LY3962673, an oral, highly potent, mutant-selective, and non-covalent KRAS G12D inhibitor demonstrates robust anti-tumor activity in KRAS G12D models

被引:1
|
作者
Gong, Xueqian
Gao, Hong
Bender, Mark H.
Ming, Wenyu
Zhang, Youyan
Stewart, Trent R.
Yu, Chun Ping
Xu, Wei Guo
You, Aurthur Xintian
Bian, Wen Ting
Li, Binghui
Wang, Tao
Bian, Huimin
Tandon, Manuj
Capen, Andrew
Cavitt, Rachel N.
Anderson, Bryan D.
Bocchinfuso, Wayne
Klippel, Anke
Iyer, Chandrasekar
机构
关键词
D O I
10.1158/1538-7445.AM2024-3316
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
3316
引用
收藏
页数:2
相关论文
共 50 条
  • [1] Preclinical characterization of LY3962673, an orally bioavailable, highly potent, and selective KRAS G12D inhibitor
    Iyer, Chandrasekar
    Li, Binghui
    Stewart, Trent R.
    Wang, Tao
    Capen, Andrew
    Cavitt, Rachel
    Anderson, Bryan D.
    Bocchinfuso, Wayne
    Zhao, Gaiying
    Rodriguez, Michael J.
    Carballares, Santiago
    Cooke, Andrew
    Bondi, Robert
    Burns, Lee
    Kelamangalath, Lakshmi
    Wallace, Ross
    Kolakowski, Gabrielle
    Henry, James R.
    Si, Chong
    MOLECULAR CANCER THERAPEUTICS, 2023, 22 (12)
  • [2] MOONRAY-01, a phase 1 study of LY3962673, a potent, orally bioavailable, and selective KRAS G12D inhibitor in KRAS G12D-mutant solid tumors
    Lakhani, Nehal J.
    Melisi, Davide
    Subbiah, Vivek
    Ammakkanavar, Natraj Reddy
    O'Reilly, Eileen M.
    Cassier, Philippe Alexandre
    Wainberg, Zev A.
    Duffy, Austin G.
    Patnaik, Amita
    Fujiwara, Yutaka
    Oberstein, Paul Eliezer
    Garcia-Carbonero, Rocio
    Wright, Jennifer
    Lin, Aimee K.
    Li, Jian
    Axelson, Michael D.
    Garrido-Laguna, Ignacio
    JOURNAL OF CLINICAL ONCOLOGY, 2025, 43 (4_SUPPL) : TPS845 - TPS845
  • [3] INCB161734: A novel, potent, and orally bioavailable KRAS G12D selective inhibitor demonstrates antitumor activity in KRAS G12D mutant tumors
    Farren, Matthew R.
    Roman, Valerie
    Gallion, Alexandra
    Allali-Hassani, Abdellah
    Sokolsky, Alexander
    Kong, Weixi
    Smith, Amanda
    Wang, Hui
    Correa, Gina
    Deller, Marc
    Epling, Leslie B.
    Procak, Jessica
    Zhang, Guofeng
    Pecko, Katherine
    Kennedy, Keith
    Boer, Jason
    Kurzeja-Lipinski, Kerri
    Covington, Maryanne
    Chen, Kwang-Jong
    Wallower, Renee
    Rocha, Jennifer
    Pan, Rina
    Perry, Anthony
    Yuska, Brad
    Wang, Xiaozhao
    Macarron, Ricardo
    Kim, Sunkyu
    CANCER RESEARCH, 2024, 84 (06)
  • [4] Exploring the switch II pocket of KRAS(G12D) with mutant-selective monobody inhibitors
    Hattori, Takamitsu
    Akkapeddi, Padma
    Khan, Imran
    Koide, Akiko
    Glasser, Eliezra
    Ketavarapu, Gayatri
    Whaby, Michael
    Zuberi, Mariyam
    Teng, Kai Wen
    Lefler, Julia
    Maso, Lorenzo
    Bang, Injin
    Ostrowski, Michael C.
    O'Bryan, John P.
    Koide, Shohei
    MOLECULAR CANCER RESEARCH, 