Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C16H14F3N5O |
Molecular Weight | 349.3111 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@]([H])(c1c(cncn1)F)[C@](Cn2cncn2)(c3ccc(cc3F)F)O
InChI
InChIKey=BCEHBSKCWLPMDN-MGPLVRAMSA-N
InChI=1S/C16H14F3N5O/c1-10(15-14(19)5-20-7-22-15)16(25,6-24-9-21-8-23-24)12-3-2-11(17)4-13(12)18/h2-5,7-10,25H,6H2,1H3/t10-,16+/m0/s1
Molecular Formula | C16H14F3N5O |
Molecular Weight | 349.3111 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment:: description was created based on several sources, including:
http://www.drugbank.ca/drugs/DB00582
Curator's Comment:: description was created based on several sources, including:
http://www.drugbank.ca/drugs/DB00582
Voriconazole (vor-i-KON-a-zole, brand name Vfend, Pfizer) is a triazole antifungal medication. VFEND® (voriconazole) is available as film-coated tablets for oral administration, and as a lyophilized powder for solution for intravenous infusion. Voriconazole is a triazole antifungal agent indicated for use in the treatment of fungal infections including invasive aspergillosis, esophageal candidiasis, and serious fungal infections caused by Scedosporium apiospermum (asexual form of Pseudallescheria boydii) and Fusarium spp. including Fusarium solani. Fungal plasma membranes are similar to mammalian plasma membranes, differing in having the nonpolar sterol ergosterol, rather than cholesterol, as the principal sterol. Membrane sterols such as ergosterol provide structure, modulation of membrane fluidity, and possibly control of some physiologic events. Voriconazole effects the formation of the fungal plasma membrane by indirectly inhibiting the biosynthesis of ergosterol. This results in plasma membrane permeability changes and inhibition of growth. The primary mode of action of voriconazole is the inhibition of fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylation, an essential step in fungal ergosterol biosynthesis. The accumulation of 14 alpha-methyl sterols correlates with the subsequent loss of ergosterol in the fungal cell wall and may be responsible for the antifungal activity of voriconazole. Voriconazole has been shown to be more selective for fungal cytochrome P-450 enzymes than for various mammalian cytochrome P-450 enzyme systems. The most common side effects associated with voriconazole include transient visual disturbances, fever, rash, vomiting, nausea, diarrhea, headache, sepsis, peripheral edema, abdominal pain, and respiratory disorder. Unlike most adverse effects, which are similar to other azole antifungal agents, visual disturbances (such as blurred vision or increased sensitivity to light) are unique to voriconazole. Though rare, there have been cases of serious hepatic reactions during treatment with voriconazole (a class effect of azole antifungal agents). Liver function tests should be evaluated at the start of and during the course of therapy. Voriconazole is phototoxic. It has been associated with an increased risk of squamous-cell carcinoma of the skin
CNS Activity
Originator
Sources: http://www.prnewswire.com/news-releases/fda-approves-pfizer-antifungal-medicine-vfendr-voriconazole-77623937.html
Curator's Comment:: # Pfizer researchers in Sandwich, England
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1780 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Curative | VFEND Approved Useuse in the treatment of the fungal infections Launch Date1.07084159E12 |
|||
Curative | VFEND Approved Useuse in the treatment of the fungal infections Launch Date1.07084159E12 |
|||
Curative | VFEND Approved Useuse in the treatment of the fungal infections Launch Date1.07084159E12 |
|||
Curative | VFEND Approved Useuse in the treatment of the fungal infections Launch Date1.07084159E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.13 μg/mL |
6 mg/kg single, intravenous dose: 6 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.31 μg/mL |
