Lazcluze (lazertinib)

To treat non-small cell lung cancer

FDA Approval: 8/19/2024

Research Synopsis

  • * Research has shown that lazertinib is effective in managing advanced NSCLC, with a notable overall response rate in clinical trials, such as 55.3% in patients with EGFR T790M mutation after prior TKI treatments.
  • * A study highlighted that lazertinib was well-tolerated by patients, with mild side effects such as rash being the most common, and no significant cardiac safety concerns reported.
  • * However, resistance mechanisms, specifically the EGFR C797S mutation, have been identified that can lead to treatment failure with lazertinib, indicating the need for ongoing research to overcome resistance.
  • * Lazertinib has been studied in combination therapies, such as with amivantamab, showing promise for increased effectiveness compared to single-agent treatments.
  • * Comparing lazertinib to other third-generation inhibitors, research indicates that it could offer fewer side effects and improved tolerability for patients with specific EGFR mutations.
  • * A recent pharmacokinetic study found that acid-reducing agents did not significantly affect the pharmacokinetics of lazertinib, thus no dosage adjustments are necessary when these agents are used.
  • * Laboratory research involving lazertinib suggests it may enhance the efficacy of traditional chemotherapeutic agents against multidrug-resistant cancer cells, indicating potential for broader application in treatment regimens.
  • * Overall, lazertinib represents a significant advancement in the treatment of EGFR mutation-positive NSCLC, with ongoing studies aiming to refine its use and address resistance challenges in the clinical setting.
  • * Future research directions include exploring combination therapies and developing next-generation EGFR inhibitors that can target multiple mutations effectively, further improving outcomes for patients with advanced lung cancer.

Related articles

Research articles about Lazcluze (lazertinib)

Lazcluze (lazertinib)

Lazertinib in patients with EGFR mutation-positive advanced non-small-cell lung cancer: results from the dose escalation and dose expansion parts of a first-in-human, open-label, multicentre, phase 1-2 study.

London, UK

2 hours ago

1 Received

  • * Conducted in Korea, the trial involved 127 patients and focused on the drug's safety, tolerability, and effectiveness, with no significant adverse effects reported during the dose escalation and expansion phases.
  • * The most common side effects were mild skin reactions, such as rash and itching, with the study ongoing to further assess the drug's impact.

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EGFR C797S as a Resistance Mechanism of Lazertinib in Non-small Cell Lung Cancer with EGFR T790M Mutation.

London, UK

2 hours ago

1 Received

  • * Third-generation EGFR TKIs, such as lazertinib, are now considered standard treatments for these resistant cases, showing early promise in clinical trials.
  • * The research reports an instance where a patient developed resistance to lazertinib due to an additional mutation (EGFR C797S) in their cancer cells, highlighting the need for further understanding of resistance mechanisms.

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Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC.

London, UK

2 hours ago

1 Received

  • Osimertinib is the current standard treatment for advanced EGFR+ NSCLC, with almonertinib approved in China in March 2020 for a specific mutation (EGFR T790M).
  • The review highlights various third-generation EGFR TKIs under late-stage clinical development, discussing their trial results, study designs, and chemical structures when available.
  • It also summarizes past clinical trial results of other third-generation TKIs and details ongoing combination trials that could lead to new standard treatments for advanced EGFR+ NSCLC.

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Lazertinib: First Approval.

London, UK

2 hours ago

1 Received

  • Lazertinib (LECLAZA) is an oral, third-generation EGFR tyrosine kinase inhibitor aimed at treating non-small cell lung cancer (NSCLC).
  • It specifically targets the T790M mutation and certain activating mutations in the EGFR gene, while avoiding effects on the normal EGFR gene.
  • The drug gained its first approval in January 2021 for patients with advanced or metastatic NSCLC who have the T790M mutation and have previously undergone EGFR-TKI treatment.

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Correction to: Lazertinib: First Approval.

London, UK

2 hours ago

1 Received

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Cardiac Safety Assessment of Lazertinib: Findings From Patients With Mutation-Positive Advanced NSCLC and Preclinical Studies.

