache | grade 3, <1% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Weight loss | grade 3, <1% | 160 mg 1 times / day multiple, oral Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
unhealthy, 22 to 82 years n = 500 Health Status: unhealthy Condition: colorectal cancer Age Group: 22 to 82 years Sex: M+F Population Size: 500 Sources: Page: 203085Orig1s000MedR.pdf - p.59 |
Decreased appetite | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
|
Dry mouth | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
|
Dysphonia | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
|
Alopecia | 25% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Rash | 25% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Anorexia | 42% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hypertension | 42% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Diarrhea | 58% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Fatigue | 58% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hand and foot skin reaction | 58% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Mucositis | 67% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Voice alteration | 75% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hypertension | grade 3, 25% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hand and foot skin reaction | grade 3, 42% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Diarrhea | grade 3, 8% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Fatigue | grade 3, 8% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Rash | grade 3, 8% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Voice alteration | grade 3, 8% | 220 mg 1 times / day multiple, oral Highest studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Fatigue | 17% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Mucositis | 25% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Alopecia | 33% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Voice alteration | 42% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Anorexia | 50% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Diarrhea | 50% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hypertension | 50% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Rash | 50% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hand and foot skin reaction | 67% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Diarrhea | grade 3, 17% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hypertension | grade 3, 17% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hand and foot skin reaction | grade 3, 25% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Anorexia | grade 3, 8% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Mucositis | grade 3, 8% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Rash | grade 3, 8% | 160 mg 1 times / day multiple, oral MTD|Recommended Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hand and foot skin reaction | 13% DLT |
120 mg 1 times / day multiple, oral Studied dose Dose: 120 mg, 1 times / day Route: oral Route: multiple Dose: 120 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 8 Sources: |
Infection | 25% DLT |
120 mg 1 times / day multiple, oral Studied dose Dose: 120 mg, 1 times / day Route: oral Route: multiple Dose: 120 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 8 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 8 Sources: |
Allergic reaction | 8% DLT |
160 mg 1 times / day multiple, oral Studied dose Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Vomiting | 8% DLT |
160 mg 1 times / day multiple, oral Studied dose Dose: 160 mg, 1 times / day Route: oral Route: multiple Dose: 160 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Hand and foot skin reaction | 17% DLT |
220 mg 1 times / day multiple, oral Studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Abdominal pain | 8% DLT |
220 mg 1 times / day multiple, oral Studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Asthma bronchial | 8% DLT |
220 mg 1 times / day multiple, oral Studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Pruritic rash | 8% DLT |
220 mg 1 times / day multiple, oral Studied dose Dose: 220 mg, 1 times / day Route: oral Route: multiple Dose: 220 mg, 1 times / day Sources: |
unhealthy, median age 60 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: median age 60 years Sex: M+F Population Size: 12 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes [IC50 44.7 uM] | ||||
yes [Ki 0.6 uM] | unknown Comment: The effect of regorafenib on the PK of CYP2C8, CYP2C9, CYP2C19 and CYP3A4 probe substrates are being evaluated in an ongoing study. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203085Orig1s000ClinPharmR.pdf#page=9 Page: - |
|||
yes [Ki 11.1 uM] | unknown Comment: The effect of regorafenib on the PK of CYP2C8, CYP2C9, CYP2C19 and CYP3A4 probe substrates are being evaluated in an ongoing study. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203085Orig1s000ClinPharmR.pdf#page=29 Page: - |
|||
yes [Ki 16.4 uM] | unknown Comment: Acts via metabolite M2. The effect of regorafenib on the PK of CYP2C8, CYP2C9, CYP2C19 and CYP3A4 probe substrates are being evaluated in an ongoing study. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203085Orig1s000ClinPharmR.pdf#page=9 Page: - |
|||
yes [Ki 2.1 uM] | ||||
yes [Ki 3 uM] | ||||
yes [Ki 4.7 uM] | unknown Comment: The effect of regorafenib on the PK of CYP2C8, CYP2C9, CYP2C19 and CYP3A4 probe substrates are being evaluated in an ongoing study. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203085Orig1s000ClinPharmR.pdf#page=9 Page: - |
|||
yes [Ki 7.8 uM] | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | ||||
major | yes (co-administration study) Comment: The administration of ketoconazole 400 mg daily for 18 days with a single 160 mg dose of regorafenib increased the mean AUC of regorafenib by 33% and decreased the mean AUC of M2 and M5 each by 93%. The administration of rifampin 600 mg daily for 9 days with a single 160 mg dose of regorafenib decreased the mean AUC of regorafenib by 50% and increased the mean AUC of M5 by 264%; the mean AUC of M2 was similar with and without rifampin. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203085Orig1s000ClinPharmR.pdf#page=9 Page: - |
|||
no | ||||
no | ||||
no | ||||
no | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sample Use Guides
160 mg Stivarga orally, once daily for the first 21 days of each 28-day cycle. Take with a low-fat meal.
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=24347491
For the migration inhibition assay, human lymphatic endothelial cells (LECs) were grown overnight on a gelatin-coated six-well plate, serum starved for 6 hr in EBM-2 media containing 0.1% BSA and treated with 100 nmol/L regorafenib for 1 hr. Regorafenib inhibited the proliferation of 19 cell lines derived from human colon cancers, with IC50 values ranging from 2.6 to 10 umol/L.
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24768591
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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300000039151
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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1371319
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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1019206-88-2
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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DTXSID70144349
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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68646
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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MGN125FS9D
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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DBSALT001750
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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AB-31
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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1600201
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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MGN125FS9D
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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C184955
Created by
admin on Sat Dec 16 05:14:24 GMT 2023 , Edited by admin on Sat Dec 16 05:14:24 GMT 2023
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