Literature DB >> 34096690

Sotorasib for Lung Cancers with KRAS p.G12C Mutation.

Ferdinandos Skoulidis1, Bob T Li1, Grace K Dy1, Timothy J Price1, Gerald S Falchook1, Jürgen Wolf1, Antoine Italiano1, Martin Schuler1, Hossein Borghaei1, Fabrice Barlesi1, Terufumi Kato1, Alessandra Curioni-Fontecedro1, Adrian Sacher1, Alexander Spira1, Suresh S Ramalingam1, Toshiaki Takahashi1, Benjamin Besse1, Abraham Anderson1, Agnes Ang1, Qui Tran1, Omar Mather1, Haby Henary1, Gataree Ngarmchamnanrith1, Gregory Friberg1, Vamsidhar Velcheti1, Ramaswamy Govindan1.   

Abstract

BACKGROUND: Sotorasib showed anticancer activity in patients with KRAS p.G12C-mutated advanced solid tumors in a phase 1 study, and particularly promising anticancer activity was observed in a subgroup of patients with non-small-cell lung cancer (NSCLC).
METHODS: In a single-group, phase 2 trial, we investigated the activity of sotorasib, administered orally at a dose of 960 mg once daily, in patients with KRAS p.G12C-mutated advanced NSCLC previously treated with standard therapies. The primary end point was objective response (complete or partial response) according to independent central review. Key secondary end points included duration of response, disease control (defined as complete response, partial response, or stable disease), progression-free survival, overall survival, and safety. Exploratory biomarkers were evaluated for their association with response to sotorasib therapy.
RESULTS: Among the 126 enrolled patients, the majority (81.0%) had previously received both platinum-based chemotherapy and inhibitors of programmed death 1 (PD-1) or programmed death ligand 1 (PD-L1). According to central review, 124 patients had measurable disease at baseline and were evaluated for response. An objective response was observed in 46 patients (37.1%; 95% confidence interval [CI], 28.6 to 46.2), including in 4 (3.2%) who had a complete response and in 42 (33.9%) who had a partial response. The median duration of response was 11.1 months (95% CI, 6.9 to could not be evaluated). Disease control occurred in 100 patients (80.6%; 95% CI, 72.6 to 87.2). The median progression-free survival was 6.8 months (95% CI, 5.1 to 8.2), and the median overall survival was 12.5 months (95% CI, 10.0 to could not be evaluated). Treatment-related adverse events occurred in 88 of 126 patients (69.8%), including grade 3 events in 25 patients (19.8%) and a grade 4 event in 1 (0.8%). Responses were observed in subgroups defined according to PD-L1 expression, tumor mutational burden, and co-occurring mutations in STK11, KEAP1, or TP53.
CONCLUSIONS: In this phase 2 trial, sotorasib therapy led to a durable clinical benefit without new safety signals in patients with previously treated KRAS p.G12C-mutated NSCLC. (Funded by Amgen and the National Institutes of Health; CodeBreaK100 ClinicalTrials.gov number, NCT03600883.).
Copyright © 2021 Massachusetts Medical Society.

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Year:  2021        PMID: 34096690      PMCID: PMC9116274          DOI: 10.1056/NEJMoa2103695

Source DB:  PubMed          Journal:  N Engl J Med        ISSN: 0028-4793            Impact factor:   176.079


  37 in total

1.  Mutation patterns in a population-based non-small cell lung cancer cohort and prognostic impact of concomitant mutations in KRAS and TP53 or STK11.

Authors:  Linnéa La Fleur; Elin Falk-Sörqvist; Patrik Smeds; Anders Berglund; Magnus Sundström; Johanna Sm Mattsson; Eva Brandén; Hirsh Koyi; Johan Isaksson; Hans Brunnström; Mats Nilsson; Patrick Micke; Lotte Moens; Johan Botling
Journal:  Lung Cancer       Date:  2019-01-09       Impact factor: 5.705

Review 2.  Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design.

Authors:  Jonathan M L Ostrem; Kevan M Shokat
Journal:  Nat Rev Drug Discov       Date:  2016-07-29       Impact factor: 84.694

3.  Cancer Statistics, 2021.

Authors:  Rebecca L Siegel; Kimberly D Miller; Hannah E Fuchs; Ahmedin Jemal
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4.  Prospective randomized trial of docetaxel versus best supportive care in patients with non-small-cell lung cancer previously treated with platinum-based chemotherapy.

