Abstract

Pexidartinib is an orally active small molecule inhibitor of tyrosine kinase. It is selective towards the colony-stimulating factor 1 receptor (CSF1R) and has been approved by FDA for the clinical use in tenosynovial giant cell tumor (TGCT). CSF1R is over expressed in various types of solid tumors and facilitates monocyte differentiation and survival of tumor-associated macrophages. TGCT is rare and has over expressed CSF1. Based on the phase III clinical reports, pexidartinib has been approved. To make the treatment economical and for patients’ safety, studies are ongoing to improve synthetic efficiency as well as to reduce associated toxicity. Based on the reported preclinical data, clinical studies are ongoing for various other types of solid tumors. Studies focusing on the use of pexidartinib, a CSF1R inhibitor as potential anticancer therapeutics against different types of solid tumor will play a significant role in the discovery of anticancer agents as well as for the management of other disease conditions.