491
Views
37
CrossRef citations to date
0
Altmetric
Review

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

&
Pages 947-956 | Received 04 Mar 2016, Accepted 16 Jun 2016, Published online: 11 Jul 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.

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.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.