Evaluating posaconazole, its pharmacology, efficacy and safety for the prophylaxis and treatment of fungal infections

ABSTRACT

Introduction

Invasive fungal diseases (IFDs) are a significant cause of morbidity and mortality among immunocompromised patients. Safe and effective antifungal medications used for prophylaxis and treatment are pivotal in their management. Posaconazole is a promising triazole antifungal agent.

Areas covered

The authors discuss the pharmacological properties of posaconazole, including pharmacokinetics/pharmacodynamics, safety and tolerability profile, together with efficacy data for prophylaxis and treatment as well as its use in special populations based on current literature.

Expert opinion

Posaconazole has a favorable safety and tolerability profile; however, caution is advised when co-administered with agents that are CYP3A4 inhibitors, because their concentration may significantly increase, and their levels should be closely monitored. It has an extended spectrum of activity against yeasts and filamentous fungi. It is successfully used as prophylaxis for patients with acute myeloid leukemia (AML)/myelodysplastic syndrome (MDS) and post-hematopoietic cell transplantation (HCT) with graft-versus-host disease (GVHD). It is the first line treatment for oropharyngeal candidiasis and is also used as a salvage treatment for refractory IFDs. Currently available formulations include the oral suspension, delayed-release tablets and solution for intravenous infusion, all with different PK/PD properties and indications. Its use in children and adolescents is currently being examined in Phase-II clinical trials.

KEYWORDS:

• Posaconazole
• invasive fungal diseases
• review
• efficacy
• safety
• azoles
• candidiasis
• aspergillosis
• rare fungi
• therapy
• prophylaxis

Declaration of interest

E Roilides has received research grants from Gilead Sciences, Merck & Co, Pfizer and Astellas. They are also are/have been a consultant for Astellas, Merck & Co., Gilead Sciences and Pfizer and has served on the speaker’s bureaus of Astellas, Gilead Sciences, Merck & Co., and Pfizer. The author(s) have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This manuscript was not funded.