… of pexidartinib using radiolabeled drug and to assess the dose proportionality of pexidartinib
following single oral doses. … received a single oral dose of [ 14 C]‐pexidartinib 400 mg with …

… (A) Dose proportionality in the steady-state … pexidartinib drug level in patients and that
higher doses did not result in increased exposure. Because prolonged and potent inhibition of …

… inhibitor that targets colony-stimulating factor 1 receptor (CSF1R). In the ENLIVEN study,
pexidartinib … Thereafter, pexidartinib was approved in the United States for the treatment of adult …

… enzymes due to induction or inhibition could potentially modify pexidartinib exposure. Overall,
… CYP3A4 inhibitors, or UGT inhibitors. Pexidartinib pharmacokinetics is dose proportional, …

… Pexidartinib, an oral small molecule inhibitor of the colony-… , based on the dose-exposure
proportionality of pexidartinib, to … on the dose-exposure proportionality of pexidartinib, and each …

… Pexidartinib is a kinase inhibitor that induces tumor response and improvements in … dose.
These profiles indicate that pexidartinib exposure was generally dose proportional over the …

… dose-proportional manner over the dose … inhibitors should thus be avoided; if concomitant
use with strong CYP3A or UGT inhibitors cannot be avoided, a reduced pexidartinib dosage (…

… Additionally, a pharmacokinetic (PK) model predicted that a moderate CYP3A4 inhibitor and
… against in vivo data from clinical studies (dose-proportional study in fasted state and food-…

… dose proportional from 400 to 600 mg. ZAAD-1006 (ZAAD), a N-glucuronide, is the primary
plasma metabolite of pexidartinib… a CYP3A4 inducer or inhibitor or a UGT1A4 inhibitor. Given …

… Pexidartinib exposure increased in a generally dose-proportional manner over the dose …
In the first randomized trial in this disease, the oral selective CSF1R inhibitor called pexidartinib …