RMC-9805, a first-in-class, mutant-selective, covalent and oral KRASG12D(ON) inhibitor that induces apoptosis and drives tumor regression in preclinical models of KRASG12D cancers

被引：22
|
作者：
Jiang, Lingyan
Menard, Marie
Weller, Caroline
Wang, Zhican
Burnett, Les
Aronchik, Ida
Steele, Shelby
Flagella, Mike
Zhao, Ruiping
Evans, James W. W.
Chin, Shook
Chou, Kang-Jye
Mu, Yunming
Longhi, Michael
McDowell, Laura
Knox, John E.
Gill, Adrian
Smith, Jacqueline A.
Singh, Mallika
Quintana, Elsa
Jiang, Jingjing
机构：
来源：
CANCER RESEARCH | 2023年 / 83卷 / 07期
关键词：
D O I：
10.1158/1538-7445.AM2023-526
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
526
引用
收藏
页数：3
相关论文
共 17 条
  • [1] Discovery of RMC-9805, an oral, covalent tri-complex KRASG12D(ON) inhibitor
    Knox, John E.
    Burnett, G. Leslie
    Weller, Caroline
    Jiang, Lingyan
    Zhang, Dongyu
    Vita, Nicole
    Marquez, Abby
    Seamon, Kyle J.
    Gould, Andrea
    Menard, Marie
    Quintana, Elsa
    Chen, Zhe
    Wang, Zhican
    Wang, Zhengping
    Koltun, Elena S.
    Singh, Malika
    Jiang, Jingjing
    Wildes, David
    Smith, Jacqueline A. M.
    Gill, Adrian L.
    CANCER RESEARCH, 2024, 84 (07)
  • [2] RMC-9805, a first-in-class, mutant-selective, covalent and orally bioavailable KRASG12D(ON) inhibitor, promotes cancer-associated neoantigen recognition and synergizes with immunotherapy in preclinical models
    Menard, Marie J.
    Chow, Christopher
    Chen, Kevin
    Blaj, Cristina
    Shifrin, Nataliya Tovbis
    Courtney, Haley
    Nasholm, Nicole M.
    Pham, Anna
    Kumamoto, Alice
    Ganesh, Swetha
    Evans, James W.
    Lawrence, Lindsey
    Vonmelchert, Brian
    Kwok-Parkhill, Amy C.
    Jiang, Jingjing
    Knox, John E.
    Smith, Jacqueline
    Quintana, Elsa
    CANCER RESEARCH, 2023, 83 (07)
  • [3] RM-036, a first-in-class, orally-bioavailable, Tri-Complex covalent KRASG12D(ON) inhibitor, drives profound anti-tumor activity in KRASG12D mutant tumor models
    Knox, John E.
    Jiang, Jingjing
    Burnett, G. Leslie
    Liu, Yang
    Weller, Caroline E.
    Wang, Zhican
    McDowell, Laura
    Steele, Shelby L.
    Chin, Shook
    Chou, Kang Jye
    Wang, Fang
    Zhong, Mengqi
    Koltun, Elena S.
    Wildes, David
    Singh, Mallika
    Gill, Adrian L.
    Smith, Jacqueline A.
    CANCER RESEARCH, 2022, 82 (12)
  • [4] Mutant-selective KRASG12D(ON) inhibitor suppresses proliferation in vitro and tumor growth in vivo of KrasG12D GEMM-derived PDAC organoids
    Labrecque, Mark P.
    Jiang, Lingyan
    Nasholm, Nicole
    Nayak, Biswadeep
    Yu, Xinxing
    Song, Avian
    Weller, Caroline
    Evans, James W.
    Zafra, Maria Paz
    Parsons, Marie
    Menard, Marie
    Dow, Lukas E.
