Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C37H42F2N8O4 |
Molecular Weight | 700.7774 |
Optical Activity | ( - ) |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC[C@@H]([C@H](C)O)N1N=CN(C1=O)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(OC[C@@H]5CO[C@](CN6C=NC=N6)(C5)C7=CC=C(F)C=C7F)C=C4
InChI
InChIKey=RAGOYPUPXAKGKH-XAKZXMRKSA-N
InChI=1S/C37H42F2N8O4/c1-3-35(26(2)48)47-36(49)46(25-42-47)31-7-5-29(6-8-31)43-14-16-44(17-15-43)30-9-11-32(12-10-30)50-20-27-19-37(51-21-27,22-45-24-40-23-41-45)33-13-4-28(38)18-34(33)39/h4-13,18,23-27,35,48H,3,14-17,19-22H2,1-2H3/t26-,27+,35-,37-/m0/s1
Molecular Formula | C37H42F2N8O4 |
Molecular Weight | 700.7774 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022003s021,205053s005,205596s004lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/18035188
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022003s021,205053s005,205596s004lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/18035188
Posaconazole is a triazole antifungal drug that is used to treat invasive infections by Candida species and Aspergillus species in severely immunocompromised patients. It marketed in the United States, the European Union, and in other countries by Schering-Plough under the trade name Noxafil. Noxafil is used for prophylaxis of invasive Aspergillus and Candida infections in patients, 13 years of age and older, who are at high risk of developing these infections due to being severely immunocompromised as a result of procedures such as hematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD), or due to hematologic malignancies with prolonged neutropenia from chemotherapy. Also for the treatment of oropharyngeal candidiasis, including oropharyngeal candidiasis refractory to itraconazole and/or fluconazole. Posaconazole blocks the synthesis of ergosterol, a key component of the fungal cell membrane, through the inhibition of cytochrome P-450 dependent enzyme lanosterol 14α-demethylase responsible for the conversion of lanosterol to ergosterol in the fungal cell membrane. This results in an accumulation of methylated sterol precursors and a depletion of ergosterol within the cell membrane thus weakening the structure and function of the fungal cell membrane. This may be responsible for the antifungal activity of posaconazole. It is absorbed within three to five hours and predominately eliminated through the liver, and has a half-life of about 35 hours. Oral administration of posaconazole taken with a high-fat meal exceeds 90% bioavailability and increases the concentration by four times compared to fasting state.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1780 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16107193 |
25.0 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | NOXAFIL Approved UseNoxafil is an azole antifungal agent indicated for: injection, delayed-release tablets, and oral suspension prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised, such as HSCT recipients with GVHD or those with hematologic malignancies with prolonged neutropenia from chemotherapy. (1.1) Oral suspension treatment of oropharyngeal candidiasis (OPC), including OPC refractory (rOPC) to itraconazole and/or fluconazole. (1.2) 1.1 Prophylaxis of Invasive Aspergillus and Candida Infections Noxafil® injection, delayed-release tablets, and oral suspension are indicated for prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised, such as hematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD) or those with hematologic malignancies with prolonged neutropenia from chemotherapy. Noxafil injection is indicated in patients 18 years of age and older. Noxafil delayed-release tablets and oral suspension are indicated in patients 13 years of age and older. 1.2 Treatment of Oropharyngeal Candidiasis Including Oropharyngeal Candidiasis Refractory to Itraconazole and/or Fluconazole Noxafil oral suspension is indicated for the treatment of oropharyngeal candidiasis, including oropharyngeal candidiasis refractory to itraconazole and/or fluconazole. Launch Date2006 |
|||
