U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
Structure of VISMODEGIB

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)

HIDE SMILES / InChI
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

Description
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

2012
618
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8228
 3.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8360
ERIVEDGE

Approved Use

ERIVEDGE 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 Date

1.32788165E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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

AUC

ValueDoseCo-administeredAnalytePopulation
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

T1/2

ValueDoseCo-administeredAnalytePopulation
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

Funbound

ValueDoseCo-administeredAnalytePopulation
0.45%
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/21753154/
VISMODEGIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse 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:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://pubmed.ncbi.nlm.nih.gov/24077351
DLT: Gamma-glutamyltransferase increased...
Dose limiting toxicities:
Gamma-glutamyltransferase increased (grade 3)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24077351
150 mg 1 times / day multiple, oral
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://pubmed.ncbi.nlm.nih.gov/24077351
DLT: Hypokalemia...
Dose limiting toxicities:
Hypokalemia (grade 4)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24077351
300 mg 1 times / day multiple, oral
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://pubmed.ncbi.nlm.nih.gov/24077351
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 3)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
Other AEs: Nausea, Nausea...
Other AEs:
Nausea (grade 1-2, 29.7%)
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%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
540 mg single, oral
Highest studied dose
Dose: 540 mg
Route: oral
Route: single
Dose: 540 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/21300760
https://pubmed.ncbi.nlm.nih.gov/21300762
unhealthy, adult
n = 4
Health Status: unhealthy
Condition: locally advanced or metastatic basal cell carcinoma
Age Group: adult
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/21300760
https://pubmed.ncbi.nlm.nih.gov/21300762
Sources:
https://pubmed.ncbi.nlm.nih.gov/21300760
https://pubmed.ncbi.nlm.nih.gov/21300762
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
pregnant
Health Status: pregnant
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
Other AEs: Birth defects...
Other AEs:
Birth defects (grade 5|severe)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
unhealthy
n = 10
Health Status: unhealthy
Sex: F
Population Size: 10
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
Other AEs: Amenorrhea...
Other AEs:
Amenorrhea (3 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
Disc. AE: Metastatic malignant melanoma, Ischaemic stroke...
AEs leading to
discontinuation/dose reduction:
Metastatic malignant melanoma (grade 4, 1 patient)
Ischaemic 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)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
AEs

AEs

AESignificanceDosePopulation
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:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://pubmed.ncbi.nlm.nih.gov/24077351
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
pregnant
Health Status: pregnant
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
unhealthy
n = 10
Health Status: unhealthy
Sex: F
Population Size: 10
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203388lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
unhealthy
n = 104
Health Status: unhealthy
Condition: Advanced Basal Cell Carcinoma
Sex: M+F
Population Size: 104
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000MedRpdf.pdf
Page: p. 91
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1010

inhibitor
1752
substrate
1193
inhibitor
1599

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C8
901

CYP2C19
1463

P-gp
1437

BCRP
691
CYP3A4/5
85

P-gp
1527

CYP2C18
139

CYP2C19
985
CYP1A2
689

CYP2B6
538

CYP3A4/5
120
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1673
 inconclusive
CYP2B6
985
 inconclusive
CYP3A4/5
330
 inconclusive
PXR
45
 no [IC50 83.3 uM]
P-gp
1626
 no
CYP2C19
1537
 yes
CYP2C9
1803
 yes
CYP2C8
955
 yes
no (co-administration study)
Comment: In vivo studies indicate that there was no clinically meaningful difference in the pharmacokinetics of rosiglitazone, a CYP2C8 substrate, ethinyl estradiol, or norethindrone when co-administered with vismodegib.
Page: 21.0
BCRP
765
 yes
unlikely
Comment: The applicant states that this finding is unlikely to be of clinical relevance due to the high degree of plasma protein binding of vismodegib and the low confirmed clinical occurrence of BCRP based drug-drug interactions.
Page: 57.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2C18
139
 yes
CYP2C19
985
 yes
CYP2D6
1193
 yes
P-gp
1527
 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.
Page: 21.0
CYP2C9
1010
 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.
Page: 21.0
CYP3A4/5
85
 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.
Page: 21.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1632
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:66903
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:66903
ChemicalBook
CB52500590
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB52500590
MolPort
MolPort-009-679-417
https://www.molport.com/shop/molecule-link/MolPort-009-679-417
MolPort
MolPort-047-116-774
https://www.molport.com/shop/molecule-link/MolPort-047-116-774
Selleck Chemicals
GDC-0449
http://www.selleckchem.com/products/GDC-0449.html
ZINC
ZINC000040899447
http://zinc15.docking.org/substances/ZINC000040899447
eMolecules
32176457
https://www.emolecules.com/cgi-bin/more?vid=32176457
PubMed

