A patent review of anticancer glucocorticoid receptor modulators (2014-present)

ABSTRACT

Introduction: Natural and synthetic glucocorticoids are widely employed in different diseases, among which are hematological and solid tumors. Their use is however associated with a number of serious side effects and by the occurrence of resistance. With the aim of separating their gene transactivating effect, more linked to side effects, from transrepressive properties, associated with therapeutic efficacy, a number of selective glucocorticoid modulators have been identified.

Areas covered: This review summarizes the patent applications from 2014 to present in the field of selective glucocorticoid receptor modulators employed in cancer therapy. Only few patents have been identified, that concern the identification of new molecules or the method of use of already patented compounds. In addition, a discussion of the mechanism of action of these compounds is included.

Expert opinion: Only a very limited number of patents have been applied that concern selective glucocorticoid receptor modulators and their use in cancer. Biological information is scarce for most of these patents; more research is necessary in this field in particular concerning clinical data in order to understand whether it is actually possible to improve the efficacy and therapeutic index of these compounds in cancer therapy.

KEYWORDS:

• Glucocorticoids
• glucocorticoid receptors
• selective glucocorticoid receptor modulators
• cancer

Article Highlights

• Glucocorticoids are widely used in many different diseases among which are hematological and solid tumors.

• They act through their interaction with the glucocorticoid receptor that regulates gene transcription activity.

• To reduce side effects and resistance it has been suggested that dissociating the transactivating and transrepressive activity could be important.

• A small number of compounds with these characteristics have been identified, and, for some, animal studies, and even anecdotical reports in humans have been provided.

• At the moment, it is necessary to continue with research; only when these substances will be tested in clinical trials it will be possible to clarify their real potential.

This box summarizes the 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.