Preventing | NOXAFIL Approved UseNoxafil is an azole antifungal agent indicated for: injection, delayed-release tablets, and oral suspension prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised, such as HSCT recipients with GVHD or those with hematologic malignancies with prolonged neutropenia from chemotherapy. (1.1) Oral suspension treatment of oropharyngeal candidiasis (OPC), including OPC refractory (rOPC) to itraconazole and/or fluconazole. (1.2) 1.1 Prophylaxis of Invasive Aspergillus and Candida Infections Noxafil® injection, delayed-release tablets, and oral suspension are indicated for prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised, such as hematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD) or those with hematologic malignancies with prolonged neutropenia from chemotherapy. Noxafil injection is indicated in patients 18 years of age and older. Noxafil delayed-release tablets and oral suspension are indicated in patients 13 years of age and older. 1.2 Treatment of Oropharyngeal Candidiasis Including Oropharyngeal Candidiasis Refractory to Itraconazole and/or Fluconazole Noxafil oral suspension is indicated for the treatment of oropharyngeal candidiasis, including oropharyngeal candidiasis refractory to itraconazole and/or fluconazole. Launch Date2006 |
|||
Curative | NOXAFIL Approved UseNoxafil is an azole antifungal agent indicated for: injection, delayed-release tablets, and oral suspension prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised, such as HSCT recipients with GVHD or those with hematologic malignancies with prolonged neutropenia from chemotherapy. (1.1) Oral suspension treatment of oropharyngeal candidiasis (OPC), including OPC refractory (rOPC) to itraconazole and/or fluconazole. (1.2) 1.1 Prophylaxis of Invasive Aspergillus and Candida Infections Noxafil® injection, delayed-release tablets, and oral suspension are indicated for prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised, such as hematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD) or those with hematologic malignancies with prolonged neutropenia from chemotherapy. Noxafil injection is indicated in patients 18 years of age and older. Noxafil delayed-release tablets and oral suspension are indicated in patients 13 years of age and older. 1.2 Treatment of Oropharyngeal Candidiasis Including Oropharyngeal Candidiasis Refractory to Itraconazole and/or Fluconazole Noxafil oral suspension is indicated for the treatment of oropharyngeal candidiasis, including oropharyngeal candidiasis refractory to itraconazole and/or fluconazole. Launch Date2006 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2764 ng/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
935 ng/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
|
1060 ng/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
2840 ng/mL |
300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3280 ng/mL |
300 mg 1 times / day multiple, intravenous dose: 300 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
POSACONAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9093 ng × h/mL |
400 mg 2 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
51618 ng × h/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
26200 ng × h/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
|
38400 ng × h/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
46400 ng × h/mL |
300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
36100 ng × h/mL |
300 mg 1 times / day multiple, intravenous dose: 300 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
POSACONAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
31.7 h |
400 mg 2 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
31 h |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
24.6 h |
300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2% |
300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
[NO STEREO] POSACONAZOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2% |
300 mg 1 times / day multiple, intravenous dose: 300 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
POSACONAZOLE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
300 mg 2 times / day multiple, intravenous Recommended Dose: 300 mg, 2 times / day Route: intravenous Route: multiple Dose: 300 mg, 2 times / day Sources: Page: p.3 |
unhealthy, 51.55 n = 237 Health Status: unhealthy Condition: Invasive fungal infections Age Group: 51.55 Sex: M+F Population Size: 237 Sources: Page: p.3 |
Disc. AE: Rash... AEs leading to discontinuation/dose reduction: Rash (0.84%) Sources: Page: p.3 |
1600 mg 1 times / day multiple, oral Highest studied dose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: Page: p.1310 |
