Therapy Detail

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Therapy Name Entrectinib
Synonyms
Therapy Description

Rozlytrek (entrectinib) inhibits the activity of TrkA/B/C, Ros1 fusion proteins, and Alk, which leads to induction of apoptosis and inhibition of proliferation in cells expressing these kinases (PMID: 27003761). Rozlytrek (entrectinib) is FDA approved for use in patients with ROS1 positive non-small cell lung cancer and in adult and pediatric (12 years and older) patients with solid tumors harboring NRTRK fusions without known acquired resistance mutations (FDA.gov).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Entrectinib Rozlytrek RXDX-101 ALK Inhibitor 22 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 Rozlytrek (entrectinib) inhibits the activity of TrkA/B/C, Ros1 fusion proteins, and Alk, which leads to induction of apoptosis and inhibition of proliferation in cells expressing these kinases (PMID: 27003761). Rozlytrek (entrectinib) is FDA approved for use in patients with ROS1 positive non-small cell lung cancer and in adult and pediatric (12 years and older) patients with solid tumors harboring NRTRK fusions without known acquired resistance mutations (FDA.gov).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
NPM1 - ALK anaplastic large cell lymphoma sensitive Entrectinib Preclinical - Cell line xenograft Actionable In a preclinical study, anaplastic large cell lymphoma cells harboring NPM1-ALK were sensitive to Rozlytrek (entrectinib) in culture and in cell line xenograft models, resulting in inhibition of NPM1-ALK autophosphorylation and near complete tumor regression (PMID: 26939704). 26939704
ETV6 - NTRK1 Advanced Solid Tumor predicted - sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-NTRK1 were sensitive to Rozlytrek (entrectinib) as demonstrated by reduced proliferation relative to cells expressing an empty vector in culture (PMID: 26884591). 26884591
EML4 - ALK ALK C1156Y Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing EML4-ALK with ALK C1156Y were sensitive to Rozlytrek (entrectinib), resulting in anti-proliferative activity (PMID: 26939704). 26939704
ETV6 - ROS1 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell line xenograft Actionable In a preclinical study, transformed cells expressing ETV6-ROS1 were sensitive to Rozlytrek (entrectinib), resulting in inhibition of cell proliferation in culture and decreased tumor growth in xenograft models (PMID: 26939704). 26939704
ETV6 - ALK Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-ALK demonstrated sensitivity to Rozlytrek (entrectinib) in culture (PMID: 26939704). 26939704
EML4 - ALK ALK G1202R Advanced Solid Tumor resistant Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R were resistant to Rozlytrek (entrectinib) in culture (PMID: 26939704). 26939704
ROS1 rearrange Advanced Solid Tumor sensitive Entrectinib Phase I Actionable In a clinical study, combined analysis of 2 Phase I trials showed Rozlytrek (entrectinib) treatment to result in an objective response rate of 86% (12/14) in patients with ROS-1 rearranged advanced solid tumors that were treatment-naive, but no response (0/6) in patients who received prior Xalkori (crizotinib) (PMID: 28183697). 28183697
ROS1 rearrange Advanced Solid Tumor sensitive Entrectinib Phase I Actionable In a Phase I trial, Rozlytrek (entrectinib) treatment resulted in complete response in 13% (1/12) and objection response in 75% (6/8) of patients with advanced solid tumors harboring rearrangement in ROS1 gene (AACR Apr 2016, Abstract # CT007). detail...
