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
Expanded Access to Entrectinib for Cancers With NTRK1/2/3, ROS1, or ALK Gene Fusions
- Conditions
- Cancers With NTRK, ROS1, or ALK Gene Fusions
- First Posted Date
- 2017-02-28
- Last Posted Date
- 2019-04-26
- Lead Sponsor
- Hoffmann-La Roche
- Registration Number
- NCT03066661
- Locations
- 🇺🇸
1-844-Startrk (782-7875), San Diego, California, United States
The Drug Rediscovery Protocol (DRUP Trial)
- Conditions
- CancerTumorsNeoplasmNeoplasia
- Interventions
- First Posted Date
- 2016-10-05
- Last Posted Date
- 2024-01-24
- Lead Sponsor
- The Netherlands Cancer Institute
- Target Recruit Count
- 1550
- Registration Number
- NCT02925234
- Locations
- 🇳🇱
Meander medisch centrum, Amersfoort, Netherlands
🇳🇱Netherlands Cancer Institute, Amsterdam, Netherlands
🇳🇱Amsterdam UMC, locatie AMC, Amsterdam, Netherlands
TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer
- Conditions
- Lymphoma, Non-HodgkinMultiple MyelomaAdvanced Solid Tumors
- Interventions
- First Posted Date
- 2016-02-26
- Last Posted Date
- 2025-05-06
- Lead Sponsor
- American Society of Clinical Oncology
- Target Recruit Count
- 4200
- Registration Number
- NCT02693535
- Locations
- 🇺🇸
University of Alabama at Birmingham Comprehensive Cancer Center, Birmingham, Alabama, United States
🇺🇸Cancer Treatment Centers of America-Phoenix, Phoenix, Arizona, United States
🇺🇸Sutter Auburn, Auburn, California, United States
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
- First Posted Date
- 2016-01-08
- Last Posted Date
- 2025-03-26
- Lead Sponsor
- Hoffmann-La Roche
- Target Recruit Count
- 69
- Registration Number
- NCT02650401
- Locations
- 🇺🇸
Texas Children's Cancer and Hematology Center, Houston, Texas, United States
🇺🇸UCSF Benioff Children's Hospital, San Francisco, California, United States
🇺🇸Children's Hospital Colorado, Aurora, Colorado, United States
Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma
- Conditions
- ALK Fusion Protein ExpressionNRAS wt AlleleNTRK1 Fusion PositiveNTRK2 Fusion PositiveNTRK3 Fusion PositiveRET Fusion PositiveROS1 Fusion PositiveStage IV Cutaneous MelanomaStage IIIA Cutaneous MelanomaStage IIIB Cutaneous Melanoma
- Interventions
- Other: Laboratory Biomarker Analysis
- First Posted Date
- 2015-10-27
- Last Posted Date
- 2020-01-27
- Lead Sponsor
- University of California, San Francisco
- Target Recruit Count
- 1
- Registration Number
- NCT02587650
- Locations
- 🇺🇸
University of California, San Francisco, San Francisco, California, United States
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)
- Conditions
- Pancreatic CancerAdult Solid TumorLymphoma, Large-Cell, AnaplasticPrimary Brain TumorsSarcomasBreast CancerNon-Small Cell Lung CancerOvarian CancerPapillary Thyroid CancerSalivary Gland Cancers
- Interventions
- First Posted Date
- 2015-10-05
- Last Posted Date
- 2025-03-17
- Lead Sponsor
- Hoffmann-La Roche
- Target Recruit Count
- 534
- Registration Number
- NCT02568267
- Locations
- 🇺🇸
Dignity Health St Joseph's Hospital and Medical Center, Phoenix, Arizona, United States
🇺🇸Mayo Clinic, Phoenix, Arizona, United States
🇺🇸City of Hope Cancer Center, Duarte, California, United States
Study of Oral RXDX-101 in Adult Patients With Locally Advanced or Metastatic Cancer Targeting NTRK1, NTRK2, NTRK3, ROS1, or ALK Molecular Alterations.
- Conditions
- Locally Advanced Solid TumorsMetastatic Solid Tumors
- Interventions
- First Posted Date
- 2014-03-27
- Last Posted Date
- 2021-06-09
- Lead Sponsor
- Hoffmann-La Roche
- Target Recruit Count
- 84
- Registration Number
- NCT02097810
- Locations
- 🇺🇸
Florida Cancer Specialists - Sarasota, Sarasota, Florida, United States
🇺🇸University of California, San Francisco, Helen Diller Family Comprehensive Cancer Center, San Francisco, California, United States
🇺🇸Tennessee Oncology, Nashville, Tennessee, United States
Drug Development Updates
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