unhealthy n = 3 Health Status: unhealthy Condition: Invasive fungal infections Population Size: 3 Sources: Page: p.1310 |
Disc. AE: Hepatic enzyme increased... Other AEs: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Hepatic enzyme increased (67%) Other AEs:Nausea (67%) Sources: Page: p.1310Vomiting (67%) Diarrhea (67%) Somnolence (67%) |
200 mg 3 times / day multiple, oral Recommended Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: Page: p.12 |
unhealthy n = 605 Health Status: unhealthy Condition: Aspergillus infections|Candida infections Population Size: 605 Sources: Page: p.12 |
Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (2%) Sources: Page: p.12Vomiting (2%) Hepatic enzymes increased (2%) |
300 mg 2 times / day multiple, intravenous Recommended Dose: 300 mg, 2 times / day Route: intravenous Route: multiple Dose: 300 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Aspergillus infections|Candida infections Sources: Page: p.1 |
Disc. AE: Arrhythmia, Electrocardiogram QTc interval prolonged... AEs leading to discontinuation/dose reduction: Arrhythmia Sources: Page: p.1Electrocardiogram QTc interval prolonged Hepatotoxicity |
400 mg 1 times / day multiple, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: p.13 |
unhealthy n = 557 Health Status: unhealthy Condition: Oropharyngeal Candidiasis Population Size: 557 Sources: Page: p.13 |
Disc. AE: Pneumonia... AEs leading to discontinuation/dose reduction: Pneumonia (1%) Sources: Page: p.13 |
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.14 |
unhealthy n = 239 Health Status: unhealthy Condition: Oropharyngeal Candidiasis Population Size: 239 Sources: Page: p.14 |
Disc. AE: Pulmonary function impairment, AIDS... AEs leading to discontinuation/dose reduction: Pulmonary function impairment (3%) Sources: Page: p.14AIDS (7%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Rash | 0.84% Disc. AE |
300 mg 2 times / day multiple, intravenous Recommended Dose: 300 mg, 2 times / day Route: intravenous Route: multiple Dose: 300 mg, 2 times / day Sources: Page: p.3 |
unhealthy, 51.55 n = 237 Health Status: unhealthy Condition: Invasive fungal infections Age Group: 51.55 Sex: M+F Population Size: 237 Sources: Page: p.3 |
Diarrhea | 67% | 1600 mg 1 times / day multiple, oral Highest studied dose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: Page: p.1310 |
unhealthy n = 3 Health Status: unhealthy Condition: Invasive fungal infections Population Size: 3 Sources: Page: p.1310 |
Nausea | 67% | 1600 mg 1 times / day multiple, oral Highest studied dose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: Page: p.1310 |
unhealthy n = 3 Health Status: unhealthy Condition: Invasive fungal infections Population Size: 3 Sources: Page: p.1310 |
Somnolence | 67% | 1600 mg 1 times / day multiple, oral Highest studied dose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: Page: p.1310 |
unhealthy n = 3 Health Status: unhealthy Condition: Invasive fungal infections Population Size: 3 Sources: Page: p.1310 |
Vomiting | 67% | 1600 mg 1 times / day multiple, oral Highest studied dose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: Page: p.1310 |
unhealthy n = 3 Health Status: unhealthy Condition: Invasive fungal infections Population Size: 3 Sources: Page: p.1310 |
Hepatic enzyme increased | 67% Disc. AE |
1600 mg 1 times / day multiple, oral Highest studied dose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: Page: p.1310 |
unhealthy n = 3 Health Status: unhealthy Condition: Invasive fungal infections Population Size: 3 Sources: Page: p.1310 |
Hepatic enzymes increased | 2% Disc. AE |
200 mg 3 times / day multiple, oral Recommended Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: Page: p.12 |
unhealthy n = 605 Health Status: unhealthy Condition: Aspergillus infections|Candida infections Population Size: 605 Sources: Page: p.12 |
Nausea | 2% Disc. AE |
200 mg 3 times / day multiple, oral Recommended Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: Page: p.12 |
unhealthy n = 605 Health Status: unhealthy Condition: Aspergillus infections|Candida infections Population Size: 605 Sources: Page: p.12 |
Vomiting | 2% Disc. AE |
200 mg 3 times / day multiple, oral Recommended Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: Page: p.12 |
unhealthy n = 605 Health Status: unhealthy Condition: Aspergillus infections|Candida infections Population Size: 605 Sources: Page: p.12 |
