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Olomorasib + itraconazole is a non-standard combination of two drugs: olomorasib, an investigational, oral, highly selective, second-generation covalent inhibitor of KRAS G12C developed for the treatment of KRAS G12C-mutant cancers, and itraconazole, a well-established oral antifungal agent in the triazole class. Olomorasib is under development by Lilly primarily for advanced/metastatic non-small cell lung cancer (NSCLC) with KRAS G12C mutation, often in combination with immunotherapy, and acts by inhibiting the oncogenic KRAS G12C protein found in a subset of cancers. Itraconazole is used to treat various fungal infections; its mechanism centers on inhibition of fungal lanosterol 14α-demethylase, disrupting ergosterol synthesis vital for fungal cell membranes. The combination "olomorasib + itraconazole" does not represent an established therapeutic regimen and is not currently a recognized combination therapy for any indication; itraconazole may be used in research for drug interaction or pharmacokinetic studies due to its strong CYP3A4 inhibition, which can affect the metabolism of drugs like olomorasib.
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