ETV6 - NTRK3 small intestine neuroendocrine neoplasm predicted - sensitive Entrectinib Case Reports/Case Series Actionable In a clinical study, Rozlytrek (entrectinib) treatment resulted in rapid response and tumor necrosis in a patient with a small intestine neuroendocrine tumor harboring a ETV6-NTRK3 fusion (PMID: 29118225; NCT02568267). 29118225
EML4 - ALK ALK L1196M Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing EML4-ALK with ALK L1196M were sensitive to Rozlytrek (entrectinib), resulting in anti-proliferative activity in culture (PMID: 26939704). 26939704
EML4 - ALK lung non-small cell carcinoma sensitive Entrectinib Preclinical - Cell line xenograft Actionable In a preclinical study, non-small cell lung carcinoma cells harboring EML4-ALK were sensitive to Rozlytrek (entrectinib), resulting in inhibition of cell proliferation and complete tumor regression in cell line xenograft models (PMID: 26939704). 26939704
EML4 - NTRK3 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, Rozlytrek (entrectinib) inhibited growth of transformed cells expressing EML4-NTRK3 in culture (PMID: 30279230). 30279230
EML4 - ALK ALK G1269A Advanced Solid Tumor decreased response Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing EML4-ALK with ALK G1269A demonstrated a decreased response when treated with Rozlytrek (entrectinib) compared to cells expressing wild-type EML4-ALK (PMID: 26939704). 26939704
ALK positive neuroblastoma sensitive Entrectinib Case Reports/Case Series Actionable In a Phase I trial, Rozlytrek (entrectinib) treatment resulted in partial response in a patient with ALK-positive neuroblastoma (J Clin Oncol 32:5s, 2014 (suppl; abstr 2502)). detail...
ALK rearrange Advanced Solid Tumor sensitive Entrectinib Phase I Actionable In a clinical study, combined analysis of 2 Phase I trials showed Rozlytrek (entrectinib) treatment resulted in an objective response rate of 57% (4/7) in patients with ALK rearranged advanced solid tumors that were treatment-naive, but no response (0/19) in patients who received prior Alk inhibitor treatments (PMID: 28183697). 28183697
ALK rearrange Advanced Solid Tumor sensitive Entrectinib Phase I Actionable In a Phase I trial, Rozlytrek (entrectinib) treatment resulted in objective response in 67% (4/6) of patients with advanced solid tumors harboring rearrangement in ALK gene (AACR Apr 2016, Abstract # CT007). detail...
ETV6 - NTRK3 salivary gland cancer predicted - sensitive Entrectinib Case Reports/Case Series Actionable In a clinical case study, treatment with Rozlytrek (entrectinib) obtained through a Phase I trial resulted in a durable partial response in a patient with mammary analogue secretory carcinoma of the salivary gland harboring ETV6-NTRK3 (PMID: 26884591; NCT02097810). 26884591
ALK F1245V neuroblastoma predicted - sensitive Entrectinib Case Reports/Case Series Actionable In a clinical study, combined analysis of 2 Phase I trials showed Rozlytrek (entrectinib) treatment to result in a partial response that lasted 8.3 months in a patient with neuroblastoma harboring ALK F1245V, who remained on treatment for over 3.5 years due to clinical benefit (PMID: 28183697). 28183697
ROS1 positive lung non-small cell carcinoma sensitive Entrectinib FDA approved Actionable In a combined analysis of 3 clinical trials (ALKA-372-001, STARTRK-1, STARTRK-2) that supported FDA approval, Rozlytrek (entrectinib) treatment resulted in an objective response rate of 77% (41/53), a median duration of response of 25 months in patients with ROS1 fusion positive non-small cell lung cancer, with median progression-free survival of 26 and 14 months for patients without (n=30) and with (n=23) CNS disease, respectively (Cancer Res 2019;79(13 Suppl):Abstract nr CT192; NCT02097810; NCT02568267). detail... detail...
ETV6 - NTRK2 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-NTRK2 were sensitive to Rozlytrek (entrectinib) as demonstrated by reduced proliferation relative to cells expressing an empty vector in culture (PMID: 26884591). 26884591
ETV6 - NTRK2 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-NTRK2 were sensitive to Rozlytrek (entrectinib), resulting in inhibition of cell proliferation in culture (PMID: 26939704). 26939704
ROS1 fusion lung non-small cell carcinoma sensitive Entrectinib FDA approved Actionable In a combined analysis of 3 clinical trials (ALKA-372-001, STARTRK-1, STARTRK-2) that supported FDA approval, Rozlytrek (entrectinib) treatment resulted in an objective response rate of 77% (41/53), a median duration of response of 25 months in patients with ROS1 fusion positive non-small cell lung cancer, with median progression-free survival of 26 and 14 months for patients without (n=30) and with (n=23) CNS disease, respectively (PMID: 31838015; NCT02097810; NCT02568267). detail... 31838015
ROS1 positive pancreatic cancer predicted - sensitive Entrectinib Case Reports/Case Series Actionable In a Phase I trial, Rozlytrek (entrectinib) treatment resulted in stable disease in a patient with ROS1-positive pancreatic cancer (J Clin Oncol 32:5s, 2014 (suppl; abstr 2502)). detail...