Authors:  F A Shepherd; J Dancey; R Ramlau; K Mattson; R Gralla; M O'Rourke; N Levitan; L Gressot; M Vincent; R Burkes; S Coughlin; Y Kim; J Berille
Journal:  J Clin Oncol       Date:  2000-05       Impact factor: 44.544

5.  K-ras Mutation Subtypes in NSCLC and Associated Co-occuring Mutations in Other Oncogenic Pathways.

Authors:  Matthias Scheffler; Michaela A Ihle; Rebecca Hein; Sabine Merkelbach-Bruse; Andreas H Scheel; Janna Siemanowski; Johannes Brägelmann; Anna Kron; Nima Abedpour; Frank Ueckeroth; Merle Schüller; Sophia Koleczko; Sebastian Michels; Jana Fassunke; Helen Pasternack; Carina Heydt; Monika Serke; Rieke Fischer; Wolfgang Schulte; Ulrich Gerigk; Lucia Nogova; Yon-Dschun Ko; Diana S Y Abdulla; Richard Riedel; Karl-Otto Kambartel; Joachim Lorenz; Imke Sauerland; Winfried Randerath; Britta Kaminsky; Lars Hagmeyer; Christian Grohé; Anna Eisert; Rieke Frank; Leonie Gogl; Carsten Schaepers; Alessandra Holzem; Martin Hellmich; Roman K Thomas; Martin Peifer; Martin L Sos; Reinhard Büttner; Jürgen Wolf
Journal:  J Thorac Oncol       Date:  2018-12-31       Impact factor: 15.609

6.  Nivolumab versus Docetaxel in Advanced Nonsquamous Non-Small-Cell Lung Cancer.

Authors:  Hossein Borghaei; Luis Paz-Ares; Leora Horn; David R Spigel; Martin Steins; Neal E Ready; Laura Q Chow; Everett E Vokes; Enriqueta Felip; Esther Holgado; Fabrice Barlesi; Martin Kohlhäufl; Oscar Arrieta; Marco Angelo Burgio; Jérôme Fayette; Hervé Lena; Elena Poddubskaya; David E Gerber; Scott N Gettinger; Charles M Rudin; Naiyer Rizvi; Lucio Crinò; George R Blumenschein; Scott J Antonia; Cécile Dorange; Christopher T Harbison; Friedrich Graf Finckenstein; Julie R Brahmer
Journal:  N Engl J Med       Date:  2015-09-27       Impact factor: 91.245

7.  STK11/LKB1 Mutations and PD-1 Inhibitor Resistance in KRAS-Mutant Lung Adenocarcinoma.

Authors:  Ferdinandos Skoulidis; Michael E Goldberg; Danielle M Greenawalt; Matthew D Hellmann; Mark M Awad; Justin F Gainor; Alexa B Schrock; Ryan J Hartmaier; Sally E Trabucco; Laurie Gay; Siraj M Ali; Julia A Elvin; Gaurav Singal; Jeffrey S Ross; David Fabrizio; Peter M Szabo; Han Chang; Ariella Sasson; Sujaya Srinivasan; Stefan Kirov; Joseph Szustakowski; Patrik Vitazka; Robin Edwards; Jose A Bufill; Neelesh Sharma; Sai-Hong I Ou; Nir Peled; David R Spigel; Hira Rizvi; Elizabeth Jimenez Aguilar; Brett W Carter; Jeremy Erasmus; Darragh F Halpenny; Andrew J Plodkowski; Niamh M Long; Mizuki Nishino; Warren L Denning; Ana Galan-Cobo; Haifa Hamdi; Taghreed Hirz; Pan Tong; Jing Wang; Jaime Rodriguez-Canales; Pamela A Villalobos; Edwin R Parra; Neda Kalhor; Lynette M Sholl; Jennifer L Sauter; Achim A Jungbluth; Mari Mino-Kenudson; Roxana Azimi; Yasir Y Elamin; Jianjun Zhang; Giulia C Leonardi; Fei Jiang; Kwok-Kin Wong; J Jack Lee; Vassiliki A Papadimitrakopoulou; Ignacio I Wistuba; Vincent A Miller; Garrett M Frampton; Jedd D Wolchok; Alice T Shaw; Pasi A Jänne; Philip J Stephens; Charles M Rudin; William J Geese; Lee A Albacker; John V Heymach
Journal:  Cancer Discov       Date:  2018-05-17       Impact factor: 39.397

8.  Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism.

