Pharmacologic and clinical evaluation of posaconazole

Abstract

Posaconazole, a broad-spectrum triazole antifungal agent, is approved for the prevention of invasive aspergillosis and candidiasis in addition to the treatment of oropharyngeal candidiasis. There is evidence of efficacy in the treatment and prevention of rarer, more difficult-to-treat fungal infections. Posaconazole oral suspension solution has shown limitations with respect to fasting state absorption, elevated gastrointestinal pH and increased motility. The newly approved delayed-release oral tablet and intravenous solution formulations provide an attractive treatment option by reducing interpatient variability and providing flexibility in critically ill patients. On the basis of clinical experience and further clinical studies, posaconazole was found to be a valuable pharmaceutical agent for the treatment of life-threatening fungal infections. This review will examine the development history of posaconazole and highlight the most recent advances.

Is This the Right Drug or the Dose for the Management of Onychomycosis?

“…The management of onychomycosis is a known to be a challenging endeavor owing to low cure rates and recurrence [75][76][77][78][79][80]. Due to this new molecules are gaining attraction of the researchers and subsequent clinical trials of these molecules indicate an equal investment for pharmaceutical companies.…”

One‐Pot Ullmann C–N Coupling Cyclization Toward Domino Synthesis of Fused Hexacyclic Quinolinotriazoloacridinones Catalyzed by CuI/L‐Proline

“…Heterocycles containing nitrogen atom always possess good biological and pharmacological activities. For example, triazole is a monocycle containing three nitrogen atoms, and some of its derivatives are antifungal agents with the advantages of high efficiency, broad‐spectrum antimicrobial activity . A well‐known example is fluconzaole (Fig.…”

Single‐Dose Pharmacokinetic Properties and Relative Bioavailability of Different Formulations of Posaconazole Oral Suspension in Healthy Volunteers

“…Posaconazole exhibits dose‐proportional pharmacokinetics for doses of up to 800 mg/day when administered after a high‐fat meal . Food has a significant effect on the absorption of posaconazole, which is as expected because posaconazole is lipophilic, highly permeable, and practically insoluble in water . Its poor aqueous solubility and poor dissolution in gastrointestinal fluids limit in vivo bioavailability after oral administration.…”

“…8 Food has a significant effect on the absorption of posaconazole, which is as expected because posaconazole is lipophilic, highly permeable, and practically insoluble in water. 9 Its poor aqueous solubility and poor dissolution in gastrointestinal fluids limit in vivo bioavailability after oral administration. The bioavailability of BCS class II drugs is likely to be dissolution rate limited, so even a small increase in the dissolution rate sometimes results in a large increase in bioavailability.…”