Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H14Cl2N2O3S |
Molecular Weight | 421.297 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(=O)(=O)C1=CC(Cl)=C(C=C1)C(=O)NC2=CC=C(Cl)C(=C2)C3=CC=CC=N3
InChI
InChIKey=BPQMGSKTAYIVFO-UHFFFAOYSA-N
InChI=1S/C19H14Cl2N2O3S/c1-27(25,26)13-6-7-14(17(21)11-13)19(24)23-12-5-8-16(20)15(10-12)18-4-2-3-9-22-18/h2-11H,1H3,(H,23,24)
Molecular Formula | C19H14Cl2N2O3S |
Molecular Weight | 421.297 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/24857041
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/24857041
Vismodegib (trade name Erivedge) is a drug for the treatment of basal-cell carcinoma (BCC). It was approved by FDA on January 30, 2012 and by the European Commission on 12 July 2013, for the treatment of adult patients with symptomatic metastatic BCC, or locally advanced BCC inappropriate for surgery or radiotherapy. The drug is also undergoing clinical trials for metastatic colorectal cancer, small-cell lung cancer, advanced stomach cancer, pancreatic cancer, medulloblastoma and chondrosarcoma as of June 2011. The substance acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. The Hedgehog signaling pathway plays an important role in tissue growth and repair; aberrant constitutive activation of Hedgehog pathway signaling and uncontrolled cellular proliferation may be associated with mutations in the Hedgehog-ligand cell surface receptors PTCH and SMO. SMO inhibition causes the transcription factors GLI1 and GLI2 to remain inactive, which prevents the expression of tumor mediating genes within the hedgehog pathway. This pathway is pathogenetically relevant in more than 90% of basal-cell carcinomas.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5971 Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=19443052 |
3.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ERIVEDGE Approved UseERIVEDGE capsule is indicated for the treatment of adults with metastatic basal cell carcinoma, or with locally advanced basal cell carcinoma that has recurred following surgery or who are not candidates for surgery, and who are not candidates for radiation. Launch Date2012 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5.95 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22458643 |
150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VISMODEGIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2850 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22458643 |
150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VISMODEGIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11.3 day EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22458643 |
150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VISMODEGIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.45% |
VISMODEGIB plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
170 mg/m2 1 times / day multiple, oral Dose: 170 mg/m2, 1 times / day Route: oral Route: multiple Dose: 170 mg/m2, 1 times / day Sources: |
unhealthy, 11.6 years (range: 4.4–21 years) n = 7 Health Status: unhealthy Condition: Medulloblastoma Age Group: 11.6 years (range: 4.4–21 years) Sex: M+F Population Size: 7 Sources: |
DLT: Gamma-glutamyltransferase increased... Dose limiting toxicities: Gamma-glutamyltransferase increased (grade 3) Sources: |
150 mg 1 times / day multiple, oral Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
unhealthy, 14.5 years (range: 3.9–20.3 years) n = 10 Health Status: unhealthy Condition: Medulloblastoma Age Group: 14.5 years (range: 3.9–20.3 years) Sex: M+F Population Size: 10 Sources: |
DLT: Hypokalemia... |
300 mg 1 times / day multiple, oral Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, 14.5 years (range: 3.9–20.3 years) n = 10 Health Status: unhealthy Condition: Medulloblastoma Age Group: 14.5 years (range: 3.9–20.3 years) Sex: M+F Population Size: 10 Sources: |
DLT: Thrombocytopenia... Dose limiting toxicities: Thrombocytopenia (grade 3) Sources: |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Other AEs: Nausea, Nausea... Other AEs: Nausea (grade 1-2, 29.7%) Sources: Nausea (grade 3, 0.7%) Diarrhea (grade 1-2, 28.3%) Diarrhea (grade 3, 0.7%) Constipation (grade 1-2, 21%) Vomiting (grade 1-2, 13.8%) Fatigue (grade 1-2, 34.1%) Fatigue (grade 3, 5.1%) Fatigue (grade 4, 0.7%) Weight loss (grade 1-2, 42.2%) Weight loss (grade 3, 7.2%) Decreased appetite (grade 1-2, 23.2%) Decreased appetite (grade 3, 2.2%) Muscle spasms (grade 1-2, 68.1%) Muscle spasms (grade 3, 3.6%) Arthralgia (grade 1-2, 15.2%) Arthralgia (grade 3, 0.7%) Dysgeusia (grade 1-2, 55.1%) Ageusia (grade 1-2, 10.9%) Alopecia (grade 1-2, 63.8%) Hyponatremia (grade 3, 4%) Hypokalemia (grade 3, 1%) Azotemia (grade 3, 2%) |
540 mg single, oral Highest studied dose Dose: 540 mg Route: oral Route: single Dose: 540 mg Sources: |
unhealthy, adult n = 4 Health Status: unhealthy Condition: locally advanced or metastatic basal cell carcinoma Age Group: adult Population Size: 4 Sources: |
|
150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
pregnant Health Status: pregnant Sources: |
Other AEs: Birth defects... Other AEs: Birth defects (grade 5|severe) Sources: |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy n = 10 Health Status: unhealthy Sex: F Population Size: 10 Sources: |
Other AEs: Amenorrhea... Other AEs: Amenorrhea (3 patients) Sources: |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Disc. AE: Metastatic malignant melanoma, Ischaemic stroke... AEs leading to discontinuation/dose reduction: Metastatic malignant melanoma (grade 4, 1 patient) Sources: Page: p. 91Ischaemic stroke (grade 3, 1 patient) Fatigue (grade 3, 1 patient) Muscle spasms (grade 3, 2 patients) Metastatic squamous cell carcinoma (grade 4, 1 patient) Acute myocardial infarction (grade 5, 1 patient) Dysgeusia (grade 1, 1 patient) Weight decreased (grade 2, 1 patient) Asthenia (grade 3, 1 patient) Aphagia (grade 3, 1 patient) Paraesthesia (grade 2, 1 patient) Cellulitis (grade 3, 1 patient) Hypovolaemic shock (grade 5, 1 patient) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Gamma-glutamyltransferase increased | grade 3 DLT |
