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
Cite this article:
Mayur S. Jain, Shashikant D. Barhate, Rahul D. Shimpi. Mobocertinib is an Oral kinase inhibitor targeted against EGFR and used in the treatment of Non-small cell Lung cancer: A Review. Asian Journal of Pharmaceutical Research. 2022; 12(2):179-2. doi: 10.52711/2231-5691.2022.00029
Mayur S. Jain, Shashikant D. Barhate, Rahul D. Shimpi. Mobocertinib is an Oral kinase inhibitor targeted against EGFR and used in the treatment of Non-small cell Lung cancer: A Review. Asian Journal of Pharmaceutical Research. 2022; 12(2):179-2. doi: 10.52711/2231-5691.2022.00029 Available on: https://www.asianjpr.com/AbstractView.aspx?PID=2022-12-2-12
1. www.drug bank.com
2. FDA Approved Drug Products: Exkivity (mobocertinib) capsules for oral use
3. Bethune G, Bethune D, Ridgway N, Xu Z: Epidermal growth factor receptor (EGFR) in lung cancer: an overview and update. J Thorac Dis. 2010; 2(1): 48-51.
4. Vyse S, Huang PH: Targeting EGFR exon 20 insertion mutations in non-small cell lung cancer. Signal Transduct Target Ther. 2019; 4: 5. doi: 10.1038/s41392-019-0038-9. eCollection 2019
5. Zhang S, Jin S, Griffin C, Feng Z, Lin J, Baratta M, Brake R, Venkatakrishnan K, Gupta N: Single-Dose Pharmacokinetics and Tolerability of the Oral Epidermal Growth Factor Receptor Inhibitor Mobocertinib (TAK-788) in Healthy Volunteers: Low-Fat Meal Effect and Relative Bioavailability of 2 Capsule Products. Clin Pharmacol Drug Dev. 2021 Sep; 10(9): 1028-1043. doi: 10.1002/cpdd.951. Epub 2021 Jun 12.
6. FDA grants accelerated approval to mobocertinib for metastatic non-sma". U.S. Food and Drug Administration (FDA). 16 September 2021. Retrieved 16 September 2021. This article incorporates text from this source, which is in the public domain.
7. "What Is Non-Small Cell Lung Cancer?". www.cancer.org.
8. "Non-small cell lung cancer treatment – National Cancer Institute". 1 January 1980. Retrieved 19 October 2008.
9. Non-small cell lung cancer". University of Maryland Medical Center. Retrieved 4 December 2017.
10. Liu X, Conner H, Kobayashi T, Kim H, Wen F, Abe S, et al. (August 2005). "Cigarette smoke extract induces DNA damage but not apoptosis in human bronchial epithelial cells". American Journal of Respiratory Cell and Molecular Biology. 33 (2): 121–9.