Details
| Stereochemistry | EPIMERIC |
| Molecular Formula | C35H35F2N8O5S.HO4S |
| Molecular Weight | 814.835 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OS([O-])(=O)=O.CNCC(=O)OCC1=CC=CN=C1N(C)C(=O)OC(C)[N+]2=CN(C[C@@](O)([C@@H](C)C3=NC(=CS3)C4=CC=C(C=C4)C#N)C5=CC(F)=CC=C5F)N=C2
InChI
InChIKey=LWXUIUUOMSMZKJ-KLFWAVJMSA-M
InChI=1S/C35H35F2N8O5S.H2O4S/c1-22(33-42-30(18-51-33)25-9-7-24(15-38)8-10-25)35(48,28-14-27(36)11-12-29(28)37)19-45-21-44(20-41-45)23(2)50-34(47)43(4)32-26(6-5-13-40-32)17-49-31(46)16-39-3;1-5(2,3)4/h5-14,18,20-23,39,48H,16-17,19H2,1-4H3;(H2,1,2,3,4)/q+1;/p-1/t22-,23?,35+;/m0./s1
DescriptionCurator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24187505
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
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000PharmR.pdf
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.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3390825 |
|||
Target ID: CHEMBL3390824 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Curative | CRESEMBA Approved UseCresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis. Launch Date2015 |
|||
| Curative | CRESEMBA Approved UseCresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis. Launch Date2015 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Dose | Population | Adverse 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136 |
healthy, adult n = 490 Health Status: healthy Age Group: adult Sex: M+F Population Size: 490 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136 |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (0.2%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137 |
healthy, adult n = 490 Health Status: healthy Age Group: adult Sex: M+F Population Size: 490 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137 |
Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (0.4%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138 |
healthy, adult n = 490 Health Status: healthy Age Group: adult Sex: M+F Population Size: 490 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138 |
Disc. AE: Blood creatinine increased... AEs leading to discontinuation/dose reduction: Blood creatinine increased (0.6%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139 |
healthy, adult n = 490 Health Status: healthy Age Group: adult Sex: M+F Population Size: 490 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139 |
Disc. AE: Headache... AEs leading to discontinuation/dose reduction: Headache (0.2%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134 |
healthy, adult n = 6 Health Status: healthy Age Group: adult Sex: M+F Population Size: 6 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134 |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (16.7%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135 |
healthy, adult n = 6 Health Status: healthy Age Group: adult Sex: M+F Population Size: 6 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135 |
Disc. AE: Headache... AEs leading to discontinuation/dose reduction: Headache (16.7%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140 |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (2.6%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141 |
Disc. AE: Nausea... AEs leading to discontinuation/dose reduction: Nausea (5.1%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142 |
Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (2.6%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143 |
Disc. AE: Disturbance in attention... AEs leading to discontinuation/dose reduction: Disturbance in attention (5.1%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144 |
Disc. AE: Dizziness... AEs leading to discontinuation/dose reduction: Dizziness (5.1%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145 |
Disc. AE: Headache... AEs leading to discontinuation/dose reduction: Headache (7.7%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146 |
Disc. AE: Anxiety... AEs leading to discontinuation/dose reduction: Anxiety (7.7%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146 |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147 |
Disc. AE: Hot flush... AEs leading to discontinuation/dose reduction: Hot flush (7.7%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147 |
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 n = 41 Health Status: unhealthy Condition: uncomplicated esophageal candidiasis Age Group: mean age 39.1 years Sex: M+F Population Size: 41 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 (mean) 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 n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: |
Other AEs: Rash... |
400 mg 1 times / day multiple, oral (mean) Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
unhealthy, mean age 48.4 years n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
Disc. AE: Dizziness, Hypersensitivity... Other AEs: Headache, Headache... AEs leading to discontinuation/dose reduction: Dizziness (8.3%) Other AEs:Hypersensitivity (8.3%) Nausea (8.3%) Headache (grade 1, 8.3%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31Headache (grade 2, 8.3%) Rash (grade 1, 8.3%) Rash (grade 2, 8.3%) Cough (grade 1, 16.7%) |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
Disc. AE: Pancytopenia, Cardiac arrest... AEs leading to discontinuation/dose reduction: Pancytopenia (0.4%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131Cardiac 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%) |
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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
Disc. AE: Acute respiratory failure, Chills... AEs leading to discontinuation/dose reduction: Acute respiratory failure (0.4%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149Chills (0.4%) Convulsion (0.8%) Dyspnoea (0.8%) Epilepsy (0.4%) Hypotension (0.4%) Respiratory failure (0.8%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136 |
healthy, adult n = 490 Health Status: healthy Age Group: adult Sex: M+F Population Size: 490 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137 |
healthy, adult n = 490 Health Status: healthy Age Group: adult Sex: M+F Population Size: 490 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138 |
healthy, adult n = 490 Health Status: healthy Age Group: adult Sex: M+F Population Size: 490 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139 |
healthy, adult n = 490 Health Status: healthy Age Group: adult Sex: M+F Population Size: 490 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134 |
healthy, adult n = 6 Health Status: healthy Age Group: adult Sex: M+F Population Size: 6 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135 |
healthy, adult n = 6 Health Status: healthy Age Group: adult Sex: M+F Population Size: 6 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147 |
