Rozlytrek

(Entrectinib)

ApprovedSmall molecule

Rozlytrek is a small molecule that works as a ROS1/NTRK Inhibitor.[2] It is being used across 18 indications, with its most advanced program in Approved.[1]

Rozlytrek is one of 511 small molecule programs targeting Colorectal Cancer. It is currently in Approved.

Indications

Total Trials

Active Trials

510

Competitors

FDA Applications

NDA/BLA/ANDA regulatory filings

Patents

Pipeline

Status by Indication[3][1]

Indication

Colorectal CancerApproved

Non-Small Cell Lung CarcinomaActive, not recruiting

NeuroblastomaApproved

Hepatic FailureApproved

Central Nervous System CancerApproved

Solid TumorsActive, not recruiting

Haematological MalignancyRecruiting

Solid TumorActive, not recruiting

Carcinoma, Non-Small-Cell LungActive, not recruiting

Breast CancerActive, not recruiting

Colorectal CancerApproved

Approved

Non-Small Cell Lung CarcinomaApproved

Active, not recruiting

NeuroblastomaApproved

Approved

Hepatic FailureApproved

Approved

Central Nervous System CancerApproved

Approved

Solid TumorsPreclinical

Active, not recruiting

Haematological MalignancyPreclinical

Recruiting

Solid TumorPhase 2

Active, not recruiting

Carcinoma, Non-Small-Cell LungPhase 3

Active, not recruiting

Breast CancerPhase 2

Active, not recruiting

Showing 10 of 18 indications

Competition

Competitive Landscape

744 competitors in Breast Cancer

#DrugCompanyPhaseTrials

Rozlytrek

Roche

Approved

1 2

Voltaren

Novartis

Preclinical

1 3

MS Contin

HHikma Pharmaceuticals LLC

Preclinical

3 4

Tianeptine

Pfizer

Preclinical

1 5

Ablavar

LLantheus Medical Imaging

Preclinical

2 6

Diuretic

RReprieve Cardiovascular, Inc

Preclinical

1 7

Recombinant Human Endostatin

PPeking University Third Hospital

Preclinical

1 8

Bisphosphonate

Amgen

Preclinical

2 9

Perflutren Lipid Microsphere

IImaRx Therapeutics

Preclinical

1 10

Liposomal Irinotecan and Apatinib

SSecond Affiliated Hospital, School of Medicine, Zhejiang University

Preclinical

Ranked by pipeline maturity and clinical activity. Current drug highlighted in teal.

Timeline

Expected Milestones

Q4 2026

Phase 2Recruiting

Cancer

NCT05159245

Recruiting

Resistance

NCT07199959

Q1 2027

Recruiting

Solid Tumor

NCT05525858

Q2 2027

PreclinicalActive, not recruiting

Non-Small Cell Lung Cancer

NCT03178552

Phase 2Active, not recruiting

Breast Cancer

NCT02568267

Q4 2027

Not yet recruiting

Observational Study

NCT06694129

Clinical

Trials by Indication[1]

Non-Small Cell Lung Cancer4 trials

A Study to Learn About the Effectiveness of Cancer Medicines in Patients With Metastatic Non-small Cell Lung Cancer in Norway.

Completed· Pfizer logo

Pfizer··NCT05834348·5,279 enrolled

NAUTIKA1: A Multicenter, Phase II, Neoadjuvant and Adjuvant Study of Multiple Therapies in Biomarker-selected Patients With Resectable Stages IB-III Non-small Cell Lung Cancer

Recruiting· Roche logo

Roche·Phase 2·NCT04302025·99 enrolled

A Phase II/III Multicenter Study Evaluating the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Patients With Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC) Harboring Actionable Somatic Mutations Detected in Blood (B-FAST: Blood-First Assay Screening Trial)

Active, not recruiting· Roche logo

Roche·Preclinical·NCT03178552·1,000 enrolled

Show 1 more trial

A Phase I-III, Multicenter Study Evaluating the Efficacy and Safety of Multiple Therapies in Cohorts of Patients Selected According to Biomarker Status, With Locally Advanced, Unresectable, Stage III Non-Small Cell Lung Cancer

Active, not recruiting· Roche logo

Roche·Phase 3·NCT05170204·68 enrolled

Treatment3 trials

DETERMINE Trial Treatment Arm 03: Entrectinib in Adult, Paediatric and Teenage/Young Adult Patients With ROS1 Gene Fusion-Positive Cancers.

