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Entrectinib

Generic Name
Entrectinib
Brand Names
Rozlytrek
Drug Type
Small Molecule
Chemical Formula
C31H34F2N6O2
CAS Number
1108743-60-7
Unique Ingredient Identifier
L5ORF0AN1I
Background

Entrectinib is a tropomyosin receptor tyrosine kinase (TRK) TRKA, TRKB, TRKC, proto-oncogene tyrosine-protein kinase ROS1, and anaplastic lymphoma kinase (ALK) inhibitor. It was approved by the FDA in August 2019 for use in the treatment of ROS1-positive metastatic non-small cell lung cancer and NTRK gene fusion positive solid tumors. Entrectinib's approved use is meant as a last line of therapy due to its accelerated approval based on early trial data. This therapy offers benefit over similar ALK inhibitors such as alectinib, ceritinib, and lorlatinib due to a wider range of targets.

Indication

Entrectinib is indicated for the treatment of metastatic ROS1-positive non-small cell lung cancer in adults. Entrectinib is also indicated in adults and children over 12 years old for the treatment of NTRK gene fusion-positive solid tumors which have metastasized or for which surgical resection is likely to result in severe morbidity and for which has progressed on previous therapies or for which no comparable alternative therapies are available.

FoundationOne®Liquid CDx is the only FDA-approved test for the detection of ROS1 rearrangement(s) in NSCLC for selecting patients for treatment with entrectinib.

Associated Conditions
Metastatic Non-Small Cell Lung Cancer, Metastatic Solid Neoplasm, Solid Tumors

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

Not yet recruiting
Conditions
Non-Small Cell Lung Cancer
ROS1 Gene Rearrangement
Resistance
Targeted Therapy
Interventions
First Posted Date
2024-11-19
Last Posted Date
2024-11-19
Lead Sponsor
National Cancer Center, China
Target Recruit Count
40
Registration Number
NCT06694129

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

Phase 2
Recruiting
Conditions
High Grade Glioma
CNS Tumor
Interventions
First Posted Date
2024-07-30
Last Posted Date
2025-04-10
Lead Sponsor
St. Jude Children's Research Hospital
Target Recruit Count
52
Registration Number
NCT06528691
Locations
🇺🇸

St. Jude Children's Research Hospital, Memphis, Tennessee, United States

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

First Posted Date
2024-07-01
Last Posted Date
2024-12-05
Lead Sponsor
West China Hospital
Target Recruit Count
75
Registration Number
NCT06482086
Locations
🇨🇳

West China hospital, Chengdu, Sichuan, China

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

First Posted Date
2024-01-08
Last Posted Date
2024-04-30
Lead Sponsor
Fudan University
Target Recruit Count
200
Registration Number
NCT06195228
Locations
🇨🇳

Shanxi Cancer Hospital, Shanxi, Taiyuan, China

🇨🇳

Caixia Liu, Hohhot, Inner Mongolia, China

🇨🇳

Fudan University Shanghai Cancer Center, Shanghai, Shanghai, China

A Rollover Study for Participants Previously Enrolled in a Genentech and/or F. Hoffman-La Roche Sponsored Study

First Posted Date
2023-05-17
Last Posted Date
2025-05-13
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
60
Registration Number
NCT05862285
Locations
🇨🇷

Clinica CIMCA, San José, Costa Rica

🇧🇪

GHdC Site Les Viviers, Charleroi, Belgium

🇧🇪

AZ Groeninge, Kortrijk, Belgium

and more 24 locations

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

Phase 2
Recruiting
Conditions
Haematological Malignancy
Lymphoproliferative Disorders
Malignancy
Malignant Neoplasm
Neoplasms by Histologic Type
Neoplasms by Site
Cancer
Brain Neoplasms
Melanoma
Glioma
Interventions
First Posted Date
2023-03-15
Last Posted Date
2025-05-20
Lead Sponsor
Cancer Research UK
Target Recruit Count
30
Registration Number
NCT05770544
Locations
🇬🇧

Birmingham Children's Hospital, Birmingham, United Kingdom

🇬🇧

Cardiff Children's Hospital, Cardiff, United Kingdom

🇬🇧

Sheffield's Children's Hospital, Sheffield, United Kingdom

and more 24 locations

DETERMINE (Determining Extended Therapeutic Indications for Existing Drugs in Rare Molecularly Defined Indications Using a National Evaluation Platform Trial) - Master Screening Protocol

First Posted Date
2023-02-10
Last Posted Date
2024-03-20
Lead Sponsor
Cancer Research UK
Target Recruit Count
825
Registration Number
NCT05722886
Locations
🇬🇧

Belfast City Hospital, Belfast, United Kingdom

🇬🇧

Bristol Royal Hospital for Children, Bristol, United Kingdom

🇬🇧

The Beatson Hospital, Glasgow, United Kingdom

and more 22 locations

KPMNG Study of MOlecular Profiling Guided Therapy Based on Genomic Alterations in Advanced Solid Tumors II

First Posted Date
2022-09-02
Last Posted Date
2025-04-27
Lead Sponsor
Seoul National University Bundang Hospital
Target Recruit Count
1000
Registration Number
NCT05525858
Locations
🇰🇷

Soonchunhyang University Hospital Bucheon, Bucheon, Korea, Republic of

🇰🇷

Chungbuk National University Hospital, Chungju, Korea, Republic of

🇰🇷

Keimyung University Dongsan Hospital, Daegu, Korea, Republic of

and more 29 locations
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