Picture of RORgamma Modulators 2016: A comparative analysis of the landscape of RORgamma antagonists and agonists

RORgamma Modulators 2016: A comparative analysis of the landscape of RORgamma antagonists and agonists

April 2016


Retinoic acid-related orphan nuclear receptor gamma (RORgamma) is a hot, but „difficult-to-drug“ target. More than 30 companies are active in drug discovery and development. Technology companies with expertise in discovery of drugs targeting nuclear hormone receptors are preferred partners of Big Pharma and Biotech companies if they have identified novel scaffolds of RORgamma antagonists. More than ten such technology-pharma partnerships have been founded and already lead to first successes. Three RORgamma antagonists (inverse agonists) are already in clinical development and more to follow in 2016 and thereafter. 


The report explains the scientific rationale for discovering antagonists of RORgamma for treatment of autoimmune and inflammatory diseases, but also of agonists of RORgamma for treatment of cancer. Clinical as well as non-clinical data for target validation of RORgamma are provided. Lead and up-side indications for development including the key product profile are discussed. Potential safety concers for novel RORgamma modulators were identified. Drug discovery approaches of technology and pharmaceutical companies are shown regarding strategies in partnering as well as in technologies applied for structure-based drug discovery. Based on the experience in the past, estimates of the required time from start of a discovery program of RORgamma modulators until entry into human studies are calculated. The competitive landscape of RORgamma modulator development and discovery projects is analyzed and the profiles of companies elaborated, separately for unpartnered technology or pharmaceutical companies and for partnerships between technology and pharmaceutical companies.


The report provides an understanding of:



    • The target RORgamma


    • Clinical and non-clinical target validation


    • Clinical lead and up-side indications


    • Drug discovery strategies and technologies


    • Commercial value of drug discovery collaborations


    • R&D timelines from start of screening to first-in-human studies


    • Competitive landscape of RORgamma antagonists


    • Agonists of RORgamma for cancer


    • Profiles of unpartnered technology companies and lead projects


    • R&D Partnerships and their discovery approaches and lead molecules


  • Unpartnered pharmaceutical companies and their programs