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    DRUG:

    Rozlytrek (entrectinib)

    i
    Other names: RXDX-101, NMS-E628, RXDX101, RXDX 101, NMS E628, RG6268, RG 6268, NMSE628, RG-6268
    Company:
    Nerviano Medical Sciences, Roche
    Drug class:
    ALK inhibitor, TrkA receptor inhibitor, TrkB receptor inhibitor, TrkC kinase inhibitor, ROS1 inhibitor, JAK2 inhibitor, TNK2 inhibitor
    Related drugs:
    7d
    A systematic evaluation of the efficacy and safety of entrectinib in anaplastic thyroid carcinoma. (PubMed, Gene)
    Knockdown of NTRK1, which encodes TrkA, reduced cell viability and sensitized ATC cells to paclitaxel. Entrectinib was well tolerated at the administered dose, with no significant changes in body weight and serum biochemical markers. Collectively, these findings identify TrkA as a potential therapeutic target in ATC and support further investigation of entrectinib-based combination strategies to improve ATC treatment outcomes.
    Journal
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    NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1)
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    Rozlytrek (entrectinib) • paclitaxel
    9d
    Evaluation of the Effects of Nicardipine on Entrectinib Metabolism in vitro and in Rats. (PubMed, Eur J Drug Metab Pharmacokinet)
    These findings in rat models and in silico docking indicate that nicardipine increases entrectinib exposure. While these results underscore the risk of significant DDIs, further clinical studies in humans are required to confirm this interaction and determine if entrectinib dose adjustments are necessary to mitigate adverse events.
    Preclinical • Journal
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    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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    Rozlytrek (entrectinib)
    14d
    STARTRK-2: 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) (clinicaltrials.gov)
    P2, N=534, Active, not recruiting, Hoffmann-La Roche | Trial completion date: May 2026 --> Jun 2027 | Trial primary completion date: May 2026 --> Jun 2027
    Trial completion date • Trial primary completion date • Pan tumor
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1) • NTRK3 (Neurotrophic tyrosine kinase, receptor, type 3) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2)
    |
    ALK rearrangement • ROS1 rearrangement
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    Xalkori (crizotinib) • Rozlytrek (entrectinib)
    15d
    Differences Among Genomic Profiling Tests for Bone and Soft-Tissue Sarcomas in a Universal Health Insurance System. (PubMed, J Bone Joint Surg Am)
    In this cohort, the DNA+RNA-based panel showed a higher detection rate for TK fusions, although the panels were applied to different patient groups and the sensitivity and specificity could not be determined. Future studies evaluating different test types on the same tumor specimens are warranted to clarify whether the dual-sequencing approaches can improve the identification of actionable genetic events.
    Reimbursement • US reimbursement • Journal
    |
    BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1) • NTRK3 (Neurotrophic tyrosine kinase, receptor, type 3) • EML4 (EMAP Like 4) • FGFR1 (Fibroblast growth factor receptor 1) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2) • NTRK (Neurotrophic receptor tyrosine kinase) • RBPMS (RNA-binding protein with multiple splicing)
    |
    ALK fusion • NTRK fusion
    |
    FoundationOne® CDx • OncoGuide™ NCC Oncopanel System
    |
    Vitrakvi (larotrectinib) • Rozlytrek (entrectinib)
    15d
    Improving public cancer care by implementing precision medicine in Norway (2023-507894-16-00)
    P1/2, N=1000, Recruiting, Oslo University Hospital HF | N=6000 --> 1000
    Enrollment change
    |
    Avastin (bevacizumab) • Lynparza (olaparib) • Mekinist (trametinib) • Tecentriq (atezolizumab) • Zelboraf (vemurafenib) • Tafinlar (dabrafenib) • Rozlytrek (entrectinib) • imatinib • Alecensa (alectinib) • Cotellic (cobimetinib) • bortezomib • Piqray (alpelisib) • Zejula (niraparib) • Retevmo (selpercatinib) • Zykadia (ceritinib) • fulvestrant • Jemperli (dostarlimab-gxly) • Pemazyre (pemigatinib) • Tepmetko (tepotinib) • Tabrecta (capmatinib) • dexamethasone • Erivedge (vismodegib) • melphalan • dactinomycin • Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) • hydroxyurea
    20d
    Association of PD-L1 expression and clinical outcomes in ROS1-rearranged advanced non-small cell lung cancer treated with entrectinib. (PubMed, Transl Lung Cancer Res)
    No statistically significant difference was observed (P=0.65). This study did not find evidence that baseline PD-L1 expression significantly influences the efficacy of entrectinib in advanced ROS1-rearranged NSCLC patients.