Arrhythmia | Disc. AE | 300 mg 2 times / day multiple, intravenous Recommended Dose: 300 mg, 2 times / day Route: intravenous Route: multiple Dose: 300 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Aspergillus infections|Candida infections Sources: Page: p.1 |
Electrocardiogram QTc interval prolonged | Disc. AE | 300 mg 2 times / day multiple, intravenous Recommended Dose: 300 mg, 2 times / day Route: intravenous Route: multiple Dose: 300 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Aspergillus infections|Candida infections Sources: Page: p.1 |
Hepatotoxicity | Disc. AE | 300 mg 2 times / day multiple, intravenous Recommended Dose: 300 mg, 2 times / day Route: intravenous Route: multiple Dose: 300 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Aspergillus infections|Candida infections Sources: Page: p.1 |
Pneumonia | 1% Disc. AE |
400 mg 1 times / day multiple, oral Recommended Dose: 400 mg, 1 times / day Route: oral Route: multiple Dose: 400 mg, 1 times / day Sources: Page: p.13 |
unhealthy n = 557 Health Status: unhealthy Condition: Oropharyngeal Candidiasis Population Size: 557 Sources: Page: p.13 |
Pulmonary function impairment | 3% Disc. AE |
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.14 |
unhealthy n = 239 Health Status: unhealthy Condition: Oropharyngeal Candidiasis Population Size: 239 Sources: Page: p.14 |
AIDS | 7% Disc. AE |
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: Page: p.14 |
unhealthy n = 239 Health Status: unhealthy Condition: Oropharyngeal Candidiasis Population Size: 239 Sources: Page: p.14 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
Page: 15.0 |
no | |||
Page: 15.0 |
no | |||
Page: 15.0 |
no | |||
yes [IC50 3 uM] | ||||
yes [IC50 6 uM] | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/022003s000_Noxafil_ClinPharmR.pdf Page: 3.0 |
yes | |||
yes | ||||
yes | yes (co-administration study) Comment: concommitant administration of psconazole with midazolam increases midazolam plasma concentritons by 5-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022003Orig1s026,205053Orig1s010,205596Orig1s010lbl.pdf Page: 17.0 |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022003Orig1s026,205053Orig1s010,205596Orig1s010lbl.pdf Page: 16, 17, 27 |
yes | yes (co-administration study) Comment: rifabutin decreases posaconazole plasma concentrations Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022003Orig1s026,205053Orig1s010,205596Orig1s010lbl.pdf Page: 16, 17, 27 |
PubMed
Title | Date | PubMed |
---|---|---|
Activity of a new triazole, Sch 56592, compared with those of four other antifungal agents tested against clinical isolates of Candida spp. and Saccharomyces cerevisiae. | 1997 Feb |
|
In vitro susceptibilities of Candida bloodstream isolates to the new triazole antifungal agents BMS-207147, Sch 56592, and voriconazole. | 1998 Dec |
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In-vitro and in-vivo activities of SCH56592 against Cryptococcus neoformans. | 1999 Dec |
|
Activities of caspofungin, itraconazole, posaconazole, ravuconazole, voriconazole, and amphotericin B against 448 recent clinical isolates of filamentous fungi. | 2003 Aug |
|
Posaconazole: a broad-spectrum triazole antifungal. | 2005 Dec |
|
In vitro activities of posaconazole, fluconazole, itraconazole, voriconazole, and amphotericin B against a large collection of clinically important molds and yeasts. | 2006 Jun |
|
Isavuconazole: a comprehensive review of spectrum of activity of a new triazole. | 2010 Nov |
|
Multilaboratory testing of two-drug combinations of antifungals against Candida albicans, Candida glabrata, and Candida parapsilosis. | 2011 Apr |
|
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 |
|
Triazole and echinocandin MIC distributions with epidemiological cutoff values for differentiation of wild-type strains from non-wild-type strains of six uncommon species of Candida. | 2011 Nov |
|
Effect of pH on in vitro susceptibility of Candida glabrata and Candida albicans to 11 antifungal agents and implications for clinical use. | 2012 Mar |
|
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. | 2013 Nov |
Patents
Sample Use Guides
Injection:
Loading dose: 300 mg Noxafil injection intravenously twice a day on the first day. Maintenance dose: 300 mg Noxafil injection intravenously once a day, starting on the second day.
