The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity.


Journal

Nature
ISSN: 1476-4687
Titre abrégé: Nature
Pays: England
ID NLM: 0410462

Informations de publication

Date de publication:
11 2019
Historique:
received: 29 03 2019
accepted: 18 09 2019
pubmed: 2 11 2019
medline: 14 4 2020
entrez: 1 11 2019
Statut: ppublish

Résumé

KRAS is the most frequently mutated oncogene in cancer and encodes a key signalling protein in tumours

Identifiants

pubmed: 31666701
doi: 10.1038/s41586-019-1694-1
pii: 10.1038/s41586-019-1694-1
doi:

Substances chimiques

Antineoplastic Agents 0
KRAS protein, human 0
Piperazines 0
Pyridines 0
Pyrimidines 0
sotorasib 2B2VM6UC8G
Proto-Oncogene Proteins p21(ras) EC 3.6.5.2

Types de publication

Clinical Trial Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, Non-P.H.S.

Langues

eng

Sous-ensembles de citation

IM

Pagination

217-223

Subventions

Organisme : NIH HHS
ID : S10 OD021832
Pays : United States

Commentaires et corrections

Type : CommentIn
Type : CommentIn
Type : CommentIn
Type : CommentIn
Type : CommentIn

Références

Barbacid, M. ras genes. Annu. Rev. Biochem. 56, 779–827 (1987).
doi: 10.1146/annurev.bi.56.070187.004023
Simanshu, D. K., Nissley, D. V. & McCormick, F. RAS proteins and their regulators in human disease. Cell 170, 17–33 (2017).
doi: 10.1016/j.cell.2017.06.009
Ostrem, J. M., Peters, U., Sos, M. L., Wells, J. A. & Shokat, K. M. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature 503, 548–551 (2013).
doi: 10.1038/nature12796
Patricelli, M. P. et al. Selective inhibition of oncogenic KRAS output with small molecules targeting the inactive state. Cancer Discov. 6, 316–329 (2016).
doi: 10.1158/2159-8290.CD-15-1105
Janes, M. R. et al. Targeting KRAS mutant cancers with a covalent G12C-specific inhibitor. Cell 172, 578–589 (2018).
doi: 10.1016/j.cell.2018.01.006
Pai, E. F. et al. Structure of the guanine-nucleotide-binding domain of the Ha-ras oncogene product p21 in the triphosphate conformation. Nature 341, 209–214 (1989).
doi: 10.1038/341209a0
Milburn, M. V. et al. Molecular switch for signal transduction: structural differences between active and inactive forms of protooncogenic ras proteins. Science 247, 939–945 (1990).
doi: 10.1126/science.2406906
Cully, M. & Downward, J. SnapShot: Ras signaling. Cell 133, 1292–1292.e1 (2008).
doi: 10.1016/j.cell.2008.06.020
Vetter, I. R. & Wittinghofer, A. The guanine nucleotide-binding switch in three dimensions. Science 294, 1299–1304 (2001).
doi: 10.1126/science.1062023
Scheffzek, K. et al. The Ras–RasGAP complex: structural basis for GTPase activation and its loss in oncogenic Ras mutants. Science 277, 333–338 (1997).
doi: 10.1126/science.277.5324.333
Jimeno, A., Messersmith, W. A., Hirsch, F. R., Franklin, W. A. & Eckhardt, S. G. KRAS mutations and susceptibility to cetuximab and panitumumab in colorectal cancer. Cancer J. 15, 110–113 (2009).
doi: 10.1097/PPO.0b013e31819e3202
Welsh, S. J. & Corrie, P. G. Management of BRAF and MEK inhibitor toxicities in patients with metastatic melanoma. Ther. Adv. Med. Oncol. 7, 122–136 (2015).
doi: 10.1177/1758834014566428
Fakih, M. & Vincent, M. Adverse events associated with anti-EGFR therapies for the treatment of metastatic colorectal cancer. Curr. Oncol. 17, S18–S30 (2010).
pubmed: 20680104 pmcid: 20680104
AACR Project GENIE Consortium. AACR Project GENIE: powering precision medicine through an international consortium. Cancer Discov. 7, 818–831 (2017).
doi: 10.1158/2159-8290.CD-17-0151
Hansen, R. et al. The reactivity-driven biochemical mechanism of covalent KRAS
doi: 10.1038/s41594-018-0061-5
