Therapy Detail

Therapy Name Entrectinib
Therapy Description

Entrectinib (RXDX-101) 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).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Entrectinib RXDX-101 ALK Inhibitor 19 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 21 Entrectinib (RXDX-101) 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).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
ETV6-NTRK3 salivary gland cancer sensitive Entrectinib Phase I Actionable In a Phase I clinical trial, treatment with Entrectinib (RXDX-101) resulted in a durable partial response in a patient with mammary analogue secretory carcinoma harboring ETV6-NTRK3 (PMID: 26884591). 26884591
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 Entrectinib (RXDX-101), resulting in anti-proliferative activity in culture (PMID: 26939704). 26939704
ROS1 rearrange non-small cell lung carcinoma sensitive Entrectinib Phase I Actionable In a clinical study analyzing combined results of 2 Phase I trials, Entrectinib (RXDX-101) treatment resulted in complete response in 2 and partial response in 10 patients with ROS-1 rearranged non-small cell lung carcinoma that were treatment-naive (PMID: 28183697). 28183697
ALK F1245V neuroblastoma sensitive Entrectinib Phase I Actionable In a Phase I trial, Entrectinib (RXDX-101) treatment resulted in 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
ALK positive non-small cell lung carcinoma sensitive Entrectinib Phase I Actionable In a Phase I trial, Entrectinib (RXDX-101) 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...
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 Entrectinib (RXDX-101) compared to cells expressing wild-type EML4-ALK (PMID: 26939704). 26939704
ETV6-NTRK3 small intestine neuroendocrine neoplasm sensitive Entrectinib Clinical Study Actionable In a clinical study, Entrectinib (RXDX-101) treatment resulted in rapid response and tumor necrosis in a patient with small intestine neuroendocrine tumor who harbored a ETV6-NTRK3 fusion (PMID: 29118225). 29118225
ALK fusion colorectal cancer sensitive Entrectinib Phase I Actionable In a Phase I clinical trial, Entrectinib (RXDX-101) treatment resulted in partial response for more than 3 months in a colorectal cancer patient harboring a CAD-ALK gene fusion (PMID: 26633560). 26633560
ROS1 positive pancreatic cancer predicted - sensitive Entrectinib Phase I Actionable In a Phase I trial, Entrectinib (RXDX-101) treatment resulted in stable disease in a patient with ROS1-positive pancreatic cancer (J Clin Oncol 32:5s, 2014 (suppl; abstr 2502)). detail...
ETV6-NTRK1 Advanced Solid Tumor predicted - sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-NTRK1 were sensitive to Entrectinib (RXDX-101) as demonstrated by reduced proliferation relative to cells expressing an empty vector in culture (PMID: 26884591). 26884591
ETV6-NTRK3 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-NTRK3 were sensitive to Entrectinib (RXDX-101), 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 Entrectinib (RXDX-101) as demonstrated by reduced proliferation relative to cells expressing an empty vector in culture (PMID: 26884591). 26884591
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 Entrectinib (RXDX-101) in culture and in cell line xenograft models, resulting in inhibition of NPM1-ALK autophosphorylation and near complete tumor regression (PMID: 26939704). 26939704
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 Entrectinib (RXDX-101), resulting in anti-proliferative activity (PMID: 26939704). 26939704
EML4-ALK non-small cell lung carcinoma sensitive Entrectinib Preclinical - Cell line xenograft Actionable In a preclinical study, non-small cell lung carcinoma cells harboring EML4-ALK were sensitive to Entrectinib (RXDX-101), resulting in inhibition of cell proliferation and complete tumor regression in cell line xenograft models (PMID: 26939704). 26939704
ETV6-NTRK2 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-NTRK2 were sensitive to Entrectinib (RXDX-101), resulting in inhibition of cell proliferation in culture (PMID: 26939704). 26939704
ETV6-NTRK2 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ETV6-NTRK2 were sensitive to Entrectinib (RXDX-101) as demonstrated by reduced proliferation relative to cells expressing an empty vector in culture (PMID: 26884591). 26884591
ALK rearrange Advanced Solid Tumor sensitive Entrectinib Phase I Actionable In a clinical study analyzing combined results of 2 Phase I trials, Entrectinib (RXDX-101) 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 received prior Alk inhibitor treatments (PMID: 28183697). 28183697
ALK rearrange Advanced Solid Tumor sensitive Entrectinib Phase I Actionable In a Phase I trial, Entrectinib (RXDX-101) 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-ROS1 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell line xenograft Actionable In a preclinical study, transformed cells expressing ETV6-ROS1 were sensitive to Entrectinib (RXDX-101), resulting in inhibition of cell proliferation in culture and decreased tumor growth in xenograft models (PMID: 26939704). 26939704
ROS1 rearrange Advanced Solid Tumor sensitive Entrectinib Phase I Actionable In a clinical study analyzing combined results of 2 Phase I trials, Entrectinib (RXDX-101) treatment resulted 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 received prior Xalkori (crizotinib) (PMID: 28183697). 28183697
ROS1 rearrange Advanced Solid Tumor sensitive Entrectinib Phase I Actionable In a Phase I trial, Entrectinib (RXDX-101) 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...
ALK positive neuroblastoma sensitive Entrectinib Phase I Actionable In a Phase I trial, Entrectinib (RXDX-101) treatment resulted in partial response in a patient with ALK-positive neuroblastoma (J Clin Oncol 32:5s, 2014 (suppl; abstr 2502)). detail...
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 RXDX-101 (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 Entrectinib (RXDX-101) in culture (PMID: 26939704). 26939704
ETV6-NTRK3 fibrosarcoma predicted - sensitive Entrectinib Phase I Actionable In a Phase I trial, Entrectinib (RXDX-101) 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...
EML4-NTRK3 Advanced Solid Tumor sensitive Entrectinib Preclinical - Cell culture Actionable In a preclinical study, Entrectinib (RXDX-101) inhibited growth of transformed cells expressing EML4-NTRK3 in culture (PMID: 30279230). 30279230
Clinical Trial Phase Therapies Title Recruitment Status
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
NCT02650401 Phase I Entrectinib Study of RXDX-101 in Children With Recurrent or Refractory Solid Tumors and Primary CNS Tumors Recruiting
NCT03330990 Phase I Entrectinib Evaluate the Effect of Entrectinib on the Pharmacokinetics of Midazolam in Cancer Patients Completed
NCT02097810 Phase Ib/II Entrectinib A Phase 1/2a Study of Oral RXDX-101 in Adult Patients With Locally Advanced or Metastatic Cancer; Study Targeting ALK, ROS1, or TRKA/B/C Active, not recruiting
NCT02587650 Ceritinib Capmatinib Regorafenib Entrectinib Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma Recruiting
NCT03066661 Expanded access Entrectinib Expanded Access to Entrectinib for Cancers With NTRK1/2/3, ROS1, or ALK Gene Fusions Temporarily not available