Oral suspension:
Prophylaxis of invasive Aspergillus and Candida infections: 200 mg (5 mL) three times a day.
Oropharyngeal Candidiasis: Loading dose: 100 mg (2.5 mL) twice a day on the first day. Maintenance dose: 100 mg (2.5 mL) once a day for 13 days.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27799353
Curator's Comment: The HL-60 leukemia cell line was differentiated to a neutrophil-like phenotype (dHL-60 cells) then exposed to a range of posaconazole concentrations. The functional capacity and antifungal activity of these cells were assessed in vitro. Posaconazole accumulates to high concentrations in dHL-60 cells, and increases their antifungal activity in vitro and in vivo.
Unknown
Substance Class |
Chemical
Created
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on
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Fri Dec 15 15:37:24 GMT 2023
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Record UNII |
6TK1G07BHZ
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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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NDF-RT |
N0000008217
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WHO-ATC |
J02AC04
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WHO-VATC |
QJ02AC04
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NCI_THESAURUS |
C514
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NDF-RT |
N0000175487
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CFR |
21 CFR 524.1610
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FDA ORPHAN DRUG |
850521
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FDA ORPHAN DRUG |
187604
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FDA ORPHAN DRUG |
539016
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LIVERTOX |
NBK548934
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6TK1G07BHZ
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PRIMARY | |||
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C61500
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JJ-48
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282446
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SUB20322
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admin on Fri Dec 15 15:37:24 GMT 2023 , Edited by admin on Fri Dec 15 15:37:24 GMT 2023
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100000089529
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admin on Fri Dec 15 15:37:24 GMT 2023 , Edited by admin on Fri Dec 15 15:37:24 GMT 2023
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171228-49-2
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m8993
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admin on Fri Dec 15 15:37:24 GMT 2023 , Edited by admin on Fri Dec 15 15:37:24 GMT 2023
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PRIMARY | Merck Index | ||
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64355
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admin on Fri Dec 15 15:37:24 GMT 2023 , Edited by admin on Fri Dec 15 15:37:24 GMT 2023
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7421
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CHEMBL1397
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POSACONAZOLE
Created by
admin on Fri Dec 15 15:37:24 GMT 2023 , Edited by admin on Fri Dec 15 15:37:24 GMT 2023
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3483
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admin on Fri Dec 15 15:37:24 GMT 2023 , Edited by admin on Fri Dec 15 15:37:24 GMT 2023
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7713
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6TK1G07BHZ
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468595
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DTXSID6049066
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DB01263
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C101425
Created by
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Related Record | Type | Details | ||
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TARGET ORGANISM->INHIBITOR |
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TRANSPORTER -> SUBSTRATE | |||
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
FECAL
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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BINDER->LIGAND |
BINDING
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
MINOR
FECAL; URINE
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METABOLITE -> PARENT |
MINOR
PLASMA; URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
up to 28% in plasma, 1.4% urine; major posaconazole-​glucuronide produced from human liver microsomes was mediated via UGT1A4 (In vitro, Drug Metabolism and Disposition, Volume 32, Issue 2, Pages 267-271, Journal 2004)
MAJOR
PLASMA; URINE
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METABOLITE -> PARENT |
MINOR
FECAL; PLASMA; URINE
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
process impurity
Raw material used for prodcution of starting material SPOE
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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Injection PHARMACOKINETIC PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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Elimination PHARMACOKINETIC PHARMACOKINETIC PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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