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

Details

Stereochemistry ABSOLUTE
Molecular Formula C22H17F2N5OS
Molecular Weight 437.467
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ISAVUCONAZOLE

SMILES

C[C@@]([H])(c1nc(cs1)-c2ccc(cc2)C#N)[C@](Cn3cncn3)(c4cc(ccc4F)F)O

InChI

InChIKey=DDFOUSQFMYRUQK-RCDICMHDSA-N
InChI=1S/C22H17F2N5OS/c1-14(21-28-20(10-31-21)16-4-2-15(9-25)3-5-16)22(30,11-29-13-26-12-27-29)18-8-17(23)6-7-19(18)24/h2-8,10,12-14,30H,11H2,1H3/t14-,22+/m0/s1

HIDE SMILES / InChI

Molecular Formula C22H17F2N5OS
Molecular Weight 437.467
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24187505

Isavuconazole is an active form of isavuconazonium, a prodrug which is marketed under the name Cresemba. Isavuconazole inhibits lanosterol 14-alpha demethylase (or CYP51A1) and leads to the accumulation of ergosterol toxic precursors in the fungal cytoplasm. Isavuconazole is indicated for the treatment of invasive aspergillosis and invasive mucormycosis.

CNS Activity

Curator's Comment:: Oral administration of 25 mg/kg isavuconazonium sulfate to rats resulted in isavuconazole brain at levels about twice those detected in the plasma.

Originator

Curator's Comment:: # Hoffmann-La Roche

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
CRESEMBA

Approved Use

Cresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis.

Launch Date

1425600000000
Curative
CRESEMBA

Approved Use

Cresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis.

