The Challenge and Opportunity of NTRK Inhibitors in Non-Small Cell Lung Cancer

Qin, Haixia; Patel, Manish R.

doi:10.3390/ijms23062916

Cited by 17 publications

(9 citation statements)

References 44 publications

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“…Circumvention of these issues followed suit by using strategies such as irreversible inhibition to overcome drug resistance and the introduction of chirality to improve selectivity and efficacy profiles. [84][85][86][87] Clinical limitations to these methods were quickly realized [88][89][90] and the development of small-molecule kinase macrocycles has emerged as an innovative approach to supplement drug development efforts in the kinome (Table 9).…”

Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules

Acharya,

Saha,

Armstrong

et al. 2024

RSC Med. Chem.

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Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules

Acharya,

Saha,

Armstrong

et al. 2024

RSC Med. Chem.

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“…The key distinction between them is their ability to penetrate the CNS, with entrectinib being more effective at crossing the blood‒brain barrier 150 . This has been demonstrated in its successful treatment of patients with brain metastases.…”

Section: Neurotrophic Tyrosine Kinase (Ntrk)mentioning

confidence: 99%

Novel therapeutic strategies for rare mutations in non-small cell lung cancer

Gou,

Gan

et al. 2024

Sci Rep

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Lung cancer is still the leading cause of cancer-related mortality. Over the past two decades, the management of non-small cell lung cancer (NSCLC) has undergone a significant revolution. Since the first identification of activating mutations in the epidermal growth factor receptor (EGFR) gene in 2004, several genetic aberrations, such as anaplastic lymphoma kinase rearrangements (ALK), neurotrophic tropomyosin receptor kinase (NTRK) and hepatocyte growth factor receptor (MET), have been found. With the development of gene sequencing technology, the development of targeted drugs for rare mutations, such as multikinase inhibitors, has provided new strategies for treating lung cancer patients with rare mutations. Patients who harbor this type of oncologic driver might acquire a greater survival benefit from the use of targeted therapy than from the use of chemotherapy and immunotherapy. To date, more new agents and regimens can achieve satisfactory results in patients with NSCLC. In this review, we focus on recent advances and highlight the new approval of molecular targeted therapy for NSCLC patients with rare oncologic drivers.

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“…Ongoing studies seek to evaluate the efficacy and safety of the second-generation agents selitrectinib and repotrectinib, TRK inhibitors that may be able to overcome on-target treatment resistance caused by mutation of the TRK kinase domain itself [ 55 , 56 , 57 ].…”

Section: Tumor-agnostic Treatmentsmentioning

confidence: 99%

Precision Oncology Targets in Biliary Tract Cancer

Farha

Dima

Ullah

et al. 2023

Cancers

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Targeted therapies in biliary tract cancer (BTC) are emerging as options for patients not who do not respond to first-line treatment. Agents acting on tumor-specific oncogenes in BTC may target fibroblast growth factor receptor 2 (FGFR2), isocitrate dehydrogenase (IDH), B-raf kinase (BRAF), and human epidermal growth factor receptor 2 (HER-2). Additionally, given the heterogeneous genetic landscape of advanced BTCs, many harbor genetic aberrations that are common among solid tumors, including RET fusions, tropomyosin receptor kinase (TRK) fusions, and high tumor mutational burden (TMB). This review aims to provide updates on the evolving array of therapeutics available, and to summarize promising works on the horizon.

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The Challenge and Opportunity of NTRK Inhibitors in Non-Small Cell Lung Cancer

Cited by 17 publications

References 44 publications

Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules

Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules

Novel therapeutic strategies for rare mutations in non-small cell lung cancer

Precision Oncology Targets in Biliary Tract Cancer

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