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
A Study of Multiple Therapies in Biomarker-Selected Patients With Resectable Stages IB-III Non-Small Cell Lung Cancer
- Conditions
- Non-small Cell Lung Cancer
- Interventions
- Procedure: ResectionDrug: SBRTDrug: Chemotherapy
- First Posted Date
- 2020-03-10
- Last Posted Date
- 2025-05-18
- Lead Sponsor
- Genentech, Inc.
- Target Recruit Count
- 125
- Registration Number
- NCT04302025
- Locations
- 🇺🇸
University of California Los Angeles - Jonsson Comprehensive Cancer Center, Los Angeles, California, United States
🇺🇸Ellis Fischel Cancer Center, Columbia, Missouri, United States
🇺🇸UCSF Helen Diller Family CCC, San Francisco, California, United States
A Study to Investigate the Effect of Impaired Hepatic Function on the Pharmacokinetics of Entrectinib in Volunteers With Different Levels of Hepatic Function
- First Posted Date
- 2020-01-13
- Last Posted Date
- 2024-08-02
- Lead Sponsor
- Hoffmann-La Roche
- Target Recruit Count
- 38
- Registration Number
- NCT04226833
- Locations
- 🇨🇿
Pharmaceutical Research Associates CZ, s.r.o., Praha 7, Czechia
🇸🇰Summit Clinical Research s.r.o.; Oddelenie internej mediciny a klinickej farmakologie, Bratislava, Slovakia
🇭🇺CRU Hungary Kft, Miskolc, Hungary
Genetic Testing in Guiding Treatment for Patients With Brain Metastases
- Conditions
- Metastatic Malignant Neoplasm in the BrainMetastatic Malignant Solid NeoplasmPI3K Gene MutationKRAS G12C MutationNTRK Family Gene MutationCDK Gene MutationROS1 Gene Mutation
- Interventions
- First Posted Date
- 2019-06-21
- Last Posted Date
- 2025-04-02
- Lead Sponsor
- Alliance for Clinical Trials in Oncology
- Target Recruit Count
- 186
- Registration Number
- NCT03994796
- Locations
- 🇺🇸
Anchorage Radiation Therapy Center, Anchorage, Alaska, United States
🇺🇸Anchorage Associates in Radiation Medicine, Anchorage, Alaska, United States
🇺🇸Katmai Oncology Group, Anchorage, Alaska, United States
A Performance and Bioavailability Study of Entrectinib in Healthy Volunteers.
- Conditions
- Solid Tumor
- Interventions
- First Posted Date
- 2019-05-23
- Last Posted Date
- 2020-09-07
- Lead Sponsor
- Genentech, Inc.
- Target Recruit Count
- 31
- Registration Number
- NCT03961100
- Locations
- 🇬🇧
Quotient Clinical Ltd, Clinical Research Unit, Nottingham, United Kingdom
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial
- Conditions
- Accelerated Phase Chronic Myelogenous Leukemia, BCR-ABL1 PositiveAnatomic Stage IV Breast Cancer AJCC v8AnemiaAnn Arbor Stage III Hodgkin LymphomaAnn Arbor Stage III Non-Hodgkin LymphomaAnn Arbor Stage IV Hodgkin LymphomaAnn Arbor Stage IV Non-Hodgkin LymphomaAtypical Chronic Myeloid Leukemia, BCR-ABL1 NegativeBlast Phase Chronic Myelogenous Leukemia, BCR-ABL1 PositiveCastration-Resistant Prostate Carcinoma
- Interventions
- Biological: BevacizumabProcedure: Biospecimen CollectionBiological: DurvalumabBiological: IpilimumabBiological: NivolumabBiological: PembrolizumabBiological: PertuzumabOther: Quality-of-Life AssessmentBiological: Trastuzumab Emtansine
- First Posted Date
- 2019-03-18
- Last Posted Date
- 2024-03-04
- Lead Sponsor
- OHSU Knight Cancer Institute
- Target Recruit Count
- 2
- Registration Number
- NCT03878524
- Locations
- 🇺🇸
OHSU Knight Cancer Institute, Portland, Oregon, United States
A Study to Investigate the Bioequivalence of Two Different Forms of Entrectinib (Forms A and C) Under Fasted Conditions in Healthy Subjects
- Conditions
- Healthy Volunteers
- Interventions
- First Posted Date
- 2019-01-08
- Last Posted Date
- 2020-03-09
- Lead Sponsor
- Genentech, Inc.
- Target Recruit Count
- 28
- Registration Number
- NCT03796013
- Locations
- 🇺🇸
Covance Research Unit - Dallas, Dallas, Texas, United States
A Study to Investigate the Relative Bioavailability of Entrectinib Capsule Formulations F1 and F06 Under Fed Conditions in Healthy Participants
- Conditions
- Healthy Volunteers
- Interventions
- First Posted Date
- 2019-01-08
- Last Posted Date
- 2020-02-26
- Lead Sponsor
- Genentech, Inc.
- Target Recruit Count
- 14
- Registration Number
- NCT03796260
- Locations
- 🇺🇸
Covance Research Unit - Daytona, Daytona Beach, Florida, United States
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
- Conditions
- Cancer of Unknown Primary Site
- Interventions
- First Posted Date
- 2018-04-13
- Last Posted Date
- 2025-02-04
- Lead Sponsor
- Hoffmann-La Roche
- Target Recruit Count
- 528
- Registration Number
- NCT03498521
- Locations
- 🇫🇷
Centre Antoine Lacassagne, Nice, France
🇫🇷Institut Curie, Paris, France
🇫🇷CHU Lyon - Centre Hospitalier Lyon Sud, Pierre-Benite (Lyon), France
Evaluate the Effect of Entrectinib on the Pharmacokinetics of Midazolam in Cancer Patients
- Conditions
- Advanced Solid Tumor
- Interventions
- First Posted Date
- 2017-11-06
- Last Posted Date
- 2018-08-21
- Lead Sponsor
- Hoffmann-La Roche
- Target Recruit Count
- 15
- Registration Number
- NCT03330990
- Locations
- 🇺🇸
SCRI-Denver Drug Development Program, Denver, Colorado, United States
🇺🇸Florida Cancer Specialists - Sarasota (North Catttlemen Rd), Sarasota, Florida, United States
🇺🇸Tennessee Oncology, Nashville, Tennessee, United States
A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC)
- Conditions
- Non-Small Cell Lung Cancer
- Interventions
- First Posted Date
- 2017-06-07
- Last Posted Date
- 2025-05-13
- Lead Sponsor
- Hoffmann-La Roche
- Target Recruit Count
- 1000
- Registration Number
- NCT03178552
- Locations
- 🇵🇪
Instituto Nacional de Enfermedades Neoplasicas, Lima, Peru
🇵🇪Instituto Peruano de Oncología y Radioterapia, Lima, Peru
🇵🇪Clinica Ricardo Palma, San Isidro, Peru
Drug Development Updates
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