Drug updated on 11/5/2024
| Dosage Form | Capsule (oral; 100 mg, 200 mg) |
| Drug Class | Kinase inhibitors |
| Ongoing and Completed Studies | ClinicalTrials.gov |
Indication
- Indicated for the treatment of adult patients with ROSI-positive metastatic non-small cell lung cancer (NSCLC) as detected by an FDI-approved test
- Indicated for the treatment of adult and pediatric patients older than 1 month of age with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion, as detected by an FDA-approved test without a known acquired resistance mutation
- Indicated for the treatment of adult and pediatric patients older than 1 month of age with solid tumors that are metastatic or where surgical resection is likely to result in severe morbidity
- Indicated for the treatment of adult and pediatric patients older than 1 month of age with solid tumors that have progressed following treatment or have no satisfactory alternative therapy.
Latest News
Summary
- This summary is based on the review of three systematic review(s)/meta-analysis(es). [1-3]
- Effectiveness in Tumors: Entrectinib has shown effectiveness in treating various cancer types with NTRK (neurotrophic receptor kinase) gene fusions, including soft tissue sarcomas, lung cancer, salivary gland cancer, and central nervous system tumors. In a virtual cohort of 43 patients with NTRK gene fusion-positive tumors, notable benefits were observed, particularly in central nervous system tumors.
- Comparative Outcomes: In indirect treatment comparisons for ROS1 fusion-positive non-small cell lung cancer (NSCLC), entrectinib demonstrated significantly better response rates (Odds Ratio [OR]: 2.43-2.74) and improved overall survival (Hazard Ratio [HR]: 0.47-0.61) compared to crizotinib and chemotherapy. Progression-free survival was similar between entrectinib and the comparators, with one scenario suggesting potential superiority for entrectinib.
- Pooled Analysis: The pooled analysis indicated an objective response rate of 57.4% (95% Confidence Interval [CI]: 43.2-70.8) for entrectinib, while larotrectinib showed a higher response rate of 75% (95% CI: 61-85), highlighting variations in efficacy among therapies for NTRK gene fusion-positive tumors.
- Entrectinib is reported to be well tolerated in patients with NTRK gene fusion-positive tumors, with safety outcomes noted as favorable in the studies reviewed. There were fewer adverse event-related discontinuations compared to crizotinib, with an odds ratio (OR) ranging from 0.79 to 0.90.
- No specific significant safety concerns or adverse effects were highlighted in the studies reviewed, indicating a generally acceptable safety profile for entrectinib in the evaluated populations.
Product Monograph / Prescribing Information
| Document Title | Year | Source |
|---|---|---|
| Rozlytrek (entrectinib) Prescribing Information. | 2024 | Genentech., South San Francisco, CA |
Systematic Reviews / Meta-Analyses
| Document Title | Year | Source |
|---|---|---|
| NTRK Gene Fusions in Solid Tumors and TRK Inhibitors: A Systematic Review of Case Reports and Case Series | 2022 | Journal of Personalized Medicine |
| Matching-adjusted indirect comparison: entrectinib versus crizotinib in ROS1 fusion-positive non-small cell lung cancer | 2020 | Journal of comparative effectiveness research |
| Systematic review of neurotrophic tropomyosin-related kinase inhibition as a tumor-agnostic management strategy | 2020 | Future Oncology |
Clinical Practice Guidelines
| Document Title | Year | Source |
|---|---|---|
| Oncogene-addicted metastatic non-small-cell lung cancer: ESMO Clinical Practice Guideline for diagnosis, treatment and follow-up. | 2023 | Annals of Oncology |
| Metastatic Pancreatic Cancer: ASCO Guideline Update. | 2020 | Journal of Clinical Oncology |
| JSCO-ESMO-ASCO-JSMO-TOS: international expert consensus recommendations for tumour-agnostic treatments in patients with solid tumours with microsatellite instability or NTRK fusions. | 2020 | Annals of Oncology |