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ENTRECTINIB
Entrectinib is a marketed drug primarily indicated for ROS1-Positive Metastatic NSCLC. Its key strength lies in its targeted mechanism of action, providing a specific treatment option for this patient population. The primary risk is the key composition patent expiry in 2028, which could lead to increased competition from generics.
At a glance
| Generic name | ENTRECTINIB |
|---|---|
| Modality | Small molecule |
| Phase | FDA-approved |
| First approval | 2019 |
Approved indications
- ROS1-Positive Metastatic NSCLC
- NTRK Gene Fusion-Positive Solid Tumors
Common side effects
- Fatigue
- Constipation
- Dysgeusia
- Edema
- Dizziness
- Diarrhea
- Nausea
- Dysesthesia
- Dyspnea
- Myalgia
- Cognitive Impairment
- Increased Weight
Serious adverse events
- Pneumonia
- Dyspnea
- Pleural Effusion
- Sepsis
- Pulmonary Embolism
- Respiratory Failure
- Pyrexia
- Myocarditis
- Tumor Lysis Syndrome
- Large Intestine Perforation
Drug interactions
- Moderate and Strong CYP3A Inhibitors
- Moderate and Strong CYP3A Inducers
- Drugs That Prolong QTc Interval
Key clinical trials
- Study Of Entrectinib (Rxdx-101) in Children and Adolescents With Locally Advanced Or Metastatic Solid Or Primary CNS Tumors And/Or Who Have No Satisfactory Treatment Options (PHASE1, PHASE2)
- Entrectinib as a Single Agent in Upfront Therapy for Children <3 Years of Age With NTRK1/2/3 or ROS1-FUSED CNS Tumors (PHASE2)
- A Rollover Study for Participants Previously Enrolled in a Genentech and/or F. Hoffman-La Roche Sponsored Study (PHASE3)
- A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC) (PHASE2, PHASE3)
- Basket Study of Entrectinib (RXDX-101) for the Treatment of Patients With Solid Tumors Harboring NTRK 1/2/3 (Trk A/B/C), ROS1, or ALK Gene Rearrangements (Fusions) (PHASE2)
- Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study (PHASE2)
- A Study Evaluating the Efficacy and Safety of Multiple Therapies in Cohorts of Participants With Locally Advanced, Unresectable, Stage III Non-Small Cell Lung Cancer (NSCLC) (PHASE3)
- A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC) (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |