Posaconazole (SCH 56592)
For research use only.
CAS No. 171228-49-2
Posaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.
Selleck's Posaconazole (SCH 56592) has been cited by 18 publications
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Comparative mean±SD plasma concentration versus time curves of 40mg/kg oral posaconazole (PSZ) administrated in normolipidemic (NL), intermediate hyperlipidemic (IHL) or extreme hyperlipidemic (HL) rat groups. An insert showing a clear snap of the plasma concentrations for the first 7 h.
Eur J Pharm Sci, 2016, 91:190-195. . Posaconazole (SCH 56592) purchased from Selleck.
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|Description||Posaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.|
|Features||Currently the most advanced candidate for the treatment of Chagas disease.|
Posaconazole has potent trypanocidal activity. Amiodarone acts synergistically with Posaconazole. Posaconazole also affects and disrupts Ca2+ homeostasis in T. cruzi. Posaconazole blocks the biosynthesis of ergosterol, which is essential for parasite survival. Posaconazole has a clear, dose-dependent effect on proliferation of the epimastigote (extracellular) stages, with a minimal inhibitory concentration of 20 nM and an IC50 of 14 nM. Against the clinically relevant intracellular amastigote form of the parasite, Posaconazole is even more potent. Posaconazole has the minimal inhibitory concentration and IC50 values of 3 nM and 0.25 nM.  Posaconazole is active against isolates of Candida and Aspergillus spp. that exhibit resistance to Fluconazole, Voriconazole, and Amphotericin B and is much more active than the other triazoles against zygomycetes. 
|In vivo||Treatment of infected animals with amiodarone alone reduces parasitemia, increases survival 60 days pi (0% for untreated controls vs 40% for amiodarone-treated animals) and, when given in combination with Posaconazole, delays the development of parasitemia.  Coadministration of Posaconazole and Boost Plus increases drug exposure compared to the administration of Posaconazole alone in the fasted state. Food, particularly meals high in fat content, significantly increases Posaconazole bioavailability. Systemic exposure to Posaconazole increases 4- and 2.6-fold when it is consumed with a high-fat and nonfat meal, respectively.  Posaconazole and Amiodarone may constitute an effective anti-T. cruzi therapy with low side effect.  At twice-daily doses of ≥15 mg/kg of body weight, Posaconazole prolongs the survival of the mice and reduces tissue burden. |
-  Benaim G, et al. J Med Chem. 2006, 49(3), 892-389.
-  Sabatelli F, et al. Antimicrob Agents Chemother. 2006, 50(6), 2009-2015.
-  Sansone-Parsons A, et al. Antimicrob Agents Chemother. 2006, 50(5), 1881-1883.
|In vitro||DMSO||100 mg/mL (142.69 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04825275||Not yet recruiting||Drug: Posaconazole Pill||Glioblastoma|Glioblastoma Multiforme|Glioblastoma Multiforme of Brain|Glioblastoma Multiforme Adult||Milton S. Hershey Medical Center||May 2021||Early Phase 1|
|NCT04725942||Not yet recruiting||Drug: Oral Posaconazole tablets||Pulmonary Fungal Infection||Institute of Hematology & Blood Diseases Hospital|Shanxi Bethune Hospital|The Second Hospital of Hebei Medical University|Tianjin Medical University Cancer Institute and Hospital||January 2021||--|
|NCT03717623||Recruiting||Drug: Posaconazole pharmacokinetics||Posaconazole|Pharmacokinetics|Invasive Candidiases|Invasive Aspergillosis|Invasive Mycosis|Fungal Infection|Prophylaxis||Melbourne Health|Merck Sharp & Dohme Corp.||August 1 2019||Phase 4|
|NCT03796533||Unknown status||Drug: Posaconazole||Leukemia Myeloid Acute||Hospices Civils de Lyon||February 2019||Not Applicable|
|NCT04194086||Recruiting||Drug: posaconazole oral suspensions||Leukemia Acute||Zhujiang Hospital|Guangdong Provincial People''s Hospital||November 1 2018||Phase 1|Phase 2|
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