Targeting KRASG12C in colorectal cancer: the beginning of a new era

被引：28

作者：

Ciardiello, D. ^{[1
,2
,4
]}

Maiorano, B. A. ^{[1
,3
]}

Martinelli, E. ^{[2
]}

机构：

[1] IRCCS Fdn Casa Sollievo Sofferenza, Oncol Unit, San Giovanni Rotondo, Italy

[2] Luigi Vanvitelli Univ Campania, Dept Precis Med, Med Oncol Unit, Naples, Italy

[3] Univ Cattolica Sacro Cuore, Dept Translat Med & Surg, Rome, Italy

[4] IRCCS Fdn Casa Sollievo Sofferenza, Oncol Unit, I-71013 San Giovanni Rotondo, Italy

来源：

ESMO OPEN | 2023年 / 8卷 / 01期

关键词：

CRC; KRASG12C; target therapies; precision medicine; INHIBITOR; TRIAL;

D O I：

10.1016/j.esmoop.2022.100745

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

RAS mutation is considered one of the most relevant oncogenic drivers in human cancers. Unfortunately, for more than three decades, RAS has been considered an undruggable target. Recently, the discovery of selective and potent KRASG12C inhibitors represented a light at the end of the tunnel. Indeed, sotorasib and adagrasib proved clinical activity in patients with refractory metastatic colorectal cancer harboring KRASG12C mutation; however, responses are lower than expected, suggesting the presence of intrinsic resistance. Consequently, novel combinatory strategies to disrupt the RAS signaling pathways are under clinical investigation. This review aims to discuss the current knowledge and novel routes of KRASG12C inhibition in metastatic colorectal cancer.

引用

页数：7

共 45 条

[1] Epithelial-to-Mesenchymal Transition is a Cause of Both Intrinsic and Acquired Resistance to KRAS G12C Inhibitor in KRAS G12C-Mutant Non-Small Cell Lung Cancer [J].

Adachi, Yuta ;

Ito, Kentaro ;

Hayashi, Yuko ;

Kimura, Ryo ;

Tan, Tuan Zea ;

Yamaguchi, Rui ;

Ebi, Hiromichi .

CLINICAL CANCER RESEARCH, 2020, 26 (22) :5962-5973

[2] EGFR Blockade Reverts Resistance to KRASG12C Inhibition in Colorectal Cancer [J].

Amodio, Vito ;

Yaeger, Rona ;

Arcella, Pamela ;

Cancelliere, Carlotta ;

Lamba, Simona ;

Lorenzato, Annalisa ;

Arena, Sabrina ;

Montone, Monica ;

Mussolin, Benedetta ;

Bian, Yu ;

Whaley, Adele ;

Pinnelli, Marika ;

Murciano-Goroff, Yonina R. ;

Vakiani, Efsevia ;

Valeri, Nicola ;

Liao, Wei-Li ;

Bhalkikar, Anuja ;

Thyparambil, Sheeno ;

Zhao, Hui-Yong ;

de Stanchina, Elisa ;

Marsoni, Silvia ;

Siena, Salvatore ;

Bertotti, Andrea ;

Trusolino, Livio ;

Li, Bob T. ;

Rosen, Neal ;

Di Nicolantonio, Federica ;

Bardelli, Alberto ;

Misale, Sandra .

CANCER DISCOVERY, 2020, 10 (08) :1129-1139

[3] Pembrolizumab in Microsatellite-Instability-High Advanced Colorectal Cancer [J].

Andre, T. ;

Shiu, K-K ;

Kim, T. W. ;

Jensen, B., V ;

Jensen, L. H. ;

Punt, C. ;

Smith, D. ;

Garcia-Carbonero, R. ;

Benavides, M. ;

Gibbs, P. ;

de la Fouchardiere, C. ;

Rivera, F. ;

Elez, E. ;

Bendell, J. ;

Le, D. T. ;

Yoshino, T. ;

Van Cutsem, E. ;

Yang, P. ;

Farooqui, M. Z. H. ;

Marinello, P. ;

Diaz, L. A., Jr. .

NEW ENGLAND JOURNAL OF MEDICINE, 2020, 383 (23) :2207-2218

[4] Acquired Resistance to KRASG12C Inhibition in Cancer [J].

