Entrectinib: A New Selective Tyrosine Kinase Inhibitor Approved for
the Treatment of Pediatric and Adult Patients with NTRK Fusionpositive,
Recurrent or Advanced Solid Tumors

Osman, Hind M.; Tunçbìlek, Meral

doi:10.2174/0929867328666210914121324

Cited by 4 publications

(2 citation statements)

References 81 publications

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“…The FDA has granted approval for the use of Entrectinib in the treatment of NTRK gene fusion-positive solid tumors in both adult and pediatric patients. The systemic antitumor activity of this compound has also been observed [ 132 ]. Without doubt, Entrectinib is associated with certain safety concerns, including congestive heart failure, central nervous system effects, fractures, lung infections, breathing problems, cognitive impairment, fainting, pulmonary embolism, and pleural effusions.…”

Section: The Development Of Inhibitors Targeted Kinase Fusion Proteinsmentioning

confidence: 99%

Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical

et al. 2023

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Oncogenic fusion proteins, arising from chromosomal rearrangements, have emerged as prominent drivers of tumorigenesis and crucial therapeutic targets in cancer research. In recent years, the potential of small molecular inhibitors in selectively targeting fusion proteins has exhibited significant prospects, offering a novel approach to combat malignancies harboring these aberrant molecular entities. This review provides a comprehensive overview of the current state of small molecular inhibitors as therapeutic agents for oncogenic fusion proteins. We discuss the rationale for targeting fusion proteins, elucidate the mechanism of action of inhibitors, assess the challenges associated with their utilization, and provide a summary of the clinical progress achieved thus far. The objective is to provide the medicinal community with current and pertinent information and to expedite the drug discovery programs in this area.

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Section: The Development Of Inhibitors Targeted Kinase Fusion Proteinsmentioning

confidence: 99%

Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical

et al. 2023

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“…This revealed an EIF4B::NTRK3 rearrangement in addition to high tumor mutational burden (31 mutation/Mb), TP53 variant, and FGFR1 copy number gain. Subsequently the patient was treated with entrectinib, a tyrosine kinase inhibitor selective for TRKA, B, C, ALK, and ROS1 which has been approved by the Food and Drug Administration to target both NTRK and ROS1 [67]. However, 10 months after treatment was initiated the patient experienced myasthenic crisis during which treatment was held.…”

Section: Ntrk Rearrangementsmentioning

confidence: 99%

The Role of Gene Fusions in Thymic Epithelial Tumors

Roden

2023

Cancers

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Thymic epithelial tumors (TET) are rare and large molecular studies are therefore difficult to perform. However, institutional case series and rare multi-institutional studies have identified a number of interesting molecular aberrations in TET, including gene fusions in a subset of these tumors. These gene fusions can aid in the diagnosis, shed light on the pathogenesis of a subset of tumors, and potentially may provide patients with the opportunity to undergo targeted therapy or participation in clinical trials. Gene fusions that have been identified in TET include MAML2 rearrangements in 50% to 56% of mucoepidermoid carcinomas (MAML2::CRTC1), 77% to 100% of metaplastic thymomas (YAP1::MAML2), and 6% of B2 and B3 thymomas (MAML2::KMT2A); NUTM1 rearrangements in NUT carcinomas (most commonly BRD4::NUTM1); EWSR1 rearrangement in hyalinizing clear cell carcinoma (EWSR1::ATF1); and NTRK rearrangement in a thymoma (EIF4B::NTRK3). This review focuses on TET in which these fusion genes have been identified, their morphologic, immunophenotypic, and clinical characteristics and potential clinical implications of the fusion genes. Larger, multi-institutional, global studies are needed to further elucidate the molecular characteristics of these rare but sometimes very aggressive tumors in order to optimize patient management, provide patients with the opportunity to undergo targeted therapy and participate in clinical trials, and to elucidate the pathogenesis of these tumors.

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Signaling pathways involved in colorectal cancer: pathogenesis and targeted therapy

Li,

Geng,

Luo

et al. 2024

Sig Transduct Target Ther

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Colorectal cancer (CRC) remains one of the leading causes of cancer-related mortality worldwide. Its complexity is influenced by various signal transduction networks that govern cellular proliferation, survival, differentiation, and apoptosis. The pathogenesis of CRC is a testament to the dysregulation of these signaling cascades, which culminates in the malignant transformation of colonic epithelium. This review aims to dissect the foundational signaling mechanisms implicated in CRC, to elucidate the generalized principles underpinning neoplastic evolution and progression. We discuss the molecular hallmarks of CRC, including the genomic, epigenomic and microbial features of CRC to highlight the role of signal transduction in the orchestration of the tumorigenic process. Concurrently, we review the advent of targeted and immune therapies in CRC, assessing their impact on the current clinical landscape. The development of these therapies has been informed by a deepening understanding of oncogenic signaling, leading to the identification of key nodes within these networks that can be exploited pharmacologically. Furthermore, we explore the potential of integrating AI to enhance the precision of therapeutic targeting and patient stratification, emphasizing their role in personalized medicine. In summary, our review captures the dynamic interplay between aberrant signaling in CRC pathogenesis and the concerted efforts to counteract these changes through targeted therapeutic strategies, ultimately aiming to pave the way for improved prognosis and personalized treatment modalities in colorectal cancer.

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Entrectinib: A New Selective Tyrosine Kinase Inhibitor Approved for the Treatment of Pediatric and Adult Patients with NTRK Fusionpositive, Recurrent or Advanced Solid Tumors

Cited by 4 publications

References 81 publications

Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical

Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical

The Role of Gene Fusions in Thymic Epithelial Tumors

Signaling pathways involved in colorectal cancer: pathogenesis and targeted therapy

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