200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3.03 μg/mL |
3 mg/kg 2 times / day steady-state, intravenous dose: 3 mg/kg route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4.77 μg/mL |
4 mg/kg 2 times / day steady-state, intravenous dose: 4 mg/kg route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4.74 μg/mL |
300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.3 μg/mL |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3.1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19933807 |
200 mg 2 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
13.9 μg × h/mL |
6 mg/kg single, intravenous dose: 6 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
12.4 μg × h/mL |
200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
13.7 μg × h/mL |
3 mg/kg 2 times / day steady-state, intravenous dose: 3 mg/kg route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
33.9 μg × h/mL |
4 mg/kg 2 times / day steady-state, intravenous dose: 4 mg/kg route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
34 μg × h/mL |
300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
9.31 μg × h/mL |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
27.9 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19933807 |
200 mg 2 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
15.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19933807 |
200 mg 2 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
42% |
200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
42% |
300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VORICONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
16 mg/kg 1 times / day steady, oral Recommended Dose: 16 mg/kg, 1 times / day Route: oral Route: steady Dose: 16 mg/kg, 1 times / day Sources: |
unhealthy, 17 years n = 1 Health Status: unhealthy Condition: cystic fibrosis and allergic bronchopulmonary aspergillosis Age Group: 17 years Sex: F Population Size: 1 Sources: |
Disc. AE: Photophobia, Fatigue... AEs leading to discontinuation/dose reduction: Photophobia (1 patient) Sources: Fatigue (1 patient) Concentration impaired (1 patient) Insomnia (1 patient) |
200 mg 2 times / day steady, oral Recommended Dose: 200 mg, 2 times / day Route: oral Route: steady Dose: 200 mg, 2 times / day Sources: |
unhealthy, 42.7–64.5 years n = 327 Health Status: unhealthy Condition: Acute myeloid leukemia, lymphocytic leukemia, Myelodysplastic syndrome, Multiple myeloma Lymphoma and Other Age Group: 42.7–64.5 years Sex: M+F Population Size: 327 Sources: |
Disc. AE: Function liver abnormal, Hallucination, visual... AEs leading to discontinuation/dose reduction: Function liver abnormal (73 patients) Sources: Hallucination, visual (16 patients) Skin rash (6 patients) Kidney dysfunction (3 patients) Electrocardiogram QTc interval prolonged (2 patients) Gastrointestinal symptom NOS (1 patient) |
400 mg single, oral Overdose |
unhealthy, 53.4–67.5 years n = 31 Health Status: unhealthy Condition: Acute myeloid leukemia, Acute lymphoid leukemia, Lymphoma, Others Age Group: 53.4–67.5 years Sex: M+F Population Size: 31 Sources: |
Disc. AE: CRP increased, Bilirubin increased... AEs leading to discontinuation/dose reduction: CRP increased (31 patient) Sources: Bilirubin increased (31 patient) |
16 mg/kg 1 times / day steady, oral Recommended Dose: 16 mg/kg, 1 times / day Route: oral Route: steady Dose: 16 mg/kg, 1 times / day Sources: |
unhealthy, 9 years n = 1 Health Status: unhealthy Condition: cystic fibrosis and invasive aspergillosis Age Group: 9 years Sex: M Population Size: 1 Sources: |
Disc. AE: Photophobia... AEs leading to discontinuation/dose reduction: Photophobia (1 patient) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Concentration impaired | 1 patient Disc. AE |
16 mg/kg 1 times / day steady, oral Recommended Dose: 16 mg/kg, 1 times / day Route: oral Route: steady Dose: 16 mg/kg, 1 times / day Sources: |
