Features and properties of pexidartinib

Alternative names	Pexidartinib hydrochloride; Plexxikon 3397; PLX-3397; TURALIO
Class	2 ring heterocyclic compounds; anti-dementias; anti-neoplastics; fluorine compounds; pyridines; pyrroles; small molecules
Mechanism of action	Fms-like tyrosine kinase 3 inhibitors; macrophage colony stimulating factor receptor antagonists; proto oncogene protein c-kit inhibitors
Route of administration	Oral
Pharmacodynamics	Inhibits colony-stimulating factor 1 (CSF1) receptor, KIT proto-oncogene receptor tyrosine kinase (KIT) and FMS-like tyrosine kinase 3 internal tandem duplication mutation (FLT3-ITD); depletes (or shifts polarization of) tumor-associated macrophages and inhibits tumor growth in mouse models
Pharmacokinetics	Generally dose-proportional pharmacokinetics; increased drug exposure if administered with food; drug exposure increased in patients with renal impairment; potential to interact with various other drugs if used concomitantly
Adverse events (occurring in ≥ 15% of pexidartinib recipients)	Hair color changes (depigmentation), fatigue, increased aspartate aminotransferase, increased alanine aminotransferase, dysgeusia, vomiting, periorbital edema, abdominal pain, decreased appetite, pruritus, hypertension and increased alkaline phosphatase
ATC codes
WHO ATC code	LO1X-E (protein kinase inhibitors); LO4A-A (selective immunosuppressants); MO1 (anti-inflammatory and anti-rheumatic products); NO6D-X (other anti-dementia drugs)
EphMRA ATC code	L1H (protein kinase inhibitor anti-neoplastics); L4X (other immunosuppressants); M1 (anti-inflammatory and anti-rheumatic products); N6D (nootropics)
Chemical name	5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine monohydrochloride