London, UK

2 hours ago

1 Received

  • Lazertinib is a third-generation EGFR TKI that effectively targets specific mutations found in non-small cell lung cancer (NSCLC) while minimizing heart-related side effects.
  • The study evaluated the cardiac safety of lazertinib in patients with mutation-positive NSCLC, analyzing various cardiac parameters and conducting preclinical studies.
  • Results showed no significant QT prolongation or decreases in left ventricular ejection fraction among the participants, suggesting that lazertinib is safe for cardiac health in this patient population.

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Chronicles of EGFR Tyrosine Kinase Inhibitors: Targeting EGFR C797S Containing Triple Mutations.

London, UK

2 hours ago

1 Received

  • EGFR is a key player in many cancers, with mutations driving its activation, particularly in non-small cell lung cancer (NSCLC), where specific mutations like L858R and Del19 are common.
  • First-generation EGFR tyrosine kinase inhibitors (TKIs) like gefitinib have benefits but face limits due to the development of the T790M mutation after a few months of treatment, leading to reduced efficacy.
  • Newer third-generation TKIs like osimertinib aim to be selective for certain mutations but are still hindered by complications from additional mutations like C797S, highlighting the need for the next generation of EGFR inhibitors that can target these triple mutations effectively.

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MARIPOSA: phase 3 study of first-line amivantamab + lazertinib versus osimertinib in EGFR-mutant non-small-cell lung cancer.

London, UK

2 hours ago

1 Received

  • Third-generation EGFR tyrosine kinase inhibitors (TKIs), like osimertinib, are effective for -mutant non-small-cell lung cancer but most patients eventually experience relapse.
  • Amivantamab is a bispecific antibody that targets both activating and resistance mutations, and when combined with lazertinib, shows promise in treating patients both new to treatment and those who have relapsed after osimertinib.
  • The MARIPOSA study is a phase 3 trial that aims to compare the effectiveness and safety of the amivantamab-lazertinib combo with osimertinib alone for treating -mutant non-small-cell lung cancer.

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Lazertinib improves the efficacy of chemotherapeutic drugs in ABCB1 or ABCG2 overexpression cancer cells i, , and .

London, UK

2 hours ago

1 Received

  • Multidrug resistance (MDR) is a key factor in chemotherapy failure, primarily due to the overexpression of ABC transporters like ABCB1 and ABCG2, and currently, no MDR modulators are approved for clinical use.
  • Researchers found that lazertinib, a third-generation tyrosine kinase inhibitor, can boost the effectiveness of anticancer drugs that are substrates for these MDR transporters by inhibiting their drug efflux activities.
  • Lazertinib works by competitively binding to the ATP-binding site of ABCB1 and ABCG2, preventing drug transport out of the cancer cells, thus enhancing the accumulation of chemotherapy drugs without altering transporter expression or other associated signaling pathways.

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The Challenges of Third-Generation EGFR Tyrosine Kinase Inhibitors in the Therapy of Advanced NSCLC.

London, UK

2 hours ago

1 Received

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A Phase 1/2 Study of Lazertinib 240 mg in Patients With Advanced EGFR T790M-Positive NSCLC After Previous EGFR Tyrosine Kinase Inhibitors.

London, UK

2 hours ago

1 Received

  • This study assessed lazertinib, a new drug for treating advanced NSCLC (non-small cell lung cancer) with the EGFR T790M mutation in patients who had previously been treated with other EGFR inhibitors.
  • A total of 78 patients participated, showing a 55.3% overall response rate, with 1 patient achieving a complete response and many others experiencing partial responses, along with promising results for those with brain metastases.
  • Lazertinib was generally well-tolerated, with common side effects being mild to moderate, although some serious adverse effects were noted; the overall findings suggest lazertinib is effective for this patient group.

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Studies on ligand-based pharmacophore modeling approach in identifying potent future EGFR inhibitors.

London, UK

2 hours ago

1 Received

  • The study explores the role of epidermal growth factor receptor (EGFR) as a target for cancer treatments, noting that mutations in EGFR can lead to drug resistance.
  • Researchers are developing new drugs by creating a pharmacophore model based on existing EGFR inhibitors to identify safe and effective molecules using computational methods.
  • The approach successfully screened a large database of potential ligands, identifying the top candidates for further testing in biological studies, which could lead to promising new inhibitors for EGFR in cancer therapy.