unhealthy, 17 years n = 1 Health Status: unhealthy Condition: cystic fibrosis and allergic bronchopulmonary aspergillosis Age Group: 17 years Sex: F Population Size: 1 Sources: |
Fatigue | 1 patient Disc. AE |
16 mg/kg 1 times / day steady, oral Recommended Dose: 16 mg/kg, 1 times / day Route: oral Route: steady Dose: 16 mg/kg, 1 times / day Sources: |
unhealthy, 17 years n = 1 Health Status: unhealthy Condition: cystic fibrosis and allergic bronchopulmonary aspergillosis Age Group: 17 years Sex: F Population Size: 1 Sources: |
Insomnia | 1 patient Disc. AE |
16 mg/kg 1 times / day steady, oral Recommended Dose: 16 mg/kg, 1 times / day Route: oral Route: steady Dose: 16 mg/kg, 1 times / day Sources: |
unhealthy, 17 years n = 1 Health Status: unhealthy Condition: cystic fibrosis and allergic bronchopulmonary aspergillosis Age Group: 17 years Sex: F Population Size: 1 Sources: |
Photophobia | 1 patient Disc. AE |
16 mg/kg 1 times / day steady, oral Recommended Dose: 16 mg/kg, 1 times / day Route: oral Route: steady Dose: 16 mg/kg, 1 times / day Sources: |
unhealthy, 17 years n = 1 Health Status: unhealthy Condition: cystic fibrosis and allergic bronchopulmonary aspergillosis Age Group: 17 years Sex: F Population Size: 1 Sources: |
Gastrointestinal symptom NOS | 1 patient Disc. AE |
200 mg 2 times / day steady, oral Recommended Dose: 200 mg, 2 times / day Route: oral Route: steady Dose: 200 mg, 2 times / day Sources: |
unhealthy, 42.7–64.5 years n = 327 Health Status: unhealthy Condition: Acute myeloid leukemia, lymphocytic leukemia, Myelodysplastic syndrome, Multiple myeloma Lymphoma and Other Age Group: 42.7–64.5 years Sex: M+F Population Size: 327 Sources: |
Hallucination, visual | 16 patients Disc. AE |
200 mg 2 times / day steady, oral Recommended Dose: 200 mg, 2 times / day Route: oral Route: steady Dose: 200 mg, 2 times / day Sources: |
unhealthy, 42.7–64.5 years n = 327 Health Status: unhealthy Condition: Acute myeloid leukemia, lymphocytic leukemia, Myelodysplastic syndrome, Multiple myeloma Lymphoma and Other Age Group: 42.7–64.5 years Sex: M+F Population Size: 327 Sources: |
Electrocardiogram QTc interval prolonged | 2 patients Disc. AE |
200 mg 2 times / day steady, oral Recommended Dose: 200 mg, 2 times / day Route: oral Route: steady Dose: 200 mg, 2 times / day Sources: |
unhealthy, 42.7–64.5 years n = 327 Health Status: unhealthy Condition: Acute myeloid leukemia, lymphocytic leukemia, Myelodysplastic syndrome, Multiple myeloma Lymphoma and Other Age Group: 42.7–64.5 years Sex: M+F Population Size: 327 Sources: |
Kidney dysfunction | 3 patients Disc. AE |
200 mg 2 times / day steady, oral Recommended Dose: 200 mg, 2 times / day Route: oral Route: steady Dose: 200 mg, 2 times / day Sources: |
unhealthy, 42.7–64.5 years n = 327 Health Status: unhealthy Condition: Acute myeloid leukemia, lymphocytic leukemia, Myelodysplastic syndrome, Multiple myeloma Lymphoma and Other Age Group: 42.7–64.5 years Sex: M+F Population Size: 327 Sources: |
Skin rash | 6 patients Disc. AE |
200 mg 2 times / day steady, oral Recommended Dose: 200 mg, 2 times / day Route: oral Route: steady Dose: 200 mg, 2 times / day Sources: |
unhealthy, 42.7–64.5 years n = 327 Health Status: unhealthy Condition: Acute myeloid leukemia, lymphocytic leukemia, Myelodysplastic syndrome, Multiple myeloma Lymphoma and Other Age Group: 42.7–64.5 years Sex: M+F Population Size: 327 Sources: |
Function liver abnormal | 73 patients Disc. AE |
200 mg 2 times / day steady, oral Recommended Dose: 200 mg, 2 times / day Route: oral Route: steady Dose: 200 mg, 2 times / day Sources: |
unhealthy, 42.7–64.5 years n = 327 Health Status: unhealthy Condition: Acute myeloid leukemia, lymphocytic leukemia, Myelodysplastic syndrome, Multiple myeloma Lymphoma and Other Age Group: 42.7–64.5 years Sex: M+F Population Size: 327 Sources: |
Bilirubin increased | 31 patient Disc. AE |
