Recent Insights into Osimertinib Analogues against EGFR Positive
Non-small Cell Lung Cancer

Jatin      Chhabra; Priyanka      Kashyap; Rakesh      Pahwa; Rakesh      Narang; Harish      Dureja; Sukhbir      Lal; Sangeeta      Verma
doi:10.2174/1568026623666230602143605
Abstract

Background: Lung cancer is a highly lethal malignancy with a poor prognosis and the leading cause of mortality worldwide. The development of mutations makes lung cancer treatment more challenging and expensive. Successful identification of epidermal growth factor receptor (EGFR) mutations led to the discovery of various third-generation tyrosine kinase inhibitors. Osimertinib is one of the promising and efficacious third-generation EGFR inhibitors and is mainly employed in the treatment of non-small cell lung cancer. Despite the initial effective response, osimertinib causes resistance in most of the patients after around 10 months of therapy, resulting in disease progression. To mitigate the effect of developed resistance, different osimertinib derivatives have been synthesized and evaluated by numerous research groups across the globe.
Methods: Present article illustrates recent research advancements for the utilization of osimertinib and its derivatives in non-small cell lung cancer (NSCLC). Last seven years literature search has been conducted from PubMed, ScienceDirect, and Google Scholar databases, etc.
Result: The present review emphasizes the recent advancements of osimertinib analogues that lead to enhanced antitumor potential and safety profile against non-small cell lung cancer. This manuscript also summarizes the different synthetic schemes involved in the synthesis of osimertinib analogues against EGFR reported by different research groups.
Conclusion: Anticancer mechanistic insights, analytical prospects, drug interactions, pharmacokinetic considerations, and resistance profile of osimertinib are highlighted in the current manuscript.
Keywords: Non-small cell lung cancer, EGFR, Osimertinib derivatives, Mutant EGFR, Fludeoxyglucose, Chemotherapy.
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biopsy in the first-Line treatment of EGFR inhibitor naïve advanced
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[134]
 To evaluate the efficacy and safety of high-dose almonertinib versus
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mutations in advanced NSCLC With brain metastases: a multicenter,
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[135]
 Safety and efficacy of osimertinib combined with anlotinib in EGFRm+,
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[136]
 A phase 1/2 study of osimertinib in combination with gefitinib in
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[137]
 A phase IIa clinical trial to evaluate the safety and efficacy of osimertinibin
first-line patients with EGFR Mutation-positive locally
advanced or metastatic non-small cell lung cancer and concomitant
EGFR T790M mutation at time of diagnosis. NCT02841579,
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[138]
 Phase 1 study of combination dacomitinib and osimertinibfor patients
with metastatic EGFR mutant lung cancers. NCT03810807,
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[139]
 A multicentre, open-label, single-arm, molecular profiling study of
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[140]
 Phase II trial of AZD9291 in first line treatment of lung cancer
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in patients with epidermal growth factor receptor mutation
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 An open-label, non-randomised, multicentre, comparative, Phase I
study to determine the pharmacokinetics, safety and tolerability of
AZD9291 following a single oral dose to patients with advanced
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AZD9291 in patients with advanced non-small cell lung cancer
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 An open-label Phase 1/2 study of itacitinib in combination with
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DOI https://dx.doi.org/10.2174/1568026623666230602143605	Print ISSN 1568-0266
Publisher Name Bentham Science Publisher	Online ISSN 1873-4294
Current Topics in Medicinal Chemistry

Recent Insights into Osimertinib Analogues against EGFR Positive Non-small Cell Lung Cancer

Abstract

Graphical Abstract

Adaptogens—History and Future Perspectives

AlphaFold in Medicinal Chemistry: Opportunities and Challenges

Artificial intelligence for Natural Products Discovery and Development

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Current Topics in Medicinal Chemistry

Recent Insights into Osimertinib Analogues against EGFR Positive Non-small Cell Lung Cancer

Abstract

Graphical Abstract

Call for Papers in Thematic Issues

Adaptogens—History and Future Perspectives

AlphaFold in Medicinal Chemistry: Opportunities and Challenges

Artificial intelligence for Natural Products Discovery and Development

Chronic Kidney Disease

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