ETV6 - NTRK3 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-NTRK3 were sensitive to Rozlytrek (entrectinib), resulting in inhibition of cell proliferation in culture (PMID: 26939704). 26939704
ETV6 - NTRK3 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-NTRK3 were sensitive to Rozlytrek (entrectinib) as demonstrated by reduced proliferation relative to cells expressing an empty vector in culture (PMID: 26884591). 26884591
ROS1 rearrange lung non-small cell carcinoma sensitive Entrectinib Guideline Actionable Rozlytrek (entrectinib) is included in guidelines as a preferred therapy for patients with advanced or metastatic ROS1 rearrangement-positive non-small cell lung cancer (NCCN.org). detail...
ROS1 rearrange lung non-small cell carcinoma sensitive Entrectinib Phase I Actionable In a clinical study, combined analysis of 2 Phase I trials showed Rozlytrek (entrectinib) treatment to result in complete response in 15% (2/13) and partial response in 77% (10/13) patients with ROS-1 rearranged non-small cell lung carcinoma that were treatment-naive (PMID: 28183697). 28183697
EML4 - ALK ALK C1156Y ALK G1269A Advanced Solid Tumor resistant Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ALK C1156Y and G1269A compound mutation in the context of EML4-ALK were resistant to Rozlytrek (entrectinib) in culture (PMID: 31585938). 31585938
ALK positive lung non-small cell carcinoma sensitive Entrectinib Case Reports/Case Series Actionable In a Phase I trial, Rozlytrek (entrectinib) treatment resulted in stable disease in a patient with ALK-positive non-small cell lung carcinoma (J Clin Oncol 32:5s, 2014 (suppl; abstr 2502)). detail...
ETV6 - NTRK3 fibrosarcoma predicted - sensitive Entrectinib Phase I Actionable In a Phase I trial, Rozlytrek (entrectinib) treatment resulted in an objective response in a pediatric patient with infantile fibrosarcoma harboring ETV6-NTRK3 fusion (J Clin Oncol 36, 2018 (suppl; abstr 10536); NCT02650401). detail...

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Clinical Trial Phase Therapies Title Recruitment Status
NCT02650401 Phase I Entrectinib Study Of Entrectinib (Rxdx-101) in Children and Adolescents With No Curative First-Line Treatment Option, Recurrent or Refractory Solid Tumors And Primary Cns Tumors, With or Without Trk, Ros1, or Alk Fusions Recruiting
NCT02097810 Phase I Entrectinib Study of Oral RXDX-101 in Adult Patients With Locally Advanced or Metastatic Cancer Targeting NTRK1, NTRK2, NTRK3, ROS1, or ALK Molecular Alterations. (STARTRK-1) Active, not recruiting
NCT03066661 Expanded access Entrectinib Expanded Access to Entrectinib for Cancers With NTRK1/2/3, ROS1, or ALK Gene Fusions No longer available
NCT03330990 Phase I Entrectinib Evaluate the Effect of Entrectinib on the Pharmacokinetics of Midazolam in Cancer Patients Completed
NCT02568267 Phase II Entrectinib Basket Study of Entrectinib (RXDX-101) for the Treatment of Patients With Solid Tumors Harboring NTRK1/2/3, ROS1, or ALK Gene Rearrangements (STARTRK-2) Recruiting
NCT02587650 Phase II Ceritinib Capmatinib Regorafenib Entrectinib Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma Terminated
NCT03994796 Phase II Abemaciclib GDC-0084 Entrectinib Genetic Testing in Guiding Treatment for Patients With Brain Metastases Recruiting
NCT03178552 Phase II Entrectinib Carboplatin + Cisplatin + Gemcitabine Atezolizumab Carboplatin + Cisplatin + Pemetrexed Alectinib A Study to Evaluate Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC) (B-FAST) Recruiting


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