400 mg single, oral Overdose |
unhealthy, 53.4–67.5 years n = 31 Health Status: unhealthy Condition: Acute myeloid leukemia, Acute lymphoid leukemia, Lymphoma, Others Age Group: 53.4–67.5 years Sex: M+F Population Size: 31 Sources: |
CRP increased | 31 patient Disc. AE |
400 mg single, oral Overdose |
unhealthy, 53.4–67.5 years n = 31 Health Status: unhealthy Condition: Acute myeloid leukemia, Acute lymphoid leukemia, Lymphoma, Others Age Group: 53.4–67.5 years Sex: M+F Population Size: 31 Sources: |
Photophobia | 1 patient Disc. AE |
16 mg/kg 1 times / day steady, oral Recommended Dose: 16 mg/kg, 1 times / day Route: oral Route: steady Dose: 16 mg/kg, 1 times / day Sources: |
unhealthy, 9 years n = 1 Health Status: unhealthy Condition: cystic fibrosis and invasive aspergillosis Age Group: 9 years Sex: M Population Size: 1 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/23653047/ Page: 17.0 |
likely | |||
no | ||||
no | ||||
Page: 12, 13, 14 |
yes [Ki 14 uM] | |||
Page: 12, 13, 14 |
yes [Ki 22 uM] | |||
Page: 12, 13, 14 |
yes [Ki 7 uM] | |||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 2, 10,13, 21-23, 26-27 |
major | yes (co-administration study) Comment: from FDA label pp26-28: rifampin decreased voriconazole Cmax by 93% and AUC by 96% and fluconazole increased voriconazole Cmax by 57% and AUC 79% Page: 2, 10,13, 21-23, 26-27 |
||
Page: 12.0 |
no | |||
Page: 12.0 |
no | |||
Page: 12.0 |
no | |||
Page: 11.0 |
yes [Km 21 uM] | yes (co-administration study) Comment: from FDA label pp26-28: rifampin decreased voriconazole Cmax by 93% and AUC by 96%; fluconazole increased voriconazole Cmax by 57% and AUC 79% Page: 11.0 |
||
Page: 11.0 |
yes [Km 240 uM] | yes (co-administration study) Comment: from FDA label pp26-28: rifampin decreased voriconazole Cmax by 93% and AUC by 96%; fluconazole increased voriconazole Cmax by 57% and AUC 79% Page: 11.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Coccidioidomycosis: efficacy of new agents and future prospects. | 2001 Dec |
|
Improving the outcome of invasive aspergillosis: new diagnostic tools and new therapeutic strategies. | 2002 |
|
Pharmacological aspects of the new triazole voriconazole. | 2002 |
|
Successful treatment of Candida glabrata myocarditis with voriconazole. | 2002 |
|
Voriconazole: in the treatment of invasive aspergillosis. | 2002 |
|
Successful treatment of Paecilomyces lilacinus endophthalmitis with voriconazole. | 2002 |
|
Gateways to Clinical Trials. | 2002 Apr |
|
Recent advances in the epidemiology, prevention, diagnosis, and treatment of fungal pneumonia. | 2002 Apr |
|
Effect of voriconazole on the pharmacokinetics of cyclosporine in renal transplant patients. | 2002 Apr |
|
Safety and pharmacokinetics of oral voriconazole in patients at risk of fungal infection: a dose escalation study. | 2002 Apr |
|
Voriconazole versus amphotericin B for primary therapy of invasive aspergillosis. | 2002 Aug 8 |
|
Use of voriconazole to successfully treat disseminated Trichosporon asahii infection in a patient with acute myeloid leukaemia. | 2002 Dec |
|
Usefulness of a colorimetric method for testing antifungal drug susceptibilities of Aspergillus species to voriconazole. | 2002 Dec |
|
Voriconazole in the management of invasive aspergillosis in two patients with acute myeloid leukemia undergoing stem cell transplantation. | 2002 Dec |
|
Case Reports. Chronic and acute Aspergillus meningitis. | 2002 Dec |
|
Voriconazole versus amphotericin B for invasive aspergillosis. | 2002 Dec 19 |
|
Voriconazole versus amphotericin B for invasive aspergillosis. | 2002 Dec 19 |
|
A multidrug, including voriconazole, resistant oral Candida infection in an AIDS patient effectively treated with echinocandin. | 2002 Jan |
|
In vitro activity of three new triazoles and one echinocandin against Candida bloodstream isolates from cancer patients. | 2002 Jul |
|