Authors:  Piro Lito; Martha Solomon; Lian-Sheng Li; Rasmus Hansen; Neal Rosen
Journal:  Science       Date:  2016-01-14       Impact factor: 47.728

9.  Rapid non-uniform adaptation to conformation-specific KRAS(G12C) inhibition.

Authors:  Jenny Y Xue; Yulei Zhao; Jordan Aronowitz; Trang T Mai; Alberto Vides; Besnik Qeriqi; Dongsung Kim; Chuanchuan Li; Elisa de Stanchina; Linas Mazutis; Davide Risso; Piro Lito
Journal:  Nature       Date:  2020-01-08       Impact factor: 49.962

10.  KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors.

Authors:  David S Hong; Marwan G Fakih; John H Strickler; Jayesh Desai; Gregory A Durm; Geoffrey I Shapiro; Gerald S Falchook; Timothy J Price; Adrian Sacher; Crystal S Denlinger; Yung-Jue Bang; Grace K Dy; John C Krauss; Yasutoshi Kuboki; James C Kuo; Andrew L Coveler; Keunchil Park; Tae Won Kim; Fabrice Barlesi; Pamela N Munster; Suresh S Ramalingam; Timothy F Burns; Funda Meric-Bernstam; Haby Henary; Jude Ngang; Gataree Ngarmchamnanrith; June Kim; Brett E Houk; Jude Canon; J Russell Lipford; Gregory Friberg; Piro Lito; Ramaswamy Govindan; Bob T Li
Journal:  N Engl J Med       Date:  2020-09-20       Impact factor: 176.079

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  139 in total

1.  Sotorasib effective in KRAS-mutant NSCLC.

Authors:  Peter Sidaway
Journal:  Nat Rev Clin Oncol       Date:  2021-06-17       Impact factor: 66.675

Review 2.  Targeting Mutated KRAS Genes to Treat Solid Tumours.

Authors:  Tharani Krishnan; Rachel Roberts-Thomson; Vy Broadbridge; Timothy Price
Journal:  Mol Diagn Ther       Date:  2021-12-16       Impact factor: 4.074

Review 3.  Older Patients with Lung Cancer: a Summary of Seminal Contributions to Optimal Patient Care.

Authors:  Alina Basnet; Asrar Alahmadi; Ajeet Gajra
Journal:  Curr Oncol Rep       Date:  2022-07-28       Impact factor: 5.945

Review 4.  [Targeted treatment of non-small cell lung cancer].

Authors:  Matthias Scheffler; Sebastian Michels; Lucia Nogova
Journal:  Inn Med (Heidelb)       Date:  2022-06-27

Review 5.  Targeting KRAS in pancreatic cancer: new drugs on the horizon.

Authors:  Sahar F Bannoura; Md Hafiz Uddin; Misako Nagasaka; Farzeen Fazili; Mohammed Najeeb Al-Hallak; Philip A Philip; Bassel El-Rayes; Asfar S Azmi
Journal:  Cancer Metastasis Rev       Date:  2021-09-09       Impact factor: 9.237

6.  The KRAS-G12C inhibitor: activity and resistance.

Authors:  Jiao Liu; Rui Kang; Daolin Tang
Journal:  Cancer Gene Ther       Date:  2021-09-01       Impact factor: 5.854

7.  Direct Target Site Identification of a Sulfonyl-Triazole Covalent Kinase Probe by LC-MS Chemical Proteomics.

Authors:  Rebecca L McCloud; Kun Yuan; Keira E Mahoney; Dina L Bai; Jeffrey Shabanowitz; Mark M Ross; Donald F Hunt; Ku-Lung Hsu
Journal:  Anal Chem       Date:  2021-08-25       Impact factor: 8.008

8.  Acquired Resistance to KRASG12C Inhibition in Cancer.

Authors:  Mark M Awad; Shengwu Liu; Igor I Rybkin; Kathryn C Arbour; Julien Dilly; Viola W Zhu; Melissa L Johnson; Rebecca S Heist; Tejas Patil; Gregory J Riely; Joseph O Jacobson; Xiaoping Yang; Nicole S Persky; David E Root; Kristen E Lowder; Hanrong Feng; Shannon S Zhang; Kevin M Haigis; Yin P Hung; Lynette M Sholl; Brian M Wolpin; Julie Wiese; Jason Christiansen; Jessica Lee; Alexa B Schrock; Lee P Lim; Kavita Garg; Mark Li; Lars D Engstrom; Laura Waters; J David Lawson; Peter Olson; Piro Lito; Sai-Hong I Ou; James G Christensen; Pasi A Jänne; Andrew J Aguirre
Journal:  N Engl J Med       Date:  2021-06-24       Impact factor: 91.245

Review 9.  Emerging strategies to target RAS signaling in human cancer therapy.

Authors:  Kun Chen; Yalei Zhang; Ling Qian; Peng Wang
Journal:  J Hematol Oncol       Date:  2021-07-23       Impact factor: 17.388

Review 10.  Targeted therapy in advanced non-small cell lung cancer: current advances and future trends.

Authors:  Umair Majeed; Rami Manochakian; Yujie Zhao; Yanyan Lou
Journal:  J Hematol Oncol       Date:  2021-07-08       Impact factor: 17.388

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