ROZLYTREK (entrectinib)
ROZLYTREK is indicated for the treatment of ROS1-positive metastatic non-small cell lung cancer (NSCLC) in adults; NTRK gene fusion-positive solid tumors in adult and pediatric patients older than 1 month.
How ROZLYTREK Works
Entrectinib and its major active metabolite, M5, inhibit the tropomyosin receptor tyrosine kinases TRKA, TRKB, and TRKC, as well as ROS1 and ALK. In certain cancers, these kinases form fusion proteins that hyperactivate downstream signaling pathways, resulting in unconstrained cell proliferation. By blocking these specific kinase domains, the drug inhibits the growth of tumor cells harboring NTRK, ROS1, or ALK gene fusions. Furthermore, the drug demonstrates the ability to cross the blood-brain barrier, showing anti-tumor activity in the central nervous system.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2019-08-15
- Patent Cliff
- 2038
- Routes
- ORAL
- Dosage Forms
- PELLETS, CAPSULE
ROZLYTREK Approval History
What ROZLYTREK Treats
2 indicationsROZLYTREK is approved for 2 conditions since its original approval in 2019. These indications span multiple therapeutic areas including oncology, immunology, and more.
- ROS1-positive metastatic non-small cell lung cancer (NSCLC) in adults
- NTRK gene fusion-positive solid tumors in adult and pediatric patients older than 1 month
ROZLYTREK Target & Pathway
ProTarget
A JAK family member critical for blood cell production and involved in myeloproliferative disorders. JAK2 mutations drive polycythemia vera and myelofibrosis. Inhibiting JAK2 reduces abnormal blood cell production and spleen enlargement.
ROZLYTREK Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
Same target(s) AND same indication — head-to-head.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in ROZLYTREK's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications ROZLYTREK treats. First-in-class if their pivotal trials read out positive.
Clinical Trial Registry
25 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT06528691 | GLOBOTRK NCI-2024-02977 | Ph 2 | recruiting | Entrectinib as a Single Agent in Upfront Therapy for Children <3 Years of Age With NTRK1/2/3 or ROS1-FUSED CNS Tumors |
| NCT05862285 UmbrellaMAX | BX44273 2022-003414-36, 2023-504263-16-00 | Ph 3 | recruiting | A Rollover Study for Participants Previously Enrolled in a Genentech and/or F. Hoffman-La Roche Sponsored Study |
| NCT04589845 | BO41932 2020-001847-16, 2023-507418-28-00 | Ph 2 | active not recruiting | Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study |
| NCT05170204 HORIZON 1 | BO42777 2023-503920-14-00 | Ph 3 | active not recruiting | 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) |
| NCT05396859 | STUDY00023205 NCI-2022-02156, STUDY00023205 | Ph 1 | active not recruiting | Entrectinib in Combination With ASTX727 for the Treatment of Relapsed/Refractory TP53 Mutated Acute Myeloid Leukemia |
| NCT03994796 | A071701 NCI-2019-00744, U10CA180821 | Ph 2 | active not recruiting | Genetic Testing in Guiding Treatment for Patients With Brain Metastases |
| NCT04302025 | ML41591 | Ph 2 | recruiting | A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC) |
| NCT02650401 STARTRK-NG | RXDX-101-03 CO40778, 2023-505088-35-00 | Ph 1, Ph 2 | active not recruiting | 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 |
| NCT03178552 B-FAST | BO29554 2017-000076-28 | Ph 2, Ph 3 | active not recruiting | A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC) |
| NCT02568267 STARTRK-2 | RXDX-101-02 2015-003385-84, GO40782 | Ph 2 | active not recruiting | 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) |