Antifungal triazoles and polymorphonuclear leukocytes synergize to cause increased hyphal damage to Scedosporium prolificans and Scedosporium apiospermum. | 2002 Jul |
|
Voriconazole. | 2002 Jul 22 |
|
New drugs, old drugs - dear drugs, cheap drugs. | 2002 Jun 15 |
|
Voriconazole in the treatment of aspergillosis, scedosporiosis and other invasive fungal infections in children. | 2002 Mar |
|
Clinical evaluation of a frozen commercially prepared microdilution panel for antifungal susceptibility testing of seven antifungal agents, including the new triazoles posaconazole, ravuconazole, and voriconazole. | 2002 May |
|
Voriconazole versus liposomal amphotericin B for empirical antifungal therapy. | 2002 May 30 |
|
Voriconazole versus liposomal amphotericin B for empirical antifungal therapy. | 2002 May 30 |
|
Voriconazole -- better chances for patients with invasive mycoses. | 2002 May 31 |
|
Management of mycoses in patients with hematologic disease and cancer -- review of the literature. | 2002 May 31 |
|
Management of mycoses in surgical patients -- review of the literature. | 2002 May 31 |
|
Decisions about voriconazole versus liposomal amphotericin B. | 2002 May 9 |
|
Gateways to clinical trials. | 2002 Nov |
|
In vitro susceptibilities of cerebrospinal fluid isolates of Cryptococcus neoformans collected during a ten-year period against fluconazole, voriconazole and posaconazole (SCH56592). | 2002 Nov |
|
An unusual case of pulmonary invasive aspergillosis and aspergilloma cured with voriconazole in a patient with cystic fibrosis. | 2002 Nov 1 |
|
The safety of voriconazole. | 2002 Nov 15 |
|
[Antifungal treatments]. | 2002 Nov 30 |
|
In vitro activities of investigational triazoles against Fusarium species: effects of inoculum size and incubation time on broth microdilution susceptibility test results. | 2002 Oct |
|
Voriconazole treatment of disseminated paecilomyces infection in a patient with acquired immunodeficiency syndrome. | 2002 Oct 1 |
|
Pseudallescheria boydii (Anamorph Scedosporium apiospermum). Infection in solid organ transplant recipients in a tertiary medical center and review of the literature. | 2002 Sep |
|
Cerebral aspergillosis caused by Neosartorya hiratsukae, Brazil. | 2002 Sep |
|
Emergence of nosocomial candidemia at a teaching hospital in Taiwan from 1981 to 2000: increased susceptibility of Candida species to fluconazole. | 2002 Winter |
|
Characterization of a lanosterol 14 alpha-demethylase from Pneumocystis carinii. | 2003 Aug |
|
Successful control of disseminated Scedosporium prolificans infection with a combination of voriconazole and terbinafine. | 2003 Feb |
|
In vitro activity of voriconazole, itraconazole, caspofungin, anidulafungin (VER002, LY303366) and amphotericin B against aspergillus spp. | 2003 Feb |
|
Antifungal pharmacotherapy for invasive mould infections. | 2003 Feb |
|
Disseminated infection due to Cylindrocarpon (Fusarium) lichenicola in a neutropenic patient with acute leukaemia: report of a case and review of the literature. | 2003 Jan |
|
In vitro activities of voriconazole, posaconazole, and four licensed systemic antifungal agents against Candida species infrequently isolated from blood. | 2003 Jan |
|
Activity of voriconazole against corneal isolates of Scedosporium apiospermum. | 2003 Jan |
|
In vitro susceptibilities of zygomycetes to conventional and new antifungals. | 2003 Jan |
|
Arthritis and osteomyelitis due to Aspergillus fumigatus: a 17 years old boy with chronic granulomatous disease. | 2003 Jan 31 |
|
Voriconazole: a new triazole antifungal agent. | 2003 Mar 1 |
Sample Use Guides
In Vivo Use Guide
Curator's Comment:: I.V. for Injection requires reconstitution to 10 mg/mL and subsequent dilution to 5 mg/mL or less prior to administration as an infusion, at a maximum rate of 3 mg/kg per hour over 1-2 hours
Tablets should be taken at least one hour before, or one hour following, a meal.
