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**Iclepertin + itraconazole** is a combination of **iclepertin**, a small molecule inhibitor of GlyT1 (glycine transporter 1), and **itraconazole**, a triazole antifungal agent and potent inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme. - **Iclepertin** acts by inhibiting GlyT1, increasing glycine concentrations at NMDA receptors in the CNS, aiming to improve cognitive impairment, mainly in patients with schizophrenia and other cognitive disorders[4]. - **Itraconazole** is primarily used to treat fungal infections but here functions as a CYP3A4 inhibitor, which can affect the pharmacokinetics of drugs that are CYP3A4 substrates like iclepertin[4]. - Trials have specifically studied iclepertin in combination with itraconazole to assess drug-drug interactions, demonstrating that itraconazole increases systemic exposure to iclepertin due to CYP3A4 inhibition, but this combination is generally well tolerated without clinically significant safety concerns[4].
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