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BI 1026706 + itraconazole is a combination of the investigational small molecule BI 1026706, a potent antagonist of the bradykinin 1 receptor (B1R), and itraconazole, an approved antifungal agent that inhibits fungal cytochrome P450-dependent synthesis of ergosterol. BI 1026706 acts by blocking bradykinin B1 receptor-mediated inflammatory signaling, and has been evaluated for anti-inflammatory effects particularly in diseases involving vascular leakage and inflammation, such as diabetic macular edema and experimental lung inflammation. Itraconazole’s primary mechanism is antifungal but it is sometimes co-administered for drug-drug interaction assessment, as in phase 1 pharmacokinetic studies to evaluate CYP450-related metabolism of investigational drugs. The combination is not known to have a unique therapeutic indication beyond such pharmacokinetic interaction studies[4].
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