Drug intelligence / Profile preview

ASK120067 + itraconazole

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

Overview

ASK120067 + itraconazole is a combination of two drugs. - **ASK120067 (limertinib)** is an orally bioavailable, third-generation small molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that selectively and irreversibly targets both sensitizing EGFR mutations and the T790M resistance mutation. It has demonstrated efficacy in non-small cell lung cancer (NSCLC) patients with EGFR T790M mutations who have progressed after first- or second-generation EGFR TKIs. Limertinib also shows activity against other kinases such as BTK and ITK, suggesting potential for broader anti-tumor applications[1][2][3][5][6][8]. - **Itraconazole** is a triazole antifungal agent commonly used to treat fungal infections; it is also known to inhibit CYP3A4 and can increase plasma concentrations of co-administered drugs metabolized by this enzyme. The combination may be studied or used to evaluate pharmacokinetic interactions—itraconazole can increase exposure to ASK120067 by inhibiting its metabolism via CYP3A4—or for other investigational purposes.

Brand names
limertinib
Other names
ASK 120067ASK120067ASK-120067limertinib
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)BTK (Bruton tyrosine kinase)CYP3A4 (Cytochrome P450 3A4)ITK (Interleukin 2-inducible T-cell kinase)

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