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lazertinib

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Overview

Generic Name(s):
lazertinib
NCI Definition [1]:
An orally available third-generation, selective inhibitor of certain forms of the epidermal growth factor receptor (EGFR) with activating mutations, including the resistance mutation T790M, exon 19 deletions (Del19), and the L858R mutation, with potential antineoplastic activity. Upon administration, lazertinib specifically and irreversibly binds to and inhibits selective EGFR mutants, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Lazertinib may inhibit programmed cell death-1 ligand 1 (PD-L1) and inflammatory cytokines in specific cancer cells harboring certain EGFR mutations. Compared to some other EGFR inhibitors, lazertinib may have therapeutic benefits in tumors with T790M- or L858R-mediated drug resistance. In addition, lazertinib penetrates the blood-brain barrier (BBB). This agent shows minimal activity against wild-type EGFR (wtEGFR), and does not cause dose-limiting toxicities, which occur during the use of non-selective EGFR inhibitors and inhibit wtEGFR. EGFR, a receptor tyrosine kinase (RTK) mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.

Clinical Trials

View Clinical Trials for lazertinib

Lazertinib has been investigated in 7 clinical trials, of which 7 are open and 0 are closed. Of the trials investigating lazertinib, 2 are phase 1 (2 open), 2 are phase 1/phase 2 (2 open), 1 is phase 2 (1 open), and 2 are phase 3 (2 open).

EGFR Exon 19 Deletion, EGFR L858R, and EGFR A763_Y764insFQEA are the most frequent biomarker inclusion criteria for lazertinib clinical trials.

Non-small cell lung carcinoma and non-squamous non-small cell lung carcinoma are the most common diseases being investigated in lazertinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Lazertinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating lazertinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
yh25448, yh-25448, yh 25448, lazertinib, gns-1480
Drug Categories [2]:
EGFR inhibitors
Drug Target(s) [2]:
EGFR
NCIT ID [1]:
C148147

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.