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Mobocertinib Is an Oral Kinase Inhibitor Targeted Against EFGR and Used in the Treatment of Non-small Cell Lung Cancer: A Review


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1 Shree Sureshdada Jain Institute of Pharmaceutical Education and Research, Jamner, Maharashtra, India
     

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Mobocertinib is a kinase inhibitor targeted against human epidermal growth factor receptor (EGFR). It is used particularly in the action of non-small cell lung cancer (NSCLC) caused by exon 20 placing mutations in the EGFR gene, which are classically linked through a poorer prognosis (as compared to "classical" EGFR mutants causing NSCLC) and are linked with opposition to standard targeted EGFR inhibitors. Mobocertinib appears to be an effective means of treating this otherwise treatment-resistant NSCLC, exerting an inhibitory effect on EGFR exon 20 insertion mutant variants at concentrations 1.5- to 10-fold lower than those required to inhibit wild-type EGFR.2 Mobocertinib, below the brand name Exkivity (Takeda Pharmaceuticals Inc.), was granted accelerated agreement by the FDA in September 2021 for the action of locally advanced or metastatic NSCLC in patients with EGFR exon 20 insertion mutations who have failed previous therapies.1


Keywords

Mobocertinib, non-small cell lung cancer, EGFR exon 20 insertion mutations
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  • www.drug bank.com
  • FDA Approved Drug Products: Exkivity (mobocertinib) capsules for oral use
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  • Mobocertinib Is an Oral Kinase Inhibitor Targeted Against EFGR and Used in the Treatment of Non-small Cell Lung Cancer: A Review

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Authors

Mayur S. Jain
Shree Sureshdada Jain Institute of Pharmaceutical Education and Research, Jamner, Maharashtra, India
Shashikant D. Barhate
Shree Sureshdada Jain Institute of Pharmaceutical Education and Research, Jamner, Maharashtra, India
Rahul D. Shimpi
Shree Sureshdada Jain Institute of Pharmaceutical Education and Research, Jamner, Maharashtra, India

Abstract


Mobocertinib is a kinase inhibitor targeted against human epidermal growth factor receptor (EGFR). It is used particularly in the action of non-small cell lung cancer (NSCLC) caused by exon 20 placing mutations in the EGFR gene, which are classically linked through a poorer prognosis (as compared to "classical" EGFR mutants causing NSCLC) and are linked with opposition to standard targeted EGFR inhibitors. Mobocertinib appears to be an effective means of treating this otherwise treatment-resistant NSCLC, exerting an inhibitory effect on EGFR exon 20 insertion mutant variants at concentrations 1.5- to 10-fold lower than those required to inhibit wild-type EGFR.2 Mobocertinib, below the brand name Exkivity (Takeda Pharmaceuticals Inc.), was granted accelerated agreement by the FDA in September 2021 for the action of locally advanced or metastatic NSCLC in patients with EGFR exon 20 insertion mutations who have failed previous therapies.1


Keywords


Mobocertinib, non-small cell lung cancer, EGFR exon 20 insertion mutations

References