selumetinib + rifampicin

Selumetinib + rifampicin is the co-administration of two drugs: selumetinib, an oral, selective, non-ATP-competitive inhibitor of MEK1 and MEK2 (mitogen-activated protein kinase kinases 1 and 2), and rifampicin, a well-known antibiotic and potent inducer of cytochrome P450 3A4 (CYP3A4) enzymes. Selumetinib is indicated primarily for the treatment of symptomatic, inoperable plexiform neurofibromas in patients with neurofibromatosis type 1 (NF1)[1][2][3][4][5]. Rifampicin is used to treat bacterial infections such as tuberculosis and acts as a strong CYP3A4 inducer, significantly increasing the metabolism of drugs processed via this pathway, including selumetinib. Combining these two drugs is of pharmacokinetic interest due to the potential for rifampicin to lower the plasma concentration and efficacy of selumetinib by accelerating its metabolism.

Other names

selumetinibrifampin