Catalog No.S1257 Synonyms: SCH56592
Molecular Weight(MW): 700.78
Posaconazole 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.
Cited by 8 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 purchased from Selleck.
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|Description||Posaconazole 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.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|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||Recruiting||Drug: Posaconazole||Leukemia Myeloid Acute||Hospices Civils de Lyon||February 2019||Not Applicable|
|NCT03421366||Not yet recruiting||Drug: Posaconazole||Cystic Fibrosis||Bayside Health||February 5 2018||--|
|NCT03336502||Completed||Drug: Posaconazole||Fungal Infection||Merck Sharp & Dohme Corp.||December 20 2017||Phase 1|
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