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Efficacy and Safety of Rezivertinib (BPI-7711) in Patients With Locally Advanced or Metastatic/Recurrent EGFR
Yuankai Shi1, Shiman Wu2, Ke Wang3
1Department of Medical Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing Key Laboratory of Clinical Study on Anticancer Molecular Targeted Drugs, Beijing, People's Republic of China.
Introduction:
Rezivertinib (BPI-7711) is a novel third-generation EGFR tyrosine kinase inhibitor (TKI) targeting both EGFR-sensitizing mutations and EGFR T790M mutation. This study aimed to evaluate the efficacy and safety of rezivertinib in patients with locally advanced or metastatic/recurrent EGFR T790M-mutated NSCLC.
Methods:
Patients with locally advanced or metastatic/recurrent NSCLC with confirmed EGFR T790M mutation who progressed after first-/second-generation EGFR TKI therapy or primary EGFR T790M mutation were enrolled. Patients received rezivertinib at 180 mg orally once daily until disease progression, unacceptable toxicity, or withdrawal of consent. The primary end point was objective response rate (ORR) assessed by blinded independent central review per Response Evaluation Criteria in Solid Tumors version 1.1. Secondary end points included disease control rate (DCR), duration of response, progression-free survival (PFS), overall survival, and safety. This study is registered with Clinical Trials.gov (NCT03812809).
Results:
A total of 226 patients were enrolled from July 5, 2019, to January 22, 2020. By the data cutoff date on January 24, 2022, the median duration of follow-up was 23.3 months (95% confidence interval [CI]: 22.8-24.0). The ORR by blinded independent central review was 64.6% (95% CI: 58.0%-70.8%), and DCR was 89.8% (95% CI: 85.1%-93.4%). The median duration of response was 12.5 months (95% CI: 10.0-13.9), and median PFS was 12.2 months (95% CI: 9.6-13.9). The median overall survival was 23.9 months (95% CI: 20.0-not calculated [NC]). Among 91 (40.3%) patients with central nervous system (CNS) metastases, the median CNS PFS was 16.6 months (95% CI: 11.1-NC). In 29 patients with more than or equal to one brain target lesion at baseline, the CNS ORR and CNS DCR were 69.0% (95% CI: 49.2%-84.7%) and 100% (95% CI: 88.1%-100%), respectively. Time to progression of CNS was 16.5 months (95% CI: 9.7-NC). Of 226 patients, 188 (83.2%) had at least one treatment-related adverse event, whereas grade more than or equal to 3 occurred in 45 (19.9%) patients. No interstitial lung disease was reported.
Conclusions:
Rezivertinib was found to have promising efficacy and favorable safety profile for patients with locally advanced or metastatic/recurrent NSCLC with EGFR T790M mutation.
Insights
Rezivertinib shows promising efficacy in treating advanced non-small cell lung cancer (NSCLC) with EGFR T790M mutations. This third-generation EGFR tyrosine kinase inhibitor (TKI) demonstrated significant response rates and favorable safety in a recent clinical study.
Area of Science:
- Oncology
- Pharmacology
- Clinical Trials
Background:
- Non-small cell lung cancer (NSCLC) remains a leading cause of cancer-related deaths worldwide.
- Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitors (TKIs) have revolutionized NSCLC treatment, but resistance mutations, particularly T790M, limit long-term efficacy.
- Novel therapeutic strategies targeting resistance mutations are crucial for improving patient outcomes.
Purpose of the Study:
- To evaluate the efficacy and safety of rezivertinib, a third-generation EGFR TKI, in patients with locally advanced or metastatic/recurrent NSCLC harboring the EGFR T790M mutation.
- To assess rezivertinib's impact on objective response rate (ORR), disease control rate (DCR), progression-free survival (PFS), and overall survival (OS).
- To investigate the safety profile and tolerability of rezivertinib in this patient population.
Main Methods:
- A prospective clinical study enrolled 226 patients with confirmed EGFR T790M-mutated NSCLC who had progressed on prior EGFR TKI therapy.
- Patients received rezivertinib 180 mg orally once daily until disease progression or unacceptable toxicity.
- Efficacy endpoints, including ORR and DCR, were assessed by blinded independent central review; safety was monitored throughout the study.
Main Results:
- Rezivertinib demonstrated an objective response rate (ORR) of 64.6% and a disease control rate (DCR) of 89.8%.
- Median progression-free survival (PFS) was 12.2 months, and median overall survival (OS) was 23.9 months.
- Central nervous system (CNS) metastases showed a favorable response, with a median CNS PFS of 16.6 months and a CNS ORR of 69.0% in patients with target brain lesions.
Conclusions:
- Rezivertinib exhibits promising anti-tumor activity and a favorable safety profile in patients with EGFR T790M-mutated NSCLC.
- The drug demonstrates significant efficacy in both systemic disease and central nervous system metastases.
- Rezivertinib represents a valuable therapeutic option for patients who have progressed on earlier-generation EGFR TKIs.