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/9431946
Curator's Comment:: The in vitro data obtained suggest that voriconazole may be effective in the treatment of opportunistic fungal infections.These investigators also noted that voriconazole was significantly more effective than itraconazole in reducing Aspergillus content in the lungs of immunocompromised animals with pulmonary aspergillosis.
each microdilution well containing 100 ul of the drug concentrations was inoculated with 100 ul of the diluted inoculum suspension (final volume in each well was 200 ul). Drug concentrations were 0.03 to 16 mg/ml for voriconazole. Stock inoculum suspensions of the molds were prepared from 7-day (Aspergillus spp., Bipolaris spp., P. boydii, R. arrhizus, and S. schenckii) or 7- to 10-day (B. dermatitidis and H. capsulatum) cultures grown on PDA at 35°C (cultures for Fusarium spp. were grown at 35°C for 48 to 72 h and then at 25 to 28°C until day 7
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Jun 25 21:08:32 UTC 2021
by
admin
on
Fri Jun 25 21:08:32 UTC 2021
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Record UNII |
JFU09I87TR
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C514
Created by
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NDF-RT |
N0000008217
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WHO-ATC |
J02AC03
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WHO-VATC |
QJ02AC03
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NDF-RT |
N0000175487
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LIVERTOX |
1039
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Code System | Code | Type | Description | ||
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121243
Created by
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PRIMARY | RxNorm | ||
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C102790
Created by
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PRIMARY | |||
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DB00582
Created by
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PRIMARY | |||
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N0000182140
Created by
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PRIMARY | Cytochrome P450 2C19 Inhibitors [MoA] | ||
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SUB00087MIG
Created by
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PRIMARY | |||
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CHEMBL638
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PRIMARY | |||
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137234-62-9
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
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PRIMARY | |||
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137234-62-9
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
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PRIMARY | |||
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M11501
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
|
PRIMARY | Merck Index | ||
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C1707
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
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PRIMARY | |||
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7269
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
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PRIMARY | |||
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N0000185504
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
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PRIMARY | Cytochrome P450 2C9 Inhibitors [MoA] | ||
|
1718008
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
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PRIMARY | USP-RS | ||
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JFU09I87TR
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
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PRIMARY | |||
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71616
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
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PRIMARY | |||
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2846
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
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PRIMARY | |||
|
N0000182141
Created by
admin on Fri Jun 25 21:08:32 UTC 2021 , Edited by admin on Fri Jun 25 21:08:32 UTC 2021
|
PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLIC ENZYME -> SUBSTRATE |
IN VITRO
|
||
|
BINDER->LIGAND |
Plasma protein binding is estimated to be 58% and was shown to be independent of plasma concentrations achieved following single and multiple oral doses of 200 mg or 300 mg (approximate range: 0.9-15 mg/ml).
BINDING
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
IN VITRO
|
||
|
METABOLIC ENZYME -> INHIBITOR |
IC50
|
||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
EP
|
||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
IN VITRO
|
||
|
METABOLIC ENZYME -> INHIBITOR |
IC50
|
||
|
EXCRETED UNCHANGED |
URINE
|
||
|
METABOLIC ENZYME -> INHIBITOR |
IC50
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE LESS ACTIVE -> PARENT |
MAJOR
PLASMA
|
||
|
METABOLITE LESS ACTIVE -> PARENT | |||
|
METABOLITE LESS ACTIVE -> PARENT |
MAJOR
PLASMA
|
||
|
METABOLITE -> PARENT |
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
For the calculation of contents, multiply the peak areas by 2.1
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
For the calculation of contents, multiply the peak areas by 0.7
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
For the calculation of contents, multiply the peak areas by 0.7
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
ORAL BIOAVAILABILITY | PHARMACOKINETIC |
|
|
|||
Cmax | PHARMACOKINETIC |
|
Dose |
|
||
Biological Half-life | PHARMACOKINETIC |
|
|
|||
Volume of Distribution | PHARMACOKINETIC |
|
AT STEADY-STATE |
|
||
Tmax | PHARMACOKINETIC |
|
|
|||