Article
Pharmacology & Pharmacy
Neeraj Gupta, Anna Largajolli, Han Witjes, Paul M. Diderichsen, Steven Zhang, Michael J. Hanley, Jianchang Lin, Minal Mehta
Summary: This study evaluated the efficacy and safety of mobocertinib in patients with EGFR mutations in lung cancer, and the results showed that the 160mg dose of mobocertinib had a favorable benefit-risk profile.
CLINICAL PHARMACOLOGY & THERAPEUTICS
(2022)
Article
Medicine, General & Internal
Caicun Zhou, Ke-Jing Tang, Byoung Chul Cho, Baogang Liu, Luis Paz-Ares, Susanna Cheng, Satoru Kitazono, Muthukkumaran Thiagarajan, Jonathan W. Goldman, Joshua K. Sabari, Rachel E. Sanborn, Aaron S. Mansfield, Jen-Yu Hung, Michael Boyer, Sanjay Popat, Josiane Mourao Dias, Enriqueta Felip, Margarita Majem, Mahmut Gumus, Sang-we Kim, Akira Ono, John Xie, Archan Bhattacharya, Trishala Agrawal, S. Martin Shreeve, Roland E. Knoblauch, Keunchil Park, Nicolas Girard, PAPILLON Investigators
Summary: Amivantamab plus chemotherapy demonstrated significantly longer progression-free survival and higher response rate in patients with advanced NSCLC with EGFR exon 20 insertions compared to chemotherapy alone. The combination therapy showed superior efficacy as a first-line treatment option.
NEW ENGLAND JOURNAL OF MEDICINE
(2023)
Article
Biochemistry & Molecular Biology
Mohd Imran, Shah Alam Khan, Mohammed Kanan Alshammari, Meshal Ayedh Alreshidi, Abeer Abdullah Alreshidi, Rawan Sulaiman Alghonaim, Fayez Aboud Alanazi, Sultan Alshehri, Mohammed M. Ghoneim, Faiyaz Shakeel
Summary: This article discusses the development and application of mobocertinib, an oral drug targeting the common EGFRex20ins mutation in lung cancer. Analysis of patent literature has revealed a series of patents and patent applications related to mobocertinib, providing a foundation for future scientific research. Exciting prospects are foreseen for combination therapies involving mobocertinib with other approved anticancer agents.
Editorial Material
Oncology
Jose M. Pacheco
Summary: Amivantamab is currently the only FDA-approved therapy for NSCLC with EGFR exon 20 insertions, but patients often develop disease progression on this treatment. Studies show that mobocertinib may be a potentially efficacious agent for NSCLC with EGFR exon 20 insertions.
Editorial Material
Oncology
Andres Felipe Cardona, Maria Gonzalez-Cao, Oscar Arrieta, Rafael Rosell
Summary: This study reveals the therapy dilemma faced by EGFR exon 20 insertions subgroup in NSCLC and the effectiveness of poziotinib in treating this subgroup. The study also finds that tumor growth in poziotinib-resistant exon 20 insertions can be inhibited by pharmacological inhibition of spindle assembly checkpoint components.
Review
Oncology
Francesco Passiglia, Umberto Malapelle, Nicola Normanno, Carmine Pinto
Summary: Pharmacological inhibition of EGFRex20 insertions offers new treatment opportunities for advanced NSCLC patients. Drugs like amivantamab and mobocertinib have received regulatory approval. NGS-based genotyping is considered the gold standard approach for profiling advanced NSCLC patients.
CANCER TREATMENT REVIEWS
(2022)
Article
Medicine, General & Internal
Maria Rosario Garcia Campelo, Caicun Zhou, Suresh S. Ramalingam, Huamao M. Lin, Tae Min Kim, Gregory J. Riely, Tarek Mekhail, Danny Nguyen, Erin Goodman, Minal Mehta, Sanjay Popat, Pasi A. Janne
Summary: Mobocertinib, an oral EGFR tyrosine kinase inhibitor, demonstrated durable responses in previously treated mNSCLC patients with EGFR ex20ins+ mutations. Patient-reported outcomes showed clinically meaningful improvement in lung cancer-related symptoms, with maintained health-related quality of life despite changes in some adverse event symptom scales.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Oncology
Timothee Olivier, Vinay Prasad
Summary: This study discusses the questions regarding the unmet need within the accelerated approval pathway, the lack of equipoise between new compounds and existing options, the unsupported recommendation by NCCN, and the insufficient clarity provided by postmarketing requirements. The study has implications beyond patients with exon 20 insertion, as it can prevent the misguided incorporation of new compounds into clinical practice.
TRANSLATIONAL ONCOLOGY
(2022)
Article
Oncology
Waleed Kian, Petros Christopoulos, Areen A. Remilah, Esther Levison, Elizabeth Dudnik, Walid Shalata, Bilal Krayim, Ranin Marei, Alexander Yakobson, Martin Faehling, Dolev Kahala, Inbal Sara Granot, Dina Levitas, Nir Peled, Laila C. Roisman
Summary: Mobocertinib has shown significant efficacy and good safety profile in patients with EGFRexon20ins. It is a novel TKI that selectively targets EGFRex20ins.