170 mg/m2 1 times / day multiple, oral Dose: 170 mg/m2, 1 times / day Route: oral Route: multiple Dose: 170 mg/m2, 1 times / day Sources: |
unhealthy, 11.6 years (range: 4.4–21 years) n = 7 Health Status: unhealthy Condition: Medulloblastoma Age Group: 11.6 years (range: 4.4–21 years) Sex: M+F Population Size: 7 Sources: |
Hypokalemia | grade 4 DLT |
150 mg 1 times / day multiple, oral Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
unhealthy, 14.5 years (range: 3.9–20.3 years) n = 10 Health Status: unhealthy Condition: Medulloblastoma Age Group: 14.5 years (range: 3.9–20.3 years) Sex: M+F Population Size: 10 Sources: |
Thrombocytopenia | grade 3 DLT |
300 mg 1 times / day multiple, oral Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, 14.5 years (range: 3.9–20.3 years) n = 10 Health Status: unhealthy Condition: Medulloblastoma Age Group: 14.5 years (range: 3.9–20.3 years) Sex: M+F Population Size: 10 Sources: |
Ageusia | grade 1-2, 10.9% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Vomiting | grade 1-2, 13.8% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Arthralgia | grade 1-2, 15.2% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Constipation | grade 1-2, 21% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Decreased appetite | grade 1-2, 23.2% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Diarrhea | grade 1-2, 28.3% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Nausea | grade 1-2, 29.7% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Fatigue | grade 1-2, 34.1% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Weight loss | grade 1-2, 42.2% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Dysgeusia | grade 1-2, 55.1% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Alopecia | grade 1-2, 63.8% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Muscle spasms | grade 1-2, 68.1% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Arthralgia | grade 3, 0.7% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Diarrhea | grade 3, 0.7% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Nausea | grade 3, 0.7% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Hypokalemia | grade 3, 1% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Azotemia | grade 3, 2% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Decreased appetite | grade 3, 2.2% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Muscle spasms | grade 3, 3.6% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Hyponatremia | grade 3, 4% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Fatigue | grade 3, 5.1% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Weight loss | grade 3, 7.2% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Fatigue | grade 4, 0.7% | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy, 61 years (range: 21 - 101 years) n = 138 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Age Group: 61 years (range: 21 - 101 years) Sex: M+F Population Size: 138 Sources: |
Birth defects | grade 5|severe | 150 mg 1 times / day multiple, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: |
pregnant Health Status: pregnant Sources: |
Amenorrhea | 3 patients | 150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy n = 10 Health Status: unhealthy Sex: F Population Size: 10 Sources: |
Dysgeusia | grade 1, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Paraesthesia | grade 2, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Weight decreased | grade 2, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Aphagia | grade 3, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Asthenia | grade 3, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Cellulitis | grade 3, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Fatigue | grade 3, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Ischaemic stroke | grade 3, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Muscle spasms | grade 3, 2 patients Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Metastatic malignant melanoma | grade 4, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Metastatic squamous cell carcinoma | grade 4, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Acute myocardial infarction | grade 5, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Hypovolaemic shock | grade 5, 1 patient Disc. AE |
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: Page: p. 91 |
unhealthy n = 104 Health Status: unhealthy Condition: Advanced Basal Cell Carcinoma Sex: M+F Population Size: 104 Sources: Page: p. 91 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=46 Page: 46.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=46 Page: 46.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=46 Page: 46.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=21 Page: 21.0 |
yes | no (co-administration study) Comment: the steady state concentrations of total and unbound vismodegib for patients taking a P-gp inhibitor concomitantly with vismodegib were within the range of concentrations of patients taking vismodegib alone. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=21 Page: 21.0 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=21 Page: 21.0 |
yes | unlikely Comment: Vismodegib was identified to be a substrate of CYP2C9 and CYP3A4; however, CYP inhibition would unlikely alter vismodegib concentrations because of its slow elimination via multiple pathways, including minor metabolism by several CYPs and main excretion of unchanged drug. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=21 Page: 21.0 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=21 Page: 21.0 |
