Efficacy and Safety of Lorlatinib in Korean Non-Small-Cell Lung Cancer Patients With ALK or ROS1 Rearrangement Whose Disease Failed to Respond to a Previous Tyrosine Kinase Inhibitor

Clin Lung Cancer. 2019 May;20(3):215-221. doi: 10.1016/j.cllc.2018.12.020. Epub 2018 Dec 31.

Abstract

Introduction: Non-small-cell lung cancer (NSCLC) patients harboring ALK or ROS1 rearrangements invariably acquire resistance to the first- and second-generation tyrosine kinase inhibitors (TKIs), most notably ALK G1202R and ROS1 G2032R. Lorlatinib, a novel third-generation TKI, produced remarkable results from the first-in-man phase 1 trial: an overall response rate of 46% and 50% for previously treated ALK- and ROS1-positive patients, respectively. However, the efficacy of lorlatinib has not been widely validated in Asian patients.

Patients and methods: Patients with advanced NSCLC with ALK or ROS1 rearrangements who initiated lorlatinib therapy between November 2016 and July 2018 were retrospectively analyzed.

Results: Twelve consecutive patients were included. The median age was 55 years (range, 36-76 years). Ten (83%) had ALK-positive NSCLC and 2 (17%) had ROS1-positive NSCLC. All patients had a history of first- or second-generation ALK TKI receipt. Two ALK-positive patients and one ROS1-positive patient had the G1202R and G2032R mutations, respectively. The overall response rate was 64% and the disease control rate was 91%. Of the 3 ALK-positive patients with intracranial target lesions, 1 (33%) had a complete response and 2 (67%) a partial response, producing an intracranial objective response of 100%. The median progression-free survival was 6.5 months (range, 1.0-16.5 months). The most common adverse event was hypercholesterolemia (83%), and no adverse event-related dose reductions or treatment discontinuations were reported.

Conclusion: This study is the first to report that lorlatinib is an important novel therapeutic option for Asian patients who have advanced NSCLC harboring ALK/ROS1 mutations whose disease progressed during treatment with first- and second-generation TKIs.

Keywords: Asian; PF-06463922.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Aminopyridines
  • Anaplastic Lymphoma Kinase / genetics
  • Antineoplastic Agents / therapeutic use*
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / genetics
  • Carcinoma, Non-Small-Cell Lung / mortality
  • Drug Resistance, Neoplasm
  • Female
  • Gene Rearrangement
  • Humans
  • Lactams
  • Lactams, Macrocyclic / therapeutic use*
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / genetics
  • Lung Neoplasms / mortality
  • Male
  • Middle Aged
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein-Tyrosine Kinases / genetics
  • Proto-Oncogene Proteins / genetics
  • Pyrazoles
  • Republic of Korea
  • Retrospective Studies

Substances

  • Aminopyridines
  • Antineoplastic Agents
  • Lactams
  • Lactams, Macrocyclic
  • Protein Kinase Inhibitors
  • Proto-Oncogene Proteins
  • Pyrazoles
  • ALK protein, human
  • Anaplastic Lymphoma Kinase
  • Protein-Tyrosine Kinases
  • ROS1 protein, human
  • lorlatinib