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[Analysis of the Effcacy and Safety of Amivantamab in Non-small Cell Lung Cancer 
Patients with EGFR/MET Gene Abnormalities: A Single Center's Experience].

London, UK

2 hours ago

1 Received

  • - This study evaluates the effectiveness and safety of Amivantamab, a monoclonal antibody that targets both EGFR and c-Met, in Chinese patients with non-small cell lung cancer (NSCLC) who have specific gene abnormalities.
  • - Of the 15 enrolled patients, 6 received Amivantamab alone while 9 received it with Lazertinib, showing a partial response rate of 46.7% and a disease control rate of 100% for those with EGFR exon 20 insertions.
  • - The treatment was generally well-tolerated, with common side effects like rash and paronychia, most being mild (grades 1-2), while more severe adverse effects were rare

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Amivantamab Emerges Positively from Its "Chrysalis".

London, UK

2 hours ago

1 Received

  • * In the phase I/Ib CHRYSALIS-2 study, amivantamab showed promising results when combined with lazertinib, also yielding a 33% overall response rate among patients whose cancer progressed after osimertinib treatment.
  • * Patients in the CHRYSALIS-2 study had a median overall survival of 14.8 months, indicating potential benefits of this treatment combination for those with advanced lung cancer.

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Lazertinib: on the Way to Its Throne.

London, UK

2 hours ago

1 Received

  • - Lazertinib is a third-generation oral medication that targets specific mutations in the EGFR gene, particularly effective for advanced non-small cell lung cancer (NSCLC) patients who have already undergone EGFR TKI therapy.
  • - Approved in January 2021, lazertinib has shown promising anti-tumor effects at a dose of 240 mg, with potential for fewer side effects compared to other treatments like osimertinib.
  • - Current research is exploring lazertinib’s use as a standalone treatment and in combination with other drugs, with ongoing studies aimed at enhancing its effectiveness for EGFR-mutant NSCLC patients.

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And Still They Come Over Troubled Waters: Can Asia's Third-Generation EGFR Tyrosine Kinase Inhibitors (Furmonertinib, Aumolertinib, Rezivertinib, Limertinib, Befotertinib, SH-1028, and Lazertinib) Affect Global Treatment of EGFR+ NSCLC.

London, UK

2 hours ago

1 Received

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Amivantamab in the Treatment of Metastatic NSCLC: Patient Selection and Special Considerations.

London, UK

2 hours ago

1 Received

  • Amivantamab is a bispecific antibody that gained FDA accelerated approval in May 2021 for treating non-small cell lung cancer (NSCLC) patients with specific EGFR exon 20 insertions after chemotherapy failure.
  • It works by blocking interactions and dimerization of the EGFR and MET receptors, promoting cell death and reducing receptor levels on the cell surface.
  • Early clinical trials showed a 40% response rate in patients with EGFR exon 20 insertions and ongoing Phase III trials are exploring its effectiveness in combination with chemotherapy and other therapies for various NSCLC mutations.

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Effects of Acid-Reducing Agents on the Pharmacokinetics of Lazertinib in Patients with EGFR Mutation-Positive Advanced Non-Small-Cell Lung Cancer.

London, UK

2 hours ago

1 Received

  • Lazertinib is a medication used to treat advanced EGFR mutation-positive non-small-cell lung cancer, and its effectiveness can be impacted by the use of acid-reducing agents (ARAs).
  • This study involved 234 patients and compared the pharmacokinetics of lazertinib in patients taking ARAs with those not taking them, particularly looking at key concentration metrics.
  • The results indicated no significant difference in the pharmacokinetics between the two groups, meaning ARAs do not require any dosage adjustments for lazertinib treatment.

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Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).

London, UK

2 hours ago

1 Received

  • Lazertinib (YH25448) is a new third-generation tyrosine kinase inhibitor aimed at treating EGFR mutant non-small cell lung cancer.
  • Researchers studied the crystal structures of lazertinib in complex with both wild-type and mutant EGFR to understand how it binds compared to other similar TKIs.
  • The findings reveal that lazertinib's unique binding interactions improve its effectiveness against EGFR mutations and suggest new strategies for designing better tyrosine kinase inhibitors in the future.

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