Zipalertinib in Patients With Epidermal Growth Factor Receptor Exon 20 Insertion-Positive Non–Small Cell Lung Cancer Previously Treated With Platinum-Based Chemotherapy With or Without Amivantamab

Зипалертиниб у пациентов с немелкоклеточным раком легкого с мутациями вставки в экзоне 20 рецептора эпидермального фактора роста, ранее получавших платиновую химиотерапию с амивантамабом или без него
Antonio Passaro, Ross A. Soo, Óscar Juan, Se‐Hoon Lee, Hiroshi Tanaka, Egbert F. Smit, Daniel S.W. Tan, James Chih‐Hsin Yang, Vamsidhar Velcheti, Lorenzo Antonuzzo, Danny Nguyen, Ji‐Youn Han, Annalisa Fontana, Se-Hoon Lee, Helena A. Yu, Victor Lee, Zofia Piotrowska, Alexander I. Spira, Mark A. Socinski, Delvys Rodríguez‐Abreu, E. Felip Font, Chao‐Hua Chiu, Rachel E. Sanborn, Haruyasu Murakami, Antonio Calles, Nashat Gabrail, Kazumi Nishino, M.R. García Campelo, Byoung Yong Shim, Gee-Chen Chang, Gerrina Ruiter, Se Hyun Kim, John Wrangle, H. Daga, G. Fernández-Hinojal, Sang-We Kim, Shigeki Umemura, Mariano Provencio Pulla, Erika Krasnickas Keeton, Zhihui Sunny Yang, Shengting Li, Zhiying Cindy Xu, Jeffrey A. Jones, for the REZILIENT1 Investigators, Helena Yu, Danny T. Nguyen, Gregory P. Kalemkerian, Ross Lai Kit Soo, Tsung-Ying Yang, Chao-Hua Chiu, Yasushi Goto, Ryo Ariyasu, Oscar Juan-Vidal, Gonzalo Fernández Hinojal, M. Cobo Dols, Laura Perez, Ernesto Samuel Nadal Alforia, Tatiana Hernández, Hyun Woo Lee, Sung Yong Lee, Young Saing Kim
2025-06-01

EGFR exon 20 insertion (ex20ins)duration of response (DOR)non–small cell lung cancer (NSCLC)objective response rate (ORR)zipalertinib
PURPOSE To evaluate the safety and efficacy of zipalertinib, an irreversible epidermal growth factor receptor (EGFR) inhibitor, in pretreated patients with non–small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion (ex20ins) mutations. METHODS REZILIENT1 (ClinicalTrials.gov identifier: NCT04036682 ) is a phase I/II open-label trial enrolling patients with locally advanced or metastatic EGFR ex20ins-mutant NSCLC previously treated with platinum-based chemotherapy with/without ex20ins-targeted therapies. Asymptomatic, treated and untreated stable CNS metastases are permitted. We report data from patients treated with zipalertinib 100 mg twice daily. The primary end points are objective response rate (ORR) and duration of response (DOR) by independent central review. RESULTS At data cutoff (December 10, 2024), 244 patients had received treatment with zipalertinib 100 mg twice daily. The primary efficacy population (8 months' follow-up) comprised patients who had received prior platinum-based chemotherapy without ex20ins-targeted therapy (125 patients), with amivantamab only (30 patients), or with amivantamab and other ex20ins-targeted therapy (21 patients). The confirmed ORR was 35.2% (95% CI, 28.2 to 42.8); median DOR was 8.8 months (95% CI, 8.3 to 12.7). Among patients who received prior platinum-based chemotherapy without ex20ins-targeted therapy, amivantamab only, or amivantamab and other ex20ins-targeted therapy, the confirmed ORR was 40%, 30%, and 14.3%, and median DOR was 8.8, 14.7, and 4.2 months, respectively. Among 68 patients with CNS metastases, the ORR was 30.9%. The most common grade ≥3 treatment-related adverse events were anemia (7%), pneumonitis and rash (2.5% each), and diarrhea, ALT increased, and platelet count decreased (2% each). CONCLUSION Zipalertinib demonstrated clinically meaningful efficacy with a manageable safety profile in patients with EGFR ex20ins-mutant NSCLC who received prior platinum-based chemotherapy with or without amivantamab.
1
Among 68 patients with CNS metastases, zipalertinib achieved an ORR of 30.9%; most common grade ≥3 treatment-related adverse events included anemia (7%), pneumonitis and rash (2.5% each).
2
Median DOR by prior therapy was 8.8 months (platinum only), 14.7 months (amivantamab only), and 4.2 months (amivantamab plus other targeted therapy).
3
Median duration of response (DOR) for the overall population was 8.8 months (95% CI, 8.3 to 12.7).
4
ORR varied by prior therapy: 40% in patients with prior platinum chemotherapy only, 30% with prior amivantamab only, and 14.3% with prior amivantamab plus other ex20ins-targeted therapy.
5
Zipalertinib 100 mg twice daily produced a confirmed objective response rate (ORR) of 35.2% (95% CI, 28.2 to 42.8) in EGFR exon 20 insertion–positive NSCLC previously treated with platinum chemotherapy.

Patients with EGFR exon 20 insertion–positive non–small cell lung cancer previously treated with platinum-based chemotherapy with or without amivantamab

Efficacy and safety of zipalertinib 100 mg twice daily, measured by objective response rate and duration of response (primary endpoints) and treatment-related adverse events in this patient population

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2025-06-01
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Authors
Antonio Passaro
Ross A. Soo
Óscar Juan
Se‐Hoon Lee
Hiroshi Tanaka
Egbert F. Smit
Daniel S.W. Tan
James Chih‐Hsin Yang
Vamsidhar Velcheti
Lorenzo Antonuzzo
Danny Nguyen
Ji‐Youn Han
Annalisa Fontana
Se-Hoon Lee
Helena A. Yu
Victor Lee
Zofia Piotrowska
Alexander I. Spira
Mark A. Socinski
Delvys Rodríguez‐Abreu
E. Felip Font
Chao‐Hua Chiu
Rachel E. Sanborn
Haruyasu Murakami
Antonio Calles
Nashat Gabrail
Kazumi Nishino
M.R. García Campelo
Byoung Yong Shim
Gee-Chen Chang
Gerrina Ruiter
Se Hyun Kim
John Wrangle
H. Daga
G. Fernández-Hinojal
Sang-We Kim
Shigeki Umemura
Mariano Provencio Pulla
Erika Krasnickas Keeton
Zhihui Sunny Yang
Shengting Li
Zhiying Cindy Xu
Jeffrey A. Jones
for the REZILIENT1 Investigators
Helena Yu
Danny T. Nguyen
Gregory P. Kalemkerian
Ross Lai Kit Soo
Tsung-Ying Yang
Chao-Hua Chiu
Yasushi Goto
Ryo Ariyasu
Oscar Juan-Vidal
Gonzalo Fernández Hinojal
M. Cobo Dols
Laura Perez
Ernesto Samuel Nadal Alforia
Tatiana Hernández
Hyun Woo Lee
Sung Yong Lee
Young Saing Kim
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