Carbonic anhydrase inhibitors: a review on the progress of patent literature (2011–2016)

ABSTRACT

Introduction: A large area of carbonic anhydrase (CA) research focuses on the inhibition of human CA IX and CA XII, as these isoforms have been designated as biomarkers and therapeutic targets for various cancer types.

Areas covered: Recently, the majority of CA inhibitor (CAI) patents cover compound design, synthesis, and delivery methods for the treatment of glaucoma and cancer. The analysis of included patents highlights the need for isoform specific inhibitors. This review covers the patents of medically relevant carbonic anhydrase inhibitors between 2011–2016.

Expert opinion: The improvement of structure-based drug design methods and access to the crystal structures of human CA isoforms have improved inhibitor development. This progress can be observed in relation to the selective inhibition of CA IX for cancer treatments, with one inhibitor in clinical trials. However, the design of nonclassical CAIs is essential to further improve isoform specificity and prevent sulfur allergies.

KEYWORDS:

• CA IX
• cancer
• carbonic anhydrase (CA)
• carbonic anhydrase inhibitors (CAIs)
• isoform specificity
• glaucoma

Article highlights

• Carbonic anhydrase inhibitors (CAIs) have been studied in the treatment of diseases, including hypertension, edema, obesity, and epilepsy

• New compounds and synthesis methods have been proposed for the treatment of glaucoma

• There is a need for isoform specific inhibitors of CA in order to avoid off-target side effects

• Recent patents highlight the shift in focus to the inhibition of the cancer target isoform, CA IX, with a collection of new compounds (including antibodies) and improvement in the administration of CAIs

• The development of non-classical CAIs is essential for preventing sulfur allergies

This box summarizes key points contained in the article.

Declaration of interest

The author has 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.

Additional information

Funding

This paper was not funded.