NEP010, a novel compound with minor structural modification from afatinib, exhibited significantly improved antitumor activity

Review Oncology

Third-generation EGFR and ALK inhibitors: mechanisms of resistance and management

Alissa J. Cooper et al.

Summary: Patients with non-small-cell lung cancers (NSCLCs) harboring oncogenic EGFR or ALK alterations can benefit from therapies targeting these alterations, although acquired resistance to these agents is common. Third-generation inhibitors have extended the response durations of many patients with NSCLCs harboring these alterations, albeit with differing patterns of resistance to those associated with earlier-generation agents.

NATURE REVIEWS CLINICAL ONCOLOGY (2022)

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Article Oncology

Targeted therapy in lung cancer: Are we closing the gap in years of life lost?

David J. Benjamin et al.

Summary: Patients with driver mutations in non-small cell lung cancer (NSCLC) are typically diagnosed at a younger age. Although targeted therapies show good efficacy in some patients, there is still a significant gap in years of life lost (YLL) for these younger NSCLC patients compared to older patients without driver mutations.

CANCER MEDICINE (2022)

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Review Oncology

Resistance to TKIs in EGFR-Mutated Non-Small Cell Lung Cancer: From Mechanisms to New Therapeutic Strategies

Andreas Koulouris et al.

Summary: Resistance to TKIs of EGFR in advanced NSCLC poses a therapeutic challenge, with liquid biopsies and newer-generation TKIs offering potential solutions.

CANCERS (2022)

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Review Medicine, General & Internal

Review of epidermal growth factor receptor-tyrosine kinase inhibitors administration to non-small-cell lung cancer patients undergoing hemodialysis

Chou-Chin Lan et al.

Summary: In patients with NSCLC and chronic renal failure, oral EGFR-TKIs are effective treatment options to alleviate symptoms.

WORLD JOURNAL OF CLINICAL CASES (2022)

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Article Chemistry, Medicinal

Design, synthesis and biological evaluation of novel macrocyclic derivatives bearing aniline pyrimidine scaffolds as EGFR-TKIs

Yuhui Shen et al.

Summary: A series of novel macrocyclic derivatives with aniline pyrimidine scaffolds were designed and synthesized based on EGFR-TKI Osimertinib as a lead compound. The structures of these derivatives were identified, and their pharmacological activities were evaluated. Compound H1 with a 17-membered ring exhibited the best inhibitory activity against EGFRL858R/T790M and EGFRd746-750/T790M, while compound H7 with a 17-membered ring showed the most potent anti-proliferative activity against BaF3-EGFRdel19/T790M, comparable to Osimertinib.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)

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Review Chemistry, Medicinal

Discovery of mobocertinib, a new irreversible tyrosine kinase inhibitor indicated for the treatment of non-small-cell lung cancer harboring EGFR exon 20 insertion mutations

Jun Wang et al.

Summary: EGFR mutations can cause non-small cell lung cancer, and EGFR ex20ins mutations play a key role in oncogenesis. Mobocertinib, a novel small molecule therapeutic, has high anticancer potency against EGFR ex20ins-positive lung cancer and specificity to tumors that are resistant to other EGFR TKIs. The discovery of mobocertinib from osimertinib highlights the power of structure-based drug design and precision medicine approaches in the treatment of molecularly defined tumors.

MEDICINAL CHEMISTRY RESEARCH (2022)

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Article Oncology