    Jiang, Jingjing
    Aronchik, Ida
    Singh, Mallika
    CANCER RESEARCH, 2024, 84 (02)
  • [5] Activation of oncogenic KrasG12D induces oral tumor formation
    Caulin, C
    Lang, GA
    Lozano, G
    Roop, DR
    JOURNAL OF INVESTIGATIVE DERMATOLOGY, 2004, 122 (03) : A24 - A24
  • [6] Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor
    Hallin, Jill
    Bowcut, Vickie
    Calinisan, Andrew
    Briere, David M.
    Hargis, Lauren
    Engstrom, Lars D.
    Laguer, Jade
    Medwid, James
    Vanderpool, Darin
    Lifset, Ella
    Trinh, David
    Hoffman, Natalie
    Wang, Xiaolun
    Lawson, J. David
    Gunn, Robin J.
    Smith, Christopher R.
    Thomas, Nicole C.
    Martinson, Matthew
    Bergstrom, Alex
    Sullivan, Francis
    Bouhana, Karyn
    Winski, Shannon
    He, Leo
    Fernandez-Banet, Julio
    Pavlicek, Adam
    Haling, Jacob R.
    Rahbaek, Lisa
    Marx, Matthew A.
    Olson, Peter
    Christensen, James G.
    NATURE MEDICINE, 2022, 28 (10) : 2171 - 2182
  • [7] Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor
    Jill Hallin
    Vickie Bowcut
    Andrew Calinisan
    David M. Briere
    Lauren Hargis
    Lars D. Engstrom
    Jade Laguer
    James Medwid
    Darin Vanderpool
    Ella Lifset
    David Trinh
    Natalie Hoffman
    Xiaolun Wang
    J. David Lawson
    Robin J. Gunn
    Christopher R. Smith
    Nicole C. Thomas
    Matthew Martinson
    Alex Bergstrom
    Francis Sullivan
    Karyn Bouhana
    Shannon Winski
    Leo He
    Julio Fernandez-Banet
    Adam Pavlicek
    Jacob R. Haling
    Lisa Rahbaek
    Matthew A. Marx
    Peter Olson
    James G. Christensen
    Nature Medicine, 2022, 28 : 2171 - 2182
  • [8] Preclinical studies of TSN1611, a potent, selective, and orally bioavailable KRASG12D inhibitor
    Shang, Erchang
    Zhong, Boyu
    Zhang, Tony
    Dong, Chunlan
    Ma, Shengtang
    Yang, Anjiang
    Jia, Ziyang
    Zheng, Renjuan
    Li, Jing
    Fu, Han
    Lai, Liangbao
    CANCER RESEARCH, 2024, 84 (06)
  • [9] Discovery and characterization of QTX3046, a potent, selective, and orally bioavailable non-covalent KRASG12D inhibitor
    Vo, Elizabeth Donohue
    Zhang, Yang W.
    Rominger, Dave
    Silva, Jillian M.
    Zhang, Yang J.
    Lee, Greg
    Micozzi, John
    Reid, Ben
    McDonough, Brooke
    Hospital, Audrey
    Luengo, Juan I.
    Lin, Hong
    Pitt, Cameron
    CANCER RESEARCH, 2023, 83 (08)
  • [10] Direct targeting of KRASG12X mutant cancers with RMC-6236, a first-in-class, RAS-selective, orally bioavailable, tri-complex RASMULTI(ON) inhibitor
    Koltun, Elena S.
    Rice, Meghan A.
    Gustafson, W. Clay
    Wilds, David
    Jiang, Jingjing
    Lee, Bianca J.
    Wang, Zhengping
    Chang, Stephanie
    Flagella, Mike
    Mu, Yunming
    Dinglasan, Nuntana
    Nasholm, Nicole
    Evans, James W.
    Wang, Yingyun
    Seamon, Kyle
    Liu, Yang
    Blaj, Cristina
    Knox, John
    Freilich, Rebecca
    Quintana, Elsa
    Cregg, Jim
    Bermingham, Alun
    Gill, Adrian L.
    Smith, Jacqueline Am
    Singh, Mallika
    CANCER RESEARCH, 2022, 82 (12)
12