| NCT04603807 | MO41552 2019-003859-11, 2023-507494-18-00 | Ph 3 | active not recruiting | A Study to Compare the Efficacy and Safety of Entrectinib and Crizotinib in Participants With Advanced or Metastatic ROS1 Non-small Cell Lung Cancer (NSCLC) With and Without Central Nervous System (CNS) Metastases |
| NCT05722886 DETERMINE | CRUKD/21/004 IRAS ID: 1004057 | Ph 2, Ph 3 | recruiting | DETERMINE (Determining Extended Therapeutic Indications for Existing Drugs in Rare Molecularly Defined Indications Using a National Evaluation Platform Trial) - Master Screening Protocol |
| NCT05770544 DETERMINE | CRUKD/21/004 - Treatment Arm 3 IRAS ID: 1004057 | Ph 2, Ph 3 | recruiting | DETERMINE Trial Treatment Arm 03: Entrectinib in Adult, Paediatric and Teenage/Young Adult Patients With ROS1 Gene Fusion-Positive Cancers. |
| NCT03498521 CUPISCO results posted | MX39795 2017-003040-20 | Ph 2 | completed | A Phase II Randomized Study Comparing the Efficacy and Safety of Targeted Therapy or Cancer Immunotherapy Versus Platinum-Based Chemotherapy in Patients With Cancer of Unknown Primary Site |
| NCT04632992 MyTACTIC results posted | ML42439 | Ph 2 | completed | A Study Evaluating Targeted Therapies in Participants Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response |
| NCT06482086 | 202314711 | Ph 2 | recruiting | Efficacy of Organoid-Based Drug Screening to Guide Treatment for Locally Advanced Thyroid Cancer |
| NCT06692491 SPRING | PUShenzhenH RE [2024]No.(117) | Ph 2 | not yet recruiting | Study of Precision Treatment for Rare Tumours in China Guided by PDO and NGS |
| NCT04226833 results posted | GP41174 2019-003065-17 | Ph 1 | completed | A Study to Investigate the Effect of Impaired Hepatic Function on the Pharmacokinetics of Entrectinib in Volunteers With Different Levels of Hepatic Function |
| NCT05159245 FINPROVE | FINPROVE | Ph 2 | recruiting | The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs |
| NCT03878524 | STUDY00015588 NCI-2020-02743, STUDY00015588 | Ph 1 | terminated | Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial |
| NCT02925234 DRUP | M15DRU | Ph 2 | recruiting | The Drug Rediscovery Protocol (DRUP Trial) |
| NCT04589832 results posted | MEL18-372 | Ph 1, Ph 2 | terminated | Study of PAC-1 and Entrectinib for Patients With Metastatic Uveal Melanoma |
| NCT02097810 STARTRK-1 | RXDX-101-01 GO40784 | Ph 1 | completed | Study of Oral RXDX-101 in Adult Patients With Locally Advanced or Metastatic Cancer Targeting NTRK1, NTRK2, NTRK3, ROS1, or ALK Molecular Alterations. |
| NCT02587650 results posted | 14859 NCI-2017-01421 | Ph 2 | terminated | Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma |
| NCT03330990 | RXDX-101-14 GO40785 | Ph 1 | completed | Evaluate the Effect of Entrectinib on the Pharmacokinetics of Midazolam in Cancer Patients |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
ROZLYTREK FDA Label Details
Indications & Usage
FDA Label (PDF)ROZLYTREK is indicated for the treatment of ROS1-positive metastatic non-small cell lung cancer (NSCLC) in adults; NTRK gene fusion-positive solid tumors in adult and pediatric patients older than 1 month.
ROZLYTREK Patents & Exclusivity
Patents (14 active)
Exclusivity
Pro Intelligence Preview
Deep insights for ROZLYTREK
Revenue Insights
- • Quarterly revenue tracking
- • Historical trend analysis
Patent Timeline
- • Cliff: 2038
- • 76 active patents
Trial Analysis
- • 27 total trials
- • Stage: Growth
Competitive Landscape
- • Competitor tracking
- • Same target/indication analysis
Full approval history • All patents • Revenue trends • Competitor analysis
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment