Kinase inhibitors

Protein and (lipid kinases) represent an important target class for treating human disorders, as their aberrant activity underlies a variety of pathologies, ranging from cancer, inflammatory diseases, diabetes, infectious diseases, and cardiovascular disorders.

To date more than 35 small molecule protein kinase inhibitors have been approved for human use around the world. The majority of these are for oncology indications, but a growing number are targeting immune-related conditions such as rheumatoid arthritis (tofacitinib, a Janus kinase 3 inhibitor). Two earlier inhibitors, sirolimus and everolimus (mTOR inhibitors) are used as immunosuppressants to reduce rejection of transplanted organs. Subsequently everolimus has been approved for oncology use, for the treatment of progressive, well-differentiated non-functional, neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin, in patients with unresectable, locally advanced or metastatic disease.

Approved kinase inhibitors (worldwide)

Disease abbreviations: BC (breast cancer), CMML (chronic myelomonocytic leukaemia), CML (chronic myeloid leukaemia), CRC (colorectal cancer), GIST (gastrointestinal cancer), HES (hypereosinophilic syndrome), IPF (idiopathic pulmonary fibrosis), MCL (Mantle cell lymphoma), MTC (medullary thyroid cancer), NSCLC (non-small cell lung cancer), Ph+ B-ALL (Philadelphia chromosome positive acute lymphoblastic leukemia), RA (rheumatoid arthritis), RCC (renal cell carcinoma), SEGA (subependymal giant cell astrocytoma)