healthy, adult n = 39 Health Status: healthy Age Group: adult Sex: M+F Population Size: 39 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147 |
| 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 n = 41 Health Status: unhealthy Condition: uncomplicated esophageal candidiasis Age Group: mean age 39.1 years Sex: M+F Population Size: 41 Sources: |
| Rash | 8.3% | 533.3 mg 3 times / day multiple, oral (mean) 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 n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: |
| Dizziness | 8.3% Disc. AE |
400 mg 1 times / day multiple, oral (mean) Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
unhealthy, mean age 48.4 years n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
| Hypersensitivity | 8.3% Disc. AE |
400 mg 1 times / day multiple, oral (mean) Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
unhealthy, mean age 48.4 years n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
| Nausea | 8.3% Disc. AE |
400 mg 1 times / day multiple, oral (mean) Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
unhealthy, mean age 48.4 years n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
| Cough | grade 1, 16.7% | 400 mg 1 times / day multiple, oral (mean) Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
unhealthy, mean age 48.4 years n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
| Headache | grade 1, 8.3% | 400 mg 1 times / day multiple, oral (mean) Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
unhealthy, mean age 48.4 years n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
| Rash | grade 1, 8.3% | 400 mg 1 times / day multiple, oral (mean) Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
unhealthy, mean age 48.4 years n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
| Headache | grade 2, 8.3% | 400 mg 1 times / day multiple, oral (mean) Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
unhealthy, mean age 48.4 years n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
| Rash | grade 2, 8.3% | 400 mg 1 times / day multiple, oral (mean) Studied dose Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
unhealthy, mean age 48.4 years n = 12 Health Status: unhealthy Condition: acute myeloid leukemia Age Group: mean age 48.4 years Sex: M+F Population Size: 12 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
| 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: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
unhealthy, mean age 51.1 years n = 257 Health Status: unhealthy Condition: Invasive aspergillosis Age Group: mean age 51.1 years Sex: M+F Population Size: 257 Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149 |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical 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
| Target | Modality | Activity | Metabolite | Clinical 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: 19.0 |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Drug evaluation: BAL-8557--a novel broad-spectrum triazole antifungal. | 2006 Aug |
|
| Multiple-dose pharmacokinetics and safety of the new antifungal triazole BAL4815 after intravenous infusion and oral administration of its prodrug, BAL8557, in healthy volunteers. | 2006 Jan |
|
| Single-ascending-dose pharmacokinetics and safety of the novel broad-spectrum antifungal triazole BAL4815 after intravenous infusions (50, 100, and 200 milligrams) and oral administrations (100, 200, and 400 milligrams) of its prodrug, BAL8557, in healthy volunteers. | 2006 Jan |
|
| Investigational antimicrobial drugs for bloodstream infections. | 2008 Aug |
|
| New and emerging treatments for fungal infections. | 2008 Jan |
|
| Cryptococcus gattii: An Emerging Cause of Fungal Disease in North America. | 2009 |
|
| 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 |
|
| In vitro antifungal activity of isavuconazole against 345 mucorales isolates collected at study centers in eight countries. | 2009 Jun |
|
| New triazoles and echinocandins: mode of action, in vitro activity and mechanisms of resistance. | 2009 Oct |
|
| Comparison of adverse events between oral and intravenous formulations of antimicrobial agents: a systematic review of the evidence from randomized trials. | 2009 Oct |
|
| New generation azole antifungals in clinical investigation. | 2009 Sep |
|
| 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 |
|
| Novel triazole antifungal drugs: focus on isavuconazole, ravuconazole and albaconazole. | 2010 Feb |
|
| Isavuconazole: a comprehensive review of spectrum of activity of a new triazole. | 2010 Nov |
|
| Antifungal susceptibility, serotyping, and genotyping of clinical Cryptococcus neoformans isolates collected during 18 years in a single institution in Madrid, Spain. | 2010 Nov |
|
| In vitro activity of isavuconazole against 140 reference fungal strains and 165 clinically isolated yeasts from Japan. | 2010 Oct |
|
| Microsatellite typing and susceptibilities of serial Cryptococcus neoformans isolates from Cuban patients with recurrent cryptococcal meningitis. | 2010 Oct 4 |
|
| In vitro antifungal activities of isavuconazole and comparators against rare yeast pathogens. | 2010 Sep |
|
| Chromatographic and electrophoretic techniques used in the analysis of triazole antifungal agents-a review. | 2010 Sep 15 |
|
| 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 |
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.
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| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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FDA ORPHAN DRUG |
395013
Created by
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NCI_THESAURUS |
C514
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EU-Orphan Drug |
EU/03/14/1276
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FDA ORPHAN DRUG |
394913
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FDA ORPHAN DRUG |
447814
Created by
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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1608321
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DB06636
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100000158287
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C139756
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72196309
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SUB167941
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BC-11
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31Q44514JV
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31Q44514JV
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DTXSID901026216
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CHEMBL1183349
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85977
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946075-13-4
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PRIMARY |
ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
