nilotinib + rifampin

Nilotinib + rifampin is a **combination of nilotinib**, a second-generation BCR-ABL tyrosine kinase inhibitor, and **rifampin**, a potent inducer of CYP3A4. Nilotinib is used primarily for the treatment of chronic myeloid leukemia (CML), particularly in patients with Philadelphia chromosome-positive CML who are resistant or intolerant to prior therapy, including imatinib. Rifampin is an antibiotic mainly used for tuberculosis but is clinically significant as an inducer of CYP3A4 and other drug-metabolizing enzymes. When administered together, rifampin dramatically induces the metabolism of nilotinib via CYP3A4, drastically lowering nilotinib serum concentration and exposure. This combination is generally contraindicated and strongly discouraged for clinical use due to the risk of nilotinib treatment failure from reduced drug exposure[1][2][3][5]. Nilotinib acts by inhibiting the tyrosine kinase activity of BCR-ABL, c-Kit, and PDGF receptors, whereas rifampin's mechanism is inhibition of bacterial RNA polymerase. Their clinical interaction is principally due to rifampin's effect on hepatic enzyme induction, rapidly metabolizing nilotinib to pharmacologically inactive forms[1][2][3][5].

Brand names

RifadinRimactane

Other names

nilotinibumnilotinibrifampicin