Launch Date

1425600000000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
7499 ng/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
20028 ng/mL
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
121402 ng × h/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
352805 ng × h/mL
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
130 h
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (0.2%)
Sources:
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (0.2%)
Sources:
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (0.4%)
Sources:
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Blood creatinine increased...
AEs leading to
discontinuation/dose reduction:
Blood creatinine increased (0.6%)
Sources:
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (16.7%)
Sources:
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (16.7%)
Sources:
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (2.6%)
Sources:
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (2.6%)
Sources:
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Disturbance in attention...
AEs leading to
discontinuation/dose reduction:
Disturbance in attention (5.1%)
Sources:
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Dizziness...
AEs leading to
discontinuation/dose reduction:
Dizziness (5.1%)
Sources:
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Nausea...
AEs leading to
discontinuation/dose reduction:
Nausea (5.1%)
Sources:
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Anxiety...
AEs leading to
discontinuation/dose reduction:
Anxiety (7.7%)
Sources:
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (7.7%)
Sources:
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Disc. AE: Hot flush...
AEs leading to
discontinuation/dose reduction:
Hot flush (7.7%)
Sources:
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean age 39.1 years
Health Status: unhealthy
Age Group: mean age 39.1 years
Sex: M+F
Sources:
Disc. AE: Atrioventricular block...
AEs leading to
discontinuation/dose reduction:
Atrioventricular block (grade 2, 2.4%)
Sources:
533.3 mg 3 times / day multiple, oral
Highest studied dose
Dose: 533.3 mg, 3 times / day
Route: oral
Route: multiple
Dose: 533.3 mg, 3 times / day
Sources:
unhealthy, mean age 48.4 years
Other AEs: Rash...
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
Disc. AE: Dizziness, Hypersensitivity...
Other AEs: Headache, Headache...
AEs leading to
discontinuation/dose reduction:
Dizziness (8.3%)
Hypersensitivity (8.3%)
Nausea (8.3%)
Other AEs:
Headache (grade 1, 8.3%)
Headache (grade 2, 8.3%)
Rash (grade 1, 8.3%)
Rash (grade 2, 8.3%)
Cough (grade 1, 16.7%)
Sources:
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Disc. AE: Acute respiratory failure, Chills...
AEs leading to
discontinuation/dose reduction:
Acute respiratory failure (0.4%)
Chills (0.4%)
Convulsion (0.8%)
Dyspnoea (0.8%)
Epilepsy (0.4%)
Hypotension (0.4%)
Respiratory failure (0.8%)
Sources:
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Disc. AE: Pancytopenia, Cardiac arrest...
AEs leading to
discontinuation/dose reduction:
Pancytopenia (0.4%)
Cardiac arrest (0.4%)
Cardio-respiratory arrest (0.4%)
Congestive cardiomyopathy (0.4%)
Supraventricular tachycardia (0.4%)
Optic neuropathy (0.4%)
Dysphagia (0.4%)
Small intestinal obstruction (0.4%)
Vomiting (0.4%)
Chills (0.4%)
Hepatitis acute (0.4%)
Aspergillosis (0.4%)
Bronchopneumonia (0.4%)
Bronchopulmonary aspergillosis (0.4%)
Endocarditis (0.4%)
Fungal infection (0.8%)
Infection (0.4%)
Pneumonia (0.4%)
Sepsis (0.4%)
Septic shock (0.8%)
Blood bilirubin increased (0.8%)
Blood sodium decreased (0.4%)
Transaminases increased (0.4%)
Myositis (0.4%)
Convulsion (0.8%)
Encephalopathy (0.4%)
Epilepsy (0.8%)
Confusional state (0.8%)
Renal failure (0.8%)
Renal failure acute (0.4%)
Acute respiratory failure (0.4%)
Dyspnoea (0.8%)
Respiratory distress (0.4%)
Respiratory failure (0.8%)
Dermatitis (0.4%)
Dermatitis allergic (0.4%)
Hypotension (0.4%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Diarrhea 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
healthy, adult
Headache 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
healthy, adult
Vomiting 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
healthy, adult
Blood creatinine increased 0.6%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
healthy, adult
Diarrhea 16.7%
Disc. AE
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
healthy, adult
Headache 16.7%
Disc. AE
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
healthy, adult
Diarrhea 2.6%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Vomiting 2.6%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Disturbance in attention 5.1%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Dizziness 5.1%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Nausea 5.1%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Anxiety 7.7%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Headache 7.7%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Hot flush 7.7%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, adult
Atrioventricular block grade 2, 2.4%
Disc. AE
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean age 39.1 years
Health Status: unhealthy
Age Group: mean age 39.1 years
Sex: M+F
Sources:
Rash 8.3%
533.3 mg 3 times / day multiple, oral
Highest studied dose
Dose: 533.3 mg, 3 times / day
Route: oral
Route: multiple
Dose: 533.3 mg, 3 times / day
Sources:
unhealthy, mean age 48.4 years
Dizziness 8.3%
Disc. AE
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
Hypersensitivity 8.3%
Disc. AE
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
Nausea 8.3%
Disc. AE
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
Cough grade 1, 16.7%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
Headache grade 1, 8.3%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
Rash grade 1, 8.3%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
Headache grade 2, 8.3%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
Rash grade 2, 8.3%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
Acute respiratory failure 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Chills 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Epilepsy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Hypotension 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Convulsion 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Dyspnoea 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Respiratory failure 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Acute respiratory failure 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Aspergillosis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Blood sodium decreased 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Bronchopneumonia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Bronchopulmonary aspergillosis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Cardiac arrest 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Cardio-respiratory arrest 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Chills 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Congestive cardiomyopathy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Dermatitis allergic 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Dermatitis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Dysphagia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Encephalopathy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Endocarditis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Hepatitis acute 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Hypotension 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Infection 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Myositis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Optic neuropathy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Pancytopenia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Pneumonia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Renal failure acute 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Respiratory distress 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Sepsis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Small intestinal obstruction 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Supraventricular tachycardia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Transaminases increased 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Vomiting 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Blood bilirubin increased 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Confusional state 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Convulsion 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Dyspnoea 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Epilepsy 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Fungal infection 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Renal failure 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Respiratory failure 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
Septic shock 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
yes [IC50 11.2 uM]
yes [IC50 25.7 uM]
yes [IC50 6.31 uM]
yes [IC50 92 uM]
yes [Ki 0.59 uM]
yes [Ki 0.622 uM]
yes [Ki 1.74 uM]
yes [Ki 2.86 uM]
yes [Ki 4.78 uM]
yes [Ki 4.82 uM]
yes [Ki 5.4 uM]
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
yes
yes
yes
yes (co-administration study)
Comment: Upon coadministration, ketoconazole increased the isavuconazole Cmax by 9% and isavuconazole AUC by 422% after multiple dose administration of ketoconazole (200 mg twice daily) for 24 days and a single dose of isavuconazonium equivalent to 200 mg of isavuconazole.
Page: 19
Tox targets
PubMed

