It has been estimated that approximately 30% of current R&D spend in pharmaceutical companies is focused on the development of kinase inhibitors. Protein kinases have become one of the pharmaceutical industry’s most important class of drug target. 

To date 113 current approved drugs target kinases, comprising 103 kinase inhibitors (82 FDA approved) and 10 monoclonal antibodies (9 FDA approved). Please see table below or click pdf to view structures at a higher resolution. They include Gleevec, an inhibitor of the Bcr-Abl tyrosine kinase, which has transformed chronic myelogenous leukaemia from a disease that was rapidly fatal into a manageable condition.

The current global market for kinase therapies is about US$20 billion per annum, forecast to increase markedly. There are over 100 small-molecule kinase inhibitors active in late stages of clinical development and many more are likely to be approved in the coming years. 

As only about 10% of kinases have been studied in detail there is still much to understand on the roles that protein kinases play in human health and disease. 

We believe that development of kinase inhibitors will remain at the forefront of medicine for the foreseeable future. 

Small molecular inhibitors of protein kinases approved for clinical use by the FDA (Updated January 2023)(PDF)

Abbreviations: ALL: Acute Lymphoblastic Leukaemia, GIST: Gastro-Intestinal Stromal Tumour, NSCLC: Non-Small Cell Lung Carcinoma