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PF-04958242 + itraconazole is a combination of two drugs: PF-04958242, an investigational small molecule developed to be a positive allosteric modulator of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, and itraconazole, a well-established antifungal agent belonging to the triazole class. PF-04958242 is designed to enhance glutamatergic signaling by potentiating AMPA receptor function, with primary indications in cognitive impairment related to schizophrenia and sensorineural hearing loss[1][2][4][5][7][10]. Itraconazole inhibits fungal ergosterol biosynthesis via fungal cytochrome P450 inhibition. No approved combination product is marketed, and this pairing is primarily relevant for drug-drug interaction studies, as itraconazole is known to strongly inhibit CYP3A4, thereby altering the metabolism of drugs such as PF-04958242.
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