Drug intelligence / Profile preview

mobocertinib + rifampin

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Mobocertinib + rifampin is a combination of two drugs: **mobocertinib**, an oral, irreversible tyrosine kinase inhibitor targeting epidermal growth factor receptor (EGFR) exon 20 insertion mutations, and **rifampin**, an oral antibiotic and strong inducer of cytochrome P450 3A (CYP3A). Mobocertinib is approved for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations whose disease has progressed on or after platinum-based chemotherapy[1][3][4]. Rifampin is primarily used to treat tuberculosis and other bacterial infections, but in this combination, its presence is notable because strong CYP3A inducers like rifampin greatly reduce mobocertinib blood levels, and co-administration is strongly contraindicated[2][5].

Brand names
Exkivity
Other names
mobocertinib + rifampin
02

Targets

CYP3A7 (Cytochrome P450 3A7)EGFR ex20ins (Epidermal growth factor receptor exon 20 mutant)

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