PI3K inhibitors in inflammation, autoimmunity and cancer

https://doi.org/10.1016/j.coph.2015.05.017Get rights and content
Under a Creative Commons license
open access

Highlights

  • Preclinical studies support us of PI3K inhibitors in autoimmunity and inflammation.

  • First in class PI3K inhibitor has been approved for treatment of B cell lymphoma.

  • Primary immune deficiency (APDS) caused by gain of function mutations in PIK3CD.

  • PI3K inhibitors may be used to stimulate immune responses against cancer.

  • First inhibitors against the class III PI3K VPS34 have been described.

The healthy immune system protects against infection and malignant transformation without causing significant damage to host tissues. Immune dysregulation results in diverse pathologies including autoimmune disease, chronic inflammatory disorders, allergies as well as immune deficiencies and cancer. Phosphoinositide 3-kinase (PI3K) signalling has been shown to be a key pathway in the regulation of the immune response and continues to be the focus of intense research. In recent years we have gained detailed understanding of PI3K signalling, and saw the development of potent and highly selective small molecule inhibitors, of which several are currently in clinical trials for the treatment of immune-related disorders and cancer. The role of PI3K signalling in the immune response has been the subject of detailed reviews; here we focus on relevant recent progress in pre-clinical and clinical development of PI3K inhibitors.

Cited by (0)