clinicaltrials.gov. A Phase 1/2, Study Evaluating the Safety, Tolerability, PK, and Efficacy of AMG 510 in Subjects With Solid Tumors With a Specific KRAS Mutation https://clinicaltrials.gov/ct2/show/NCT03600883 (2018).
Gentile, D. R. et al. Ras binder induces a modified switch-II Pocket in GTP and GDP states. Cell Chem. Biol. 24, 1455–1466 (2017).
doi: 10.1016/j.chembiol.2017.08.025
Schwartz, P. A. et al. Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance. Proc. Natl Acad. Sci. USA 111, 173–178 (2014).
doi: 10.1073/pnas.1313733111
Cee, V. J. et al. Systematic study of the glutathione (GSH) reactivity of N-arylacrylamides: 1. Effects of aryl substitution. J. Med. Chem. 58, 9171–9178 (2015).
doi: 10.1021/acs.jmedchem.5b01018
Jackson, P. A., Widen, J. C., Harki, D. A. & Brummond, K. M. Covalent modifiers: a chemical perspective on the reactivity of α,β-unsaturated carbonyls with thiols via hetero-Michael addition reactions. J. Med. Chem. 60, 839–885 (2017).
doi: 10.1021/acs.jmedchem.6b00788
Nichols, R. J. et al. RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers. Nat. Cell Biol. 20, 1064–1073 (2018).
doi: 10.1038/s41556-018-0169-1
Robert, C. et al. Improved overall survival in melanoma with combined dabrafenib and trametinib. N. Engl. J. Med. 372, 30–39 (2015).
doi: 10.1056/NEJMoa1412690
Saiki, A. Y. et al. MDM2 antagonists synergize broadly and robustly with compounds targeting fundamental oncogenic signaling pathways. Oncotarget 5, 2030–2043 (2014).
doi: 10.18632/oncotarget.1918
Ebert, P. J. R. et al. MAP kinase inhibition promotes T cell and anti-tumor activity in combination with PD-L1 checkpoint blockade. Immunity 44, 609–621 (2016).
doi: 10.1016/j.immuni.2016.01.024
Selby, M. J. et al. Preclinical development of ipilimumab and nivolumab combination immunotherapy: mouse tumor models, in vitro functional studies, and cynomolgus macaque toxicology. PLoS ONE 11, e0161779 (2016).
doi: 10.1371/journal.pone.0161779
Mosely, S. I. et al. Rational selection of syngeneic preclinical tumor models for immunotherapeutic drug discovery. Cancer Immunol. Res. 5, 29–41 (2017).
doi: 10.1158/2326-6066.CIR-16-0114
Spranger, S., Dai, D., Horton, B. & Gajewski, T. F. Tumor-residing Batf3 dendritic cells are required for effector T cell trafficking and adoptive T cell therapy. Cancer Cell 31, 711–723 (2017).
doi: 10.1016/j.ccell.2017.04.003
Gao, Q. et al. Cancer-cell-secreted CXCL11 promoted CD8
doi: 10.1186/s40425-019-0511-6
Lee, J. W. et al. The combination of MEK inhibitor with immunomodulatory antibodies targeting programmed death 1 and programmed death ligand 1 results in prolonged survival in Kras/p53-driven lung cancer. Journal Thorac. Oncol. 14, 1046–1060 (2019).
doi: 10.1016/j.jtho.2019.02.004
Liu, L. et al. The BRAF and MEK inhibitors Dabrafenib and Trametinib: Effects on Immune Function and in Combination with Immunomodulatory antibodies targeting PD-1, PD-L1, and CTLA-4. Clin. Cancer Res. 21, 1639–1651 (2015).
doi: 10.1158/1078-0432.CCR-14-2339
Kordiak, J. et al. Intratumor heterogeneity and tissue distribution of KRAS mutation in non-small cell lung cancer: implications for detection of mutated KRAS oncogene in exhaled breath condensate. J. Cancer Res. Clin. Oncol. 145, 241–251 (2019).
doi: 10.1007/s00432-018-2779-1
Lamy, A. et al. Metastatic colorectal cancer KRAS genotyping in routine practice: results and pitfalls. Mod. Pathol. 24, 1090–1100 (2011).
doi: 10.1038/modpathol.2011.60
Richman, S. D. et al. Intra-tumoral heterogeneity of KRAS and BRAF mutation status in patients with advanced colorectal cancer (aCRC) and cost-effectiveness of multiple sample testing. Anal. Cell. Pathol. 34, 61–66 (2011).
doi: 10.1155/2011/393521

