Drug intelligence / Profile preview

mavelertinib

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Mavelertinib is an orally available, selective, and irreversible small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, specifically targeting mutant forms such as T790M. It was developed for the treatment of non-small cell lung cancer (NSCLC) with EGFR mutations including Del 19 or L858R with or without T790M. Mavelertinib binds to and inhibits EGFR T790M, a mutation associated with acquired resistance to earlier-generation EGFR inhibitors, thereby blocking downstream signaling pathways involved in tumor cell proliferation and survival. The drug shows minimal activity against wild-type EGFR and was designed to reduce dose-limiting toxicities seen with less selective inhibitors. Mavelertinib reached phase II clinical trials but development for NSCLC has been discontinued[1][2][3][4][5]. Recent research also suggests potential for repurposing in giardiasis therapy[7].

Other names
1776112-90-3
02

Targets

EGFR exon 19del (Epidermal growth factor receptor exon 19 deletion mutant)EGFR T790M/C797S (Epidermal growth factor receptor (EGFR) T790M/C797S mutant)EGFR L858R (Epidermal growth factor receptor L858R mutant)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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