Awad, M. M. ;

Liu, S. ;

Rybkin, I. I. ;

Arbour, K. C. ;

Dilly, J. ;

Zhu, V. W. ;

Johnson, M. L. ;

Heist, R. S. ;

Patil, T. ;

Riely, G. J. ;

Jacobson, J. O. ;

Yang, X. ;

Persky, N. S. ;

Root, D. E. ;

Lowder, K. E. ;

Feng, H. ;

Zhang, S. S. ;

Haigis, K. M. ;

Hung, Y. P. ;

Sholl, L. M. ;

Wolpin, B. M. ;

Wiese, J. ;

Christiansen, J. ;

Lee, J. ;

Schrock, A. B. ;

Lim, L. P. ;

Garg, K. ;

Li, M. ;

Engstrom, L. D. ;

Waters, L. ;

Lawson, J. D. ;

Olson, P. ;

Lito, P. ;

Ou, S. -H. I. ;

Christensen, J. G. ;

Janne, P. A. ;

Aguirre, A. J. .

NEW ENGLAND JOURNAL OF MEDICINE, 2021, 384 (25) :2382-2393

[5] Targeting protein prenylation for cancer therapy [J].

Berndt, Norbert ;

Hamilton, Andrew D. ;

Sebti, Said M. .

NATURE REVIEWS CANCER, 2011, 11 (11) :775-791

[6] The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity [J].

Canon, Jude ;

Rex, Karen ;

Saiki, Anne Y. ;

Mohr, Christopher ;

Cooke, Keegan ;

Bagal, Dhanashri ;

Gaida, Kevin ;

Holt, Tyler ;

Knutson, Charles G. ;

Koppada, Neelima ;

Lanman, Brian A. ;

Werner, Jonathan ;

Rapaport, Aaron S. ;

San Miguel, Tisha ;

Ortiz, Roberto ;

Osgood, Tao ;

Sun, Ji-Rong ;

Zhu, Xiaochun ;

McCarter, John D. ;

Volak, Laurie P. ;

Houk, Brett E. ;

Fakih, Marwan G. ;

O'Neil, Bert H. ;

Price, Timothy J. ;

Falchook, Gerald S. ;

Desai, Jayesh ;

Kuo, James ;

Govindan, Ramaswamy ;

Hong, David S. ;

Ouyang, Wenjun ;

Henary, Haby ;

Arvedson, Tara ;

Cee, Victor J. ;

Lipford, J. Russell .

NATURE, 2019, 575 (7781) :217-+

[7] Isoprenylcysteine carboxylmethyltransferase is required for the impact of mutant KRAS on TAZ protein level and cancer cell self-renewal [J].

Chai, Tin Fan ;

Manu, Kanjoormana Aryan ;

Casey, Patrick J. ;

Wang, Mei .

ONCOGENE, 2020, 39 (31) :5373-5389

[8] The Prognostic Impact of KRAS G12C Mutation in Patients with Metastatic Colorectal Cancer: A Multicenter Retrospective Observational Study [J].

Chida, Keigo ;

Kotani, Daisuke ;

Masuishi, Toshiki ;

Kawakami, Takeshi ;

Kawamoto, Yasuyuki ;

Kato, Kyoko ;

Fushiki, Kunihiro ;

Sawada, Kentaro ;

Kumanishi, Ryosuke ;

Shirasu, Hiromichi ;

Matsubara, Yuki ;

Yuki, Satoshi ;

Komatsu, Yoshito ;

Yamazaki, Kentaro ;

Yoshino, Takayuki .

ONCOLOGIST, 2021, 26 (10) :845-853

[9] Clinical efficacy of sequential treatments in KRASG12C-mutant metastatic colorectal cancer: findings from a real-life multicenter Italian study (CRC-KR GOIM) [J].

Ciardiello, D. ;

Chiarazzo, C. ;

Famiglietti, V. ;

Damato, A. ;

Pinto, C. ;

Zampino, M. G. ;

Castellano, G. ;

Gervaso, L. ;

Zaniboni, A. ;

Oneda, E. ;

Rapisardi, S. ;

Bordonaro, R. ;

Zichi, C. ;

De Vita, F. ;

Di Maio, M. ;

Parisi, A. ;

Giampieri, R. ;

Berardi, R. ;

Lavacchi, D. ;

Antonuzzo, L. ;

Tamburini, E. ;

Maiorano, B. A. ;

Parrella, P. ;

Latiano, T. P. ;

Normanno, N. ;

De Stefano, A. ;

Avallone, A. ;

Martini, G. ;

Napolitano, S. ;

Troiani, T. ;

Martinelli, E. ;

Ciardiello, F. ;

De Vita, F. ;

Maiello, E. .

ESMO OPEN, 2022, 7 (05)

[10] Immunotherapy of colorectal cancer: Challenges for therapeutic efficacy [J].

Ciardiello, Davide ;

Vitiello, Pietro Paolo ;

Cardone, Claudia ;

Martini, Giulia ;

Troiani, Teresa ;

Martinelli, Erika ;

Ciardiello, Fortunato .

CANCER TREATMENT REVIEWS, 2019, 76 :22-32

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