Auteurs

Jude Canon (J)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA. jcanon@amgen.com.

Karen Rex (K)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Anne Y Saiki (AY)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Christopher Mohr (C)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Keegan Cooke (K)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Dhanashri Bagal (D)

Amgen Research, Amgen Inc, South San Francisco, CA, USA.

Kevin Gaida (K)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Tyler Holt (T)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Charles G Knutson (CG)

Amgen Research, Amgen Inc, Cambridge, MA, USA.

Neelima Koppada (N)

Amgen Research, Amgen Inc, Cambridge, MA, USA.

Brian A Lanman (BA)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Jonathan Werner (J)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Aaron S Rapaport (AS)

Amgen Research, Amgen Inc, South San Francisco, CA, USA.

Tisha San Miguel (T)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Roberto Ortiz (R)

Amgen Research, Amgen Inc, Cambridge, MA, USA.
Pfizer, La Jolla, CA, USA.

Tao Osgood (T)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Ji-Rong Sun (JR)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Xiaochun Zhu (X)

Amgen Research, Amgen Inc, Cambridge, MA, USA.
Takeda, Cambridge, MA, USA.

John D McCarter (JD)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

Laurie P Volak (LP)

Amgen Research, Amgen Inc, Cambridge, MA, USA.
Celgene, San Diego, CA, USA.

Brett E Houk (BE)

Amgen Clinical Development, Amgen Inc, Thousand Oaks, CA, USA.

Marwan G Fakih (MG)

City of Hope, Duarte, CA, USA.

Bert H O'Neil (BH)

Indiana University School of Medicine, Indianapolis, IN, USA.

Timothy J Price (TJ)

The Queen Elizabeth Hospital, Woodville, South Australia, Australia.
University of Adelaide, Adelaide, South Australia, Australia.

Gerald S Falchook (GS)

Sarah Cannon Research Institute, Denver, CO, USA.

Jayesh Desai (J)

Peter MacCallum Cancer Center, Melbourne, Victoria, Australia.

James Kuo (J)

Scientia Clinical Research, Randwick, New South Wales, Australia.

Ramaswamy Govindan (R)

Washington University School of Medicine, St Louis, MO, USA.

David S Hong (DS)

The University of Texas MD Anderson Cancer Center, Houston, TX, USA.

Wenjun Ouyang (W)

Amgen Research, Amgen Inc, South San Francisco, CA, USA.

Haby Henary (H)

Amgen Clinical Development, Amgen Inc, Thousand Oaks, CA, USA.

Tara Arvedson (T)

Amgen Research, Amgen Inc, South San Francisco, CA, USA.

Victor J Cee (VJ)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA.

J Russell Lipford (JR)

Amgen Research, Amgen Inc, Thousand Oaks, CA, USA. jlipford@amgen.com.

Articles similaires

[Redispensing of expensive oral anticancer medicines: a practical application].

Lisanne N van Merendonk, Kübra Akgöl, Bastiaan Nuijen
1.00
Humans Antineoplastic Agents Administration, Oral Drug Costs Counterfeit Drugs

Smoking Cessation and Incident Cardiovascular Disease.

Jun Hwan Cho, Seung Yong Shin, Hoseob Kim et al.
1.00
Humans Male Smoking Cessation Cardiovascular Diseases Female
Humans United States Aged Cross-Sectional Studies Medicare Part C
1.00
Humans Yoga Low Back Pain Female Male

Classifications MeSH