Recruiting·CCancer Research UK·Phase 2/3·NCT05770544·30 enrolled

Study of Precision Treatment for Rare Tumours in China Guided by PDO and NGS

Not yet recruiting·PPeking University Shenzhen Hospital·Phase 2·NCT06692491·200 enrolled

SMMART Adaptive Clinical Treatment (ACT) Trial

Withdrawn·OOHSU Knight Cancer Institute·Phase 1·NCT05238831

Trial2 trials

Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial

Terminated·OOHSU Knight Cancer Institute·Phase 1·NCT03878524·2 enrolled

The Drug Rediscovery Protocol (DRUP Trial)

Recruiting·TThe Netherlands Cancer Institute·Phase 2·NCT02925234·1,550 enrolled

Thyroid Cancer2 trials

Efficacy of Organoid-Based Drug Screening to Guide Treatment for Locally Advanced Thyroid Cancer

Recruiting·WWest China Hospital·Phase 2·NCT06482086·75 enrolled

A Retrospective and Prospective Real-world Study of Molecular Typing in the Treatment of Advanced Thyroid Cancer

Recruiting·FFudan University·Phase 4·NCT06195228·800 enrolled

Solid Tumor2 trials

Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Phase II Platform Trial

Active, not recruiting· Roche logo

Roche·Phase 2·NCT04589845·920 enrolled

KOrean Precision Medicine Networking Group Study of MOlecular Profiling Guided Therapy Based on Genomic Alterations in Advanced Solid Tumors II

Recruiting·SSeoul National University Bundang Hospital··NCT05525858·1,000 enrolled

23 more indications

Resistance1 trial

Study on the Mechanism of Acquired Resistance of Entrectinib

Recruiting·FFudan University··NCT07199959·38 enrolled

Cancers1 trial

Expanded Access to Entrectinib for Cancers With NTRK1/2/3, ROS1, or ALK Gene Fusions

No longer available· Roche logo

Roche··NCT03066661

Metastatic Cancer1 trial

Study of Oral RXDX-101 in Adult Patients With Locally Advanced or Metastatic Cancer Targeting NTRK1, NTRK2, NTRK3, ROS1, or ALK Molecular Alterations.

Completed· Roche logo

Roche·Phase 1·NCT02097810·84 enrolled

Endocrine Therapy1 trial

Neoadjuvant Study of Targeting ROS1 in Combination With Endocrine Therapy in Invasive Lobular Carcinoma of the Breast (ROSALINE)

Active, not recruiting·JJules Bordet Institute·Phase 2·NCT04551495·65 enrolled

Hepatic Function1 trial

A Study to Investigate the Effect of Impaired Hepatic Function on the Pharmacokinetics of Entrectinib in Volunteers With Different Levels of Hepatic Function

Completed· Roche logo

Roche·Phase 1·NCT04226833·38 enrolled

Advanced Solid Tumors1 trial

A Study Evaluating Targeted Therapies in Participants Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response

Completed· Roche logo

Roche·Phase 2·NCT04632992·252 enrolled

Observational Study1 trial

Real-world Observational Study of Targeted Therapy in Patients With Advanced ROS1-positive NSCLC

Not yet recruiting·NNational Cancer Center, China··NCT06694129·40 enrolled

Cancer of Unknown Primary Site1 trial

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

Completed· Roche logo

Roche·Phase 2·NCT03498521·529 enrolled

Uveal Melanoma1 trial

Study of PAC-1 and Entrectinib for Patients With Metastatic Uveal Melanoma

Terminated·—·Phase 1/2·NCT04589832·6 enrolled

Brain Metastases1 trial

Genetic Testing in Guiding Treatment for Patients With Brain Metastases

Suspended·AAlliance for Clinical Trials in Oncology·Phase 2·NCT03994796·186 enrolled