yes | unlikely Comment: Vismodegib was identified to be a substrate of CYP2C9 and CYP3A4; however, CYP inhibition would unlikely alter vismodegib concentrations because of its slow elimination via multiple pathways, including minor metabolism by several CYPs and main excretion of unchanged drug. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=21 Page: 21.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000ClinPharmR.pdf#page=37 Page: 37.0 |
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 16:57:58 GMT 2023
by
admin
on
Sat Dec 16 16:57:58 GMT 2023
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Record UNII |
25X868M3DS
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C2189
Created by
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NBK548629
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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EMA ASSESSMENT REPORTS |
ERIVEDGE (AUTHORIZED: CARCINOMA, BASAL CELL)
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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NDF-RT |
N0000184149
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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WHO-ATC |
L01XX43
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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WHO-VATC |
QL01XX43
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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Code System | Code | Type | Description | ||
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879085-55-9
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admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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PRIMARY | |||
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DB08828
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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4227
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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8130
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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25X868M3DS
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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SUB32354
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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9311
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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WW-37
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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m11477
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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PRIMARY | Merck Index | ||
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N0000184148
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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PRIMARY | Smoothened Receptor Antagonists [MoA] | ||
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24776445
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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DTXSID40236689
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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66903
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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100000124371
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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Vismodegib
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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755986
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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747691
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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PRIMARY | |||
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CHEMBL473417
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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1242987
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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PRIMARY | RxNorm | ||
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6975
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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Vismodegib
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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25X868M3DS
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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C74038
Created by
admin on Sat Dec 16 16:57:59 GMT 2023 , Edited by admin on Sat Dec 16 16:57:59 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR |
IC50
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METABOLIC ENZYME -> SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE -> PARENT |
MINOR
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METABOLITE -> PARENT |
MINOR
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METABOLITE -> PARENT |
MINOR
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METABOLITE -> PARENT |
MINOR
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METABOLITE -> PARENT |
MINOR
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METABOLITE -> PARENT |
MINOR
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METABOLITE -> PARENT |
MINOR
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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SINGLE DOSE |
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Volume of Distribution | PHARMACOKINETIC |
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