Lazertinib

Lazertinib

Lazertinib is an oral therapeutic agent designed to target and inhibit certain mutated forms of the epidermal growth factor receptor (EGFR) known to drive tumor growth and progression. By specifically targeting these mutated forms of EGFR, lazertinib offers potential antineoplastic activity, aiming to reduce tumor size and slow disease progression.

Background

EGFR is a type of receptor tyrosine kinase (RTK) that plays an essential role in cell proliferation and the vascularization of tumors. In numerous cancer types, EGFR mutations have been linked to enhanced tumor cell proliferation and malignancy. Thus, targeting these mutations has become an attractive approach in cancer therapeutics.

Mechanism of Action

Upon administration, lazertinib specifically and irreversibly binds to select EGFR mutants. These include the resistance mutation T790M, exon 19 deletions (Del19), and the L858R mutation. By doing so, lazertinib prevents EGFR mutant-mediated signaling, disrupting the tumor cell's ability to proliferate. This selective binding leads to cell death in tumor cells that express these specific EGFR mutations.

Furthermore, lazertinib might also act on the programmed cell death-1 ligand 1 (PD-L1) and certain inflammatory cytokines in cancer cells harboring these specific EGFR mutations. Such action can further enhance the drug's antineoplastic properties.

Therapeutic Advantages

Lazertinib has demonstrated potential therapeutic benefits over some other EGFR inhibitors, especially in situations where tumors exhibit resistance mediated by T790M or L858R mutations. A distinct advantage of lazertinib is its ability to penetrate the blood-brain barrier (BBB), providing an opportunity to target brain metastases.

One of the crucial aspects of lazertinib is its minimal activity against wild-type EGFR (wtEGFR). Many non-selective EGFR inhibitors inhibit wtEGFR, which can lead to dose-limiting toxicities. By sparing the wtEGFR, lazertinib aims to avoid these adverse effects.

Side Effects

Lazertinib does not commonly induce the dose-limiting toxicities that are sometimes seen with the use of non-selective EGFR inhibitors. However, as with any therapeutic agent, side effects can still occur. Patients and healthcare providers should remain vigilant for any unexpected side effects and manage them accordingly.

See Also

• Epidermal growth factor receptor
• Receptor tyrosine kinase
• Cancer therapeutics

References

Lazertinib Resources
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