PubMed

TitleDatePubMed
Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition.
2014 Jul
Patents

Patents

07888364
20
20060063779
1
JP2012500853A
1

Sample Use Guides

In Vivo Use Guide
150 mg orally once daily
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Thu Jul 06 22:24:01 UTC 2023
Edited
by admin
on Thu Jul 06 22:24:01 UTC 2023
Record UNII
25X868M3DS
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
VISMODEGIB
DASH   INN   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
GDC-0449
Code English
ERIVEDGE
Brand Name English
vismodegib [INN]
Common Name English
VISMODEGIB [VANDF]
Common Name English
Vismodegib [WHO-DD]
Common Name English
2-CHLORO-N-(4-CHLORO-3-PYRIDIN-2-YL)PHENYL)-4-(METHYLSULFONYL)BENZAMIDE
Common Name English
BENZAMIDE, 2-CHLORO-N-(4-CHLORO-3-(2-PYRIDINYL)PHENYL)-4-(METHYLSULFONYL)-
Systematic Name English
NSC-755986
Code English
VISMODEGIB [USAN]
Common Name English
NSC-747691
Code English
VISMODEGIB [MI]
Common Name English
VISMODEGIB [ORANGE BOOK]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C2189
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
LIVERTOX NBK548629
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
EMA ASSESSMENT REPORTS ERIVEDGE (AUTHORIZED: CARCINOMA, BASAL CELL)
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
NDF-RT N0000184149
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
WHO-ATC L01XX43
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
WHO-VATC QL01XX43
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
Code System Code Type Description
CAS
879085-55-9
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
DRUG BANK
DB08828
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
DRUG CENTRAL
4227
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
HSDB
8130
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
DAILYMED
25X868M3DS
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
EVMPD
SUB32354
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
INN
9311
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
USAN
WW-37
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
MERCK INDEX
M11477
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY Merck Index
NDF-RT
N0000184148
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY Smoothened Receptor Antagonists [MoA]
PUBCHEM
24776445
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
EPA CompTox
DTXSID40236689
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
CHEBI
66903
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
SMS_ID
100000124371
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
WIKIPEDIA
Vismodegib
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
NSC
755986
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
NSC
747691
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
ChEMBL
CHEMBL473417
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
RXCUI
1242987
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY RxNorm
IUPHAR
6975
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
LACTMED
Vismodegib
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
FDA UNII
25X868M3DS
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
NCI_THESAURUS
C74038
Created by admin on Thu Jul 06 22:24:02 UTC 2023 , Edited by admin on Thu Jul 06 22:24:02 UTC 2023
PRIMARY
Related Record Type Details
CYTOCHROME P450 3A5
METABOLIC ENZYME -> SUBSTRATE
MINOR
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MINOR
SMOOTHENED HOMOLOG
TARGET -> INHIBITOR
IC50
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 2C9
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
Structure of 2-CHLORO-N-(4-CHLORO-3-HYDROXY-5-(2-PYRIDINYL)PHENYL)-4-(METHYLSULFONYL)BENZAMIDE
METABOLITE -> PARENT
MINOR
Structure of 4-(2-CHLORO-5-((2-CHLORO-4-(METHYLSULFONYL)BENZOYL)AMINO)PHENYL)-4-(FORMYLAMINO)-3-BUTENOIC ACID
METABOLITE -> PARENT
MINOR
Structure of 2-CHLORO-N-(4-CHLORO-2-HYDROXY-3-(2-PYRIDINYL)PHENYL)-4-(METHYLSULFONYL)BENZAMIDE
METABOLITE -> PARENT
MINOR
Structure of 6-(2-CHLORO-5-((2-CHLORO-4-(METHYLSULFONYL)BENZOYL)AMINO)PHENYL)-3-PYRIDINYL-.BETA.-D-GLUCOPYRANOSIDURONIC ACID
METABOLITE -> PARENT
MINOR
Structure of 2-CHLORO-N-(4-CHLORO-3-(5-HYDROXY-2-PYRIDINYL)PHENYL)-4-(METHYLSULFONYL) BENZAMIDE
METABOLITE -> PARENT
MINOR
Structure of 2-CHLORO-5-((2-CHLORO-4-(METHYLSULFONYL)BENZOYL)AMINO)-3-(2-PYRIDINYL)PHENYL-.BETA.-D-GLUCOPYRANOSIDURONIC ACID
METABOLITE -> PARENT
MINOR
Structure of 2-CHLORO-5-((2-CHLORO-4-(METHYLSULFONYL)BENZOYL)AMINO)-.GAMMA.-OXO-BENZENEBUTANOIC ACID
METABOLITE -> PARENT
MINOR
Related Record Type Details
Structure of VISMODEGIB
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC SINGLE DOSE

Volume of Distribution PHARMACOKINETIC
NIH
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