Drug intelligence / Profile preview

olomorasib + itraconazole

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

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.

02

Targets

CYP51A1 (Sterol 14α-demethylase)KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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