valbenazine + ketoconazole

**valbenazine + ketoconazole** is a combination of a selective vesicular monoamine transporter 2 (VMAT2) inhibitor (**valbenazine**) and a potent CYP3A4 inhibitor (**ketoconazole**). Valbenazine is indicated for the treatment of tardive dyskinesia and chorea associated with Huntington’s disease. It acts primarily by reversible inhibition of VMAT2, resulting in presynaptic depletion of dopamine and other monoamines, and does not appreciably bind to dopaminergic, serotonergic, adrenergic, histaminergic, or muscarinic receptors. Ketoconazole, when coadministered, substantially increases valbenazine exposure by inhibiting its CYP3A4-mediated metabolism, which requires adjustment (typically reduction) of valbenazine dosing to mitigate risks of QT prolongation and other exposure-related adverse effects. The combination is not formulated or marketed as a fixed-dose product; instead, ketoconazole is occasionally used concomitantly to investigate or manage drug interactions or as required in cases of fungal infection in patients taking valbenazine[1][3][4][5].

Other names

valbenazineketoconazole