ART1 trial

A Study to Investigate the Relative Bioavailability of Entrectinib Capsule Formulations F1 and F06 Under Fed Conditions in Healthy Participants

Completed· Roche logo

Roche·Phase 1·NCT03796260·14 enrolled

Acute Myeloid Leukemia1 trial

Entrectinib in Combination With ASTX727 for the Treatment of Relapsed/Refractory TP53 Mutated Acute Myeloid Leukemia

Active, not recruiting·OOHSU Knight Cancer Institute·Phase 1·NCT05396859·13 enrolled

Immunotherapy1 trial

The Rome Trial From Histology to Target: the Road to Personalize Target Therapy and Immunotherapy

Unknown status·FFondazione per la Medicina Personalizzata·Phase 2·NCT04591431·400 enrolled

CNS Tumors1 trial

Entrectinib as a Single Agent in Upfront Therapy for Children <3 Years of Age With NTRK1/2/3 or ROS1-FUSED CNS Tumors

Recruiting·SSt. Jude Children's Research Hospital·Phase 2·NCT06528691·52 enrolled

TED1 trial

A Study to Investigate the Bioequivalence of Two Different Forms of Entrectinib (Forms A and C) Under Fasted Conditions in Healthy Subjects

Completed· Roche logo

Roche·Phase 1·NCT03796013·28 enrolled

Midazolam1 trial

Evaluate the Effect of Entrectinib on the Pharmacokinetics of Midazolam in Cancer Patients

Completed· Roche logo

Roche·Phase 1·NCT03330990·15 enrolled

Melanoma1 trial

Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma

Terminated·UUniversity of California, San Francisco·Phase 2·NCT02587650·1 enrolled

Cancer1 trial

The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs

Recruiting·HHelsinki University Central Hospital·Phase 2·NCT05159245·250 enrolled

Breast Cancer1 trial

An Open-Label, Multicenter, Global Phase 2 Basket Study of Entrectinib for the Treatment of Patients With Locally Advanced or Metastatic Solid Tumors That Harbor NTRK1/2/3, ROS1, or ALK Gene Rearrangements

Active, not recruiting· Roche logo

Roche·Phase 2·NCT02568267·534 enrolled

Carcinoma, Non-Small-Cell Lung1 trial

Randomized, Open Label, Multicenter, Phase III Study of Entrectinib Versus Crizotinib in Patients With Locally-Advanced or Metastatic Non-Small Cell Lung Cancer Harboring ROS1 Gene Rearrangements With and Without Central Nervous System Metastases

Active, not recruiting· Roche logo

Roche·Phase 3·NCT04603807·217 enrolled

Haematological Malignancy1 trial

DETERMINE (Determining Extended Therapeutic Indications for Existing Drugs in Rare Molecularly Defined Indications Using a National Evaluation Platform Trial): An Umbrella-Basket Platform Trial to Evaluate the Efficacy of Targeted Therapies in Rare Adult, Paediatric and Teenage/Young Adult (TYA) Cancers With Actionable Genomic Alterations, Including Common Cancers With Rare Actionable Alterations

Recruiting·CCancer Research UK·Preclinical·NCT05722886·825 enrolled

Solid Tumors1 trial

A Phase 1/2, Open-Label, Dose-Escalation And Expansion Study Of Entrectinib (Rxdx-101) In Pediatrics With Locally Advanced Or Metastatic Solid Or Primary CNS Tumors And/Or Who Have No Satisfactory Treatment Options

Active, not recruiting· Roche logo

Roche·Preclinical·NCT02650401·69 enrolled

Unspecified2 trials

A Performance and Bioavailability Study of Entrectinib in Healthy Volunteers.