    Clinical data • Journal • PD(L)-1 Biomarker • IO biomarker
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    PD-L1 (Programmed death ligand 1) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    PD-L1 expression • PD-L1 negative • ROS1 positive • ROS1 rearrangement
    |
    Rozlytrek (entrectinib)
    24d
    Secretory Breast Carcinoma in A Six-Year-Old Girl: Case Report With Genetic Insights and Therapeutic Implications. (PubMed, Balkan J Med Genet)
    TRK inhibitors (larotrectinib, entrectinib, repotrectinib) are FDA/EMA-approved for pediatric and adult solid tumors with NTRK fusions and have demonstrated high and durable response rates. The identification of ETV6-NTRK3 provides diagnostic specificity and offers a precision oncology option in the event of relapse. Long-term surveillance and multidisciplinary follow-up remain essential for optimal care.
    Journal • BRCA Biomarker
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • PGR (Progesterone receptor) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • PTEN (Phosphatase and tensin homolog) • NTRK3 (Neurotrophic tyrosine kinase, receptor, type 3) • PALB2 (Partner and localizer of BRCA2) • ETV6 (ETS Variant Transcription Factor 6) • CHEK2 (Checkpoint kinase 2) • MUC4 (Mucin 4, Cell Surface Associated) • NTRK (Neurotrophic receptor tyrosine kinase) • GATA3 (GATA binding protein 3)
    |
    HER-2 negative • NTRK fusion
    |
    Vitrakvi (larotrectinib) • Rozlytrek (entrectinib) • Augtyro (repotrectinib)
    1m
    A Study Evaluating the Efficacy and Safety of Multiple Therapies in Cohorts of Participants With Locally Advanced, Unresectable, Stage III Non-Small Cell Lung Cancer (NSCLC) (clinicaltrials.gov)
    P3, N=68, Active, not recruiting, Hoffmann-La Roche | Trial primary completion date: Dec 2026 --> Jun 2030
    Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    ALK positive • ALK fusion • ROS1 fusion • ROS1 positive
    |
    PD-L1 IHC 22C3 pharmDx • VENTANA PD-L1 (SP263) Assay
    |
    Imfinzi (durvalumab) • Rozlytrek (entrectinib) • Alecensa (alectinib)
    1m
    STRN::NTRK3-fused neoplasm with "monster cells" in the pelvis of a young adult female: expanding the clinicopathologic spectrum of NTRK-rearranged neoplasms. (PubMed, Virchows Arch)
    Entrectinib was administered, and an excellent response was observed. This case emphasizes the relevance of performing NGS in cases with unusual clinicopathological findings to identify potential treatment options. Importantly, the morphology deviated from the classic fibrosarcoma-like appearance described in most adult NTRK3-fused neoplasms and broadens the morphological spectrum in which these neoplasms should be considered.
    Journal
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    NTRK3 (Neurotrophic tyrosine kinase, receptor, type 3) • STRN (Striatin) • CD163 (CD163 Molecule) • CD34 (CD34 molecule) • CD68 (CD68 Molecule) • NTRK (Neurotrophic receptor tyrosine kinase) • F13A1 (Coagulation Factor XIII A Chain)
    |
    NTRK fusion
    |
    Rozlytrek (entrectinib)
    1m
    TRK inhibitors in pediatric gliomas. (PubMed, Neurooncol Adv)
    Targeted therapies with TRK inhibitors (TRKi), including larotrectinib and entrectinib, have shown promising efficacy with rapid and durable responses for patients with LGGs and HGGs. Overall, TRKi represent a significant advance for treating NTRK fusion-positive CNS tumors, especially in pediatric populations, offering new hope for patients with limited treatment options. Further studies are required to optimize their use and address unresolved challenges.
    Review • Journal
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    NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1) • NTRK3 (Neurotrophic tyrosine kinase, receptor, type 3) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    NTRK positive • NTRK fusion
    |
    Vitrakvi (larotrectinib) • Rozlytrek (entrectinib)
    1m
    Entrectinib in Combination With ASTX727 for the Treatment of Relapsed/Refractory TP53 Mutated Acute Myeloid Leukemia (clinicaltrials.gov)
    P1, N=13, Active, not recruiting, OHSU Knight Cancer Institute | Trial completion date: Jun 2026 --> Dec 2026
    Trial completion date
    |
    TP53 (Tumor protein P53)
    |
    TP53 mutation
    |
    Rozlytrek (entrectinib) • Inqovi (decitabine/cedazuridine)