PubMed

TitleDatePubMed
Drug evaluation: BAL-8557--a novel broad-spectrum triazole antifungal.
2006 Aug
Investigational antimicrobial drugs for bloodstream infections.
2008 Aug
New and investigational triazole agents for the treatment of invasive fungal infections.
2008 Dec
Isavuconazole: a new and promising antifungal triazole for the treatment of invasive fungal infections.
2008 Dec
In vitro activities of isavuconazole against opportunistic filamentous and dimorphic fungi.
2009 Feb
Efficacy of isavuconazole, voriconazole and fluconazole in temporarily neutropenic murine models of disseminated Candida tropicalis and Candida krusei.
2009 Jan
Antifungal susceptibilities among different serotypes of Cryptococcus gattii and Cryptococcus neoformans.
2009 Jan
In vitro activity of isavuconazole against Trichosporon, Rhodotorula, Geotrichum, Saccharomyces and Pichia species.
2009 Jul
New triazoles and echinocandins: mode of action, in vitro activity and mechanisms of resistance.
2009 Oct
Clinical safety and tolerability issues in use of triazole derivatives in management of fungal infections.
2010
In vitro activities of eight antifungal drugs against 55 clinical isolates of Fonsecaea spp.
2010 Apr
[Recent advances in the study of new antifungal lead compounds].
2010 Aug
Rhinocladiella aquaspersa, proven agent of verrucous skin infection and a novel type of chromoblastomycosis.
2010 Aug
In vitro antifungal susceptibilities and amplified fragment length polymorphism genotyping of a worldwide collection of 350 clinical, veterinary, and environmental Cryptococcus gattii isolates.
2010 Dec
Microsatellite typing and susceptibilities of serial Cryptococcus neoformans isolates from Cuban patients with recurrent cryptococcal meningitis.
2010 Oct 4
In vitro activity of isavuconazole against 208 Aspergillus flavus isolates in comparison with 7 other antifungal agents: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
2011 Dec
Isavuconazole activity against Aspergillus lentulus, Neosartorya udagawae, and Cryptococcus gattii, emerging fungal pathogens with reduced azole susceptibility.
2013 Sep
Isavuconazole: Pharmacology, Pharmacodynamics, and Current Clinical Experience with a New Triazole Antifungal Agent.
2015 Nov
Isavuconazole: A New Broad-Spectrum Triazole Antifungal Agent.
2015 Nov 15
Patents

Sample Use Guides

Loading Dose: 372 mg isavuconazonium sulfate (equivalent to 200 mg of isavuconazole) every 8 hours for 6 doses (48 hours) via oral (2 capsules) or intravenous administration (1 reconstituted vial) Maintenance Dose: 372 mg isavuconazonium sulfate (equivalent to 200 mg of isavuconazole) once daily via oral (2 capsules) or intravenous administration (1 reconstituted vial) starting 12 to 24 hours after the last loading dose.
Route of Administration: Other
Isavuconazole exhibited MIC50 values of 1–4 ug/ mL and MIC90 values of 4–16 ug/mL, against Mucorales isolates. MIC90 against Aspergillus fumigatus was 0.5–2 ug/ml, MIC90 against Aspergillus terreus was 0.5–4 ug/ml, MIC90 against Aspergillus flavus was 1–16 ug/ml, MIC90 against Aspergillus niger was 2–4 ug/ml.
Substance Class Chemical
Created
by admin
on Sat Jun 26 14:25:21 UTC 2021
Edited
by admin
on Sat Jun 26 14:25:21 UTC 2021
Record UNII
60UTO373KE
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ISAVUCONAZOLE
INN   MI   WHO-DD  
INN  
Official Name English
ISAVUCONAZOLE [WHO-DD]
Common Name English
4-(2-((2R,3R)-3-(2,5-DIFLUOROPHENYL)-3-HYDROXY-4-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-YL)-1,3-THIAZOL-4-YL)BENZONITRILE
Systematic Name English
BAL-4815
Code English
ISAVUCONAZOLE [MI]
Common Name English
ISAVUCONAZOLE [INN]
Common Name English
Classification Tree Code System Code
WHO-ATC J02AC05
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
NCI_THESAURUS C514
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
NDF-RT N0000175487
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
Code System Code Type Description
WIKIPEDIA
ISAVUCONAZOLE
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
EPA CompTox
241479-67-4
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
NCI_THESAURUS
C64543
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
ChEMBL
CHEMBL409153
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
NDF-RT
N0000187061
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY Organic Cation Transporter 2 Inhibitors [MoA]
CAS
241479-67-4
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
INN
8783
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
EVMPD
SUB128138
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
DRUG BANK
DB11633
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
NDF-RT
N0000185503
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY P-Glycoprotein Inhibitors [MoA]
RXCUI
1720882
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY RxNorm
MERCK INDEX
M6419
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY Merck Index
NDF-RT
N0000182141
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
FDA UNII
60UTO373KE
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
PUBCHEM
6918485
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
FECAL
METABOLIC ENZYME -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
METABOLIC ENZYME -> INDUCER
METABOLIC ENZYME -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
TARGET ORGANISM->INHIBITOR
METABOLIC ENZYME -> INHIBITOR
METABOLIC ENZYME -> INDUCER
METABOLIC ENZYME -> INDUCER
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
URINE
METABOLIC ENZYME -> SUBSTRATE
TARGET ORGANISM->INHIBITOR
TARGET ORGANISM->INHIBITOR
METABOLIC ENZYME -> INDUCER
METABOLIC ENZYME -> INDUCER
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

ORAL BIOAVAILABILITY PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC INTRAVENOUS ADMINISTRATION