Completed· Roche logo

Roche·Phase 1·NCT03961100·31 enrolled

An Open-Label, Multicenter Extension Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Study

Recruiting· Roche logo

Roche·Phase 3·NCT05862285·100 enrolled

Regulatory

FDA Approval Timeline[4]

Aug 15, 2019

ROZLYTREK

NDA NDA212725

Aug 15, 2019

ROZLYTREK

NDA NDA212725

Nov 5, 2021

ROZLYTREK

NDA NDA212725

Jul 18, 2022

ROZLYTREK

NDA NDA212725

Jun 16, 2023

ROZLYTREK

NDA NDA212725

Aug 31, 2023

ROZLYTREK

NDA NDA212725

Oct 20, 2023

ROZLYTREK

NDA NDA212725

Oct 20, 2023

ROZLYTREK

NDA NDA218550

Oct 20, 2023

ROZLYTREK

NDA NDA218550

Jan 26, 2024

ROZLYTREK

NDA NDA212725

Sources

References

[1]
ClinicalTrials.gov — 37 trial records for Entrectinib. U.S. National Library of Medicine, National Institutes of Health.
[2]
ChEMBL — Entrectinib compound record. European Bioinformatics Institute (EMBL-EBI).
[3]
Open Targets Platform — Drug–disease associations for Entrectinib. EMBL-EBI & Wellcome Sanger Institute.
[4]
OpenFDA — FDA approval records (NDA NDA212725). U.S. Food & Drug Administration.
[5]
FDA Orange Book — Patent and exclusivity data for Rozlytrek. U.S. Food & Drug Administration.
[6]
PubMed — 1 publication indexed for Entrectinib. U.S. National Library of Medicine.
[7]
SEC EDGAR — Roche company filings. U.S. Securities and Exchange Commission.

Details

Drug Info

Quick Facts

Mechanism of Action: ROS1/NTRK Inhibitor[2]
Modality: Small molecule[2]
Highest Phase: Approved[1]
Company: Roche

Patent Landscape[5]

Patent Cliff

Jul 8, 2028

Earliest patent expiration — generic entry possible after this date

Patent #Expires

9616059Jul 8, 2028

9085558Jul 8, 2028

9029356Jul 8, 2028

8673893Jul 8, 2028

9255087Jul 8, 2028

9 more patents

8299057Mar 10, 2032

9649306May 22, 2033

9085565May 22, 2033

10231965Feb 17, 2035

10561651Feb 19, 2035

11091469May 18, 2037

10738037May 18, 2037

11253515Jul 18, 2038

10398693Jul 18, 2038

Key Publications[6]

Entrectinib in ROS1+ NSCLC: Integrated Analysis of STARTRK

J Clin OncolFeb 10, 2023DOI: 10.1200/JCO.22.01692

Rozlytrek

Status by Indication[3][1]

Competitive Landscape

Expected Milestones

Q4 2026

Q1 2027

Q2 2027

Q4 2027

Trials by Indication[1]

Non-Small Cell Lung Cancer4 trials

Treatment3 trials

Trial2 trials

Thyroid Cancer2 trials

Solid Tumor2 trials

Resistance1 trial

Cancers1 trial

Metastatic Cancer1 trial

Endocrine Therapy1 trial

Hepatic Function1 trial

Advanced Solid Tumors1 trial

Observational Study1 trial

Cancer of Unknown Primary Site1 trial

Uveal Melanoma1 trial

Brain Metastases1 trial

ART1 trial

Acute Myeloid Leukemia1 trial

Immunotherapy1 trial

CNS Tumors1 trial

TED1 trial

Midazolam1 trial

Melanoma1 trial

Cancer1 trial

Breast Cancer1 trial

Carcinoma, Non-Small-Cell Lung1 trial

Haematological Malignancy1 trial

Solid Tumors1 trial

Unspecified2 trials

FDA Approval Timeline[4]

References

Drug Info

Quick Facts

Patent Landscape[5]

Key Publications[6]

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