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Pimicotinib (ABSK021/ABSK201) is a potent, highly selective small-molecule inhibitor of the colony-stimulating factor 1 receptor (CSF-1R). It is developed by Abbisko Therapeutics for the treatment of tenosynovial giant cell tumor (TGCT), a condition characterized by the overexpression of CSF-1. The combination of pimicotinib with itraconazole is specifically utilized in Phase 1 clinical trials to evaluate pharmacokinetic drug-drug interactions. Itraconazole, a strong inhibitor of the CYP3A4 enzyme, is administered alongside pimicotinib to determine the extent to which CYP3A4-mediated metabolism affects the systemic exposure and safety profile of pimicotinib. This study is crucial for understanding the metabolic clearance of pimicotinib and for providing dosing recommendations when co-administered with other CYP3A4 modulators.
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