pexidartinib (Turalio)

Indications

• tenosynovial giant cell tumor

Dosage

• 400 mg (2 capsules) orally twice daily on an empty stomach

Capsules: 200 mg

Adverse effects

• increased serum lactate dehydrogenase
• increased serum transaminases, serum alkaline phosphatase
• hypophosphatemia
• hair color changes
• increased serum cholesterol
• neutropenia, lymphopenia, anemia
• eye edema
• rash
• dysgeusia

* boxed warning: potentially fatal hepatotoxicity

Mechanism of action

• tyrosine kinase inhibitor, targeting
  • colony stimulating factor 1 receptor (CSF1R),
  • KIT proto-oncogene receptor tyrosine kinase (KIT)
  • FMS-like tyrosine kinase 3 (FLT3) harboring an internal tandem duplication (ITD) mutation.

More general terms

• small inhibitory antineoplastic agent (ib drug)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=25151352
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=73053710