An updated patent review on P-glycoprotein inhibitors (2011-2018)

ABSTRACT

Introduction: P-glycoprotein is a complex ATP-ase transporter involved in physiological and pathological functions. In particular, it is involved in the onset of multidrug resistance in cancer, in ocular disease, Chronic Rhinosinusitis, CNS diseases such as Alzheimer, Parkinson, and epilepsy. One of the aims of clinicians and pharmacologists is to monitor P-gp activity through the inhibitors and to use its activity and/or expression in physiological barriers for the early diagnosis of several pathologies. Considering P-glycoprotein activity, several substrates have been characterized but the challenge is to design ‘pure’ P-glycoprotein inhibitors.

Area covered: P-glycoprotein inhibitors display a large spectrum of activities. Here the contents of patents focused on the role of P-glycoprotein inhibitor in modulating MDR in cancer, in bioavailability, in ocular disease and Chronic Rhinosinusitis are reported.

Expert opinion: the use of P-glycoprotein inhibitor sic et simpliciter, or in coadministration with therapeutic agents, for ocular disease, and Chronic Rhinosinusitis is promising and could be suggested for additional trials. By contrast, the bioavailability of the coadministrated drugs, increased by P-glycoprotein inhibitor, deserves a wider discussion, in particular on the pharmacokinetic aspect of both P-glycoprotein inhibitor and the coadministered drug.

KEYWORDS:

• P-glycoprotein inhibitors
• multidrug resistance
• ocular disease
• Chronic Rhinosinusitis
• bioavailability

Article highlights

• Patents focusing on P-glycoprotein inhibitors from 2015 to 2018 are reported in the present article.

• P-glycoprotein inhibitors are useful for reverting MDR in oncology field.

• Moreover, P-glycoprotein is employed as a biomarker and the P-glycoprotein inhibitor as a specific therapeutic agent alone or in administration in Chronic Rhinosinusitis.

• The efficacy of several ocular diseases is increased by coadministration of P-glycoprotein inhibitor and specific drugs for topical use.

This box summarizes key points contained in the article.

Declaration of interest

The authors have no 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. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

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

Additional information

Funding

This paper was not funded.