Drug intelligence / Profile preview

rifampicin + ASK120067

Development stage
Phase 1
Lead developer
Jiangsu Aosaikang Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two drugs: - **Rifampicin** is a well-established antibiotic and a strong inducer of cytochrome P450 3A4 (CYP3A4), commonly used to treat tuberculosis and other bacterial infections. - **ASK120067** (also known as limertinib) is a novel third-generation, mutant-selective, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It targets both EGFR-sensitizing mutations and the T790M resistance mutation. Limertinib covalently binds to EGFR at cysteine 797 in the ATP-binding domain. It has demonstrated promising efficacy in patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring EGFR T790M mutations. The combination has been studied primarily for drug-drug interaction purposes; coadministration with rifampicin significantly reduces exposure to ASK120067 due to CYP3A4 induction[2][1]. This combination is not intended as a therapeutic regimen but rather for pharmacokinetic evaluation.

Brand names
limertinibalflutinib
Other names
limertinibrifampin
02

Targets

rpoB (DNA-directed RNA polymerase subunit beta)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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