Pexidartinib is a pyrrolopyridine compound with a 5-chloro-1H-pyrrolo[2,3-b]pyridine core substituted at position 3 by a [6-({[6-(trifluoromethyl)pyridin-3-yl]methyl}amino)pyridin-3-yl]methyl group. It is a potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, KIT, and FLT3 (IC50: 20 nM, 10 nM, and 160 nM, respectively). Approved by the FDA for treating adult patients with symptomatic tenosynovial giant cell tumor (TGCT), it functions as an EC 2.7.10.1 inhibitor and antineoplastic agent. It is classified as a pyrrolopyridine, organochlorine compound, aminopyridine, organofluorine compound, and secondary amino compound.