FRONTIERS IN ONCOLOGY
(2022)
Article
Oncology
Gregory J. Riely, Joel W. Neal, D. Ross Camidge, Alexander Spira, Zofia Piotrowska, Daniel B. Costa, Anne S. Tsao, Jyoti D. Patel, Shirish M. Gadgeel, Lyudmila Bazhenova, Viola W. Zhu, Howard L. West, Tarek Mekhail, Ryan D. Gentzler, Danny Nguyen, Sylvie Vincent, Steven Zhang, Jianchang Lin, Veronica Bunn, Shu Jin, Shuanglian Li, Pasi A. Janne
Summary: Mobocertinib, an oral EGFR inhibitor targeting EGFR gene mutations in non-small cell lung cancer, demonstrated antitumor activity with manageable toxicity in patients with EGFRex20ins mutations in this study, supporting further development in this patient population.
Article
Oncology
Elizabeth S. Duke, Liza Stapleford, Nicole Drezner, Anup K. Amatya, Pallavi S. Mishra-Kalyani, Yuan -Li Shen, Kimberly Maxfield, Jeanne Fourie Zirkelbach, Youwei Bi, Jiang Liu, Xinyuan Zhang, Hezhen Wang, Yuching Yang, Nan Zheng, Kelie Reece, Emily Wearne, Jacqueline J. Glen, Idara Ojofeitimi, Barbara Scepura, Abhilasha Nair, Rama Kamesh Bikkavilli, Soma Ghosh, Reena Philip, Richard Pazdur, Julia A. Beaver, Harpeet Singh, Martha Donoghue
Summary: The FDA has granted accelerated approval for a new drug to treat adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with EGFR exon 20 insertion mutations. The approval was based on data from a clinical trial and the drug showed an overall response rate of 28% with a median duration of response of 17.5 months. Common adverse reactions include diarrhea, rash, nausea, stomatitis, vomiting, decreased appetite, paronychia, fatigue, dry skin, and musculoskeletal pain. This is the first oral targeted therapy approved for patients with advanced EGFR exon 20 insertion mutation-positive NSCLC.
CLINICAL CANCER RESEARCH
(2023)
Review
Oncology
Antonio Passaro, Tony Mok, Solange Peters, Sanjay Popat, Myung-Ju Ahn, Filippo de Marinis
Summary: The first-line treatment for NSCLC patients with EGFR mutations is an EGFR TKI, but some patients have uncommon mutations with varying sensitivities to different TKIs, complicating treatment decisions. Recent studies have integrated data on the activity of different TKIs against major uncommon EGFR mutations and proposed treatment strategies for these cases.
JOURNAL OF THORACIC ONCOLOGY
(2021)
Article
Oncology
Sai-Hong I. Ou, Huamao M. Lin, Jin-Liern Hong, Yu Yin, Shu Jin, Jianchang Lin, Minal Mehta, Pingkuan Zhang, Danny Nguyen, Joel W. Neal
Summary: This study compared the effectiveness of mobocertinib with real-world treatments in patients with EGFR exon 20 insertions. The results showed that mobocertinib had better outcomes in this rare population compared to other available therapies.
Article
Oncology
Francois Gonzalvez, Sylvie Vincent, Theresa E. Baker, Alexandra E. Gould, Shuai Li, Scott D. Wardwell, Sara Nadworny, Yaoyu Ning, Sen Zhang, Wei-Sheng Huang, Yongbo Hu, Feng Li, Matthew T. Greenfield, Stephan G. Zech, Biplab Das, Narayana Narasimhan, Tim Clackson, David Dalgarno, William C. Shakespeare, Michael Fitzgerald, Johara Chouitar, Robert J. Griffin, Shengwu Liu, Kwok-Kin Wong, Xiaotian Zhu, Victor M. Rivera
Summary: Mobocertinib is a novel irreversible EGFR TKI specifically designed to target oncogenic variants containing activating EGFRex20ins mutations. Preclinical data demonstrate that mobocertinib inhibits EGFRex-20ins-driven cell lines more potently than approved EGFR TKIs, supporting its ongoing clinical development for the treatment of EGFRex20ins-mutated NSCLC.
Review
Oncology
Alex Friedlaender, Vivek Subbiah, Alessandro Russo, Giuseppe Luigi Banna, Umberto Malapelle, Christian Rolfo, Alfredo Addeo
Summary: Classic activating mutations in EGFR and HER2 are predictive of response to targeted therapies, while insertion mutations in exon 20 of either gene are generally less sensitive to treatment. Novel therapeutic strategies are being developed to effectively target tumors driven by these non-classic mutations.
NATURE REVIEWS CLINICAL ONCOLOGY
(2022)
