Spotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations

Shannon S Zhang,1 Viola W Zhu1,2 1University of California, Irvine School of Medicine, Department of Medicine, Orange, CA, USA; 2Chao Family Comprehensive Cancer Center, Orange, CA, USACorrespondence: Viola W ZhuUniversity of California, Irvine School of Medicine, Department of Medicine, 200 S Manch...

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Autores principales:	Zhang SS, Zhu VW
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	mobocertinib tak-788 nsclc egfr exon 20 insertion tki amivantamab Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/5baf978ecbe94f9e9c65f45036a12bcd
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spelling	oai:doaj.org-article:5baf978ecbe94f9e9c65f45036a12bcd2021-12-02T18:31:00ZSpotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations1179-2728https://doaj.org/article/5baf978ecbe94f9e9c65f45036a12bcd2021-07-01T00:00:00Zhttps://www.dovepress.com/spotlight-on-mobocertinib-tak-788-in-nsclc-with-egfr-exon-20-insertion-peer-reviewed-fulltext-article-LCTThttps://doaj.org/toc/1179-2728Shannon S Zhang,1 Viola W Zhu1,2 1University of California, Irvine School of Medicine, Department of Medicine, Orange, CA, USA; 2Chao Family Comprehensive Cancer Center, Orange, CA, USACorrespondence: Viola W ZhuUniversity of California, Irvine School of Medicine, Department of Medicine, 200 S Manchester Ave, Suite 410, Orange, CA, 92868, USATel +1 714-456-8105Fax +1 714-456-2242Email zhuvw@hs.uci.eduAbstract: The EGFR exon 20 insertion (EGFRex20ins) mutations are the third most common EGFR mutations seen in non-small cell lung cancer (NSCLC). More than 50 variants of EGFRex20ins mutations have been identified with A767_V769dupASV being the most common variant across multiple surveys. Treatment with currently available EGFR tyrosine kinase inhibitors (TKIs) including osimertinib is generally ineffective. Amivantamab (JNJ-372), a bispecific monoclonal antibody against EGFR and MET, has recently been approved by the US FDA for patients with advanced or metastatic NSCLC harboring EGFRex20ins mutations after disease progression on platinum-based chemotherapy. Among all the TKIs in clinical development, mobocertinib (TAK-788) has been granted priority review by the FDA for the same indication as amivantamab. Here, we provide a concise review on mobocertinib, with a focus on its chemical structure, preclinical data, and phase 1/2 trial results. Future directions will likely focus on combination approach such as TKI plus chemotherapy in the first-line setting, designing drugs with CNS activity, and exploring disease characteristics of various EGFRex20ins mutation variants and how they may affect treatment response.Keywords: mobocertinib, TAK-788, NSCLC, EGFR exon 20 insertion, TKI, amivantamabZhang SSZhu VWDove Medical Pressarticlemobocertinibtak-788nsclcegfr exon 20 insertiontkiamivantamabNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENLung Cancer: Targets and Therapy, Vol Volume 12, Pp 61-65 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	mobocertinib tak-788 nsclc egfr exon 20 insertion tki amivantamab Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	mobocertinib tak-788 nsclc egfr exon 20 insertion tki amivantamab Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Zhang SS Zhu VW Spotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations
description	Shannon S Zhang,1 Viola W Zhu1,2 1University of California, Irvine School of Medicine, Department of Medicine, Orange, CA, USA; 2Chao Family Comprehensive Cancer Center, Orange, CA, USACorrespondence: Viola W ZhuUniversity of California, Irvine School of Medicine, Department of Medicine, 200 S Manchester Ave, Suite 410, Orange, CA, 92868, USATel +1 714-456-8105Fax +1 714-456-2242Email zhuvw@hs.uci.eduAbstract: The EGFR exon 20 insertion (EGFRex20ins) mutations are the third most common EGFR mutations seen in non-small cell lung cancer (NSCLC). More than 50 variants of EGFRex20ins mutations have been identified with A767_V769dupASV being the most common variant across multiple surveys. Treatment with currently available EGFR tyrosine kinase inhibitors (TKIs) including osimertinib is generally ineffective. Amivantamab (JNJ-372), a bispecific monoclonal antibody against EGFR and MET, has recently been approved by the US FDA for patients with advanced or metastatic NSCLC harboring EGFRex20ins mutations after disease progression on platinum-based chemotherapy. Among all the TKIs in clinical development, mobocertinib (TAK-788) has been granted priority review by the FDA for the same indication as amivantamab. Here, we provide a concise review on mobocertinib, with a focus on its chemical structure, preclinical data, and phase 1/2 trial results. Future directions will likely focus on combination approach such as TKI plus chemotherapy in the first-line setting, designing drugs with CNS activity, and exploring disease characteristics of various EGFRex20ins mutation variants and how they may affect treatment response.Keywords: mobocertinib, TAK-788, NSCLC, EGFR exon 20 insertion, TKI, amivantamab
format	article
author	Zhang SS Zhu VW
author_facet	Zhang SS Zhu VW
author_sort	Zhang SS
title	Spotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations
title_short	Spotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations
title_full	Spotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations
title_fullStr	Spotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations
title_full_unstemmed	Spotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations
title_sort	spotlight on mobocertinib (tak-788) in nsclc with egfr exon 20 insertion mutations
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/5baf978ecbe94f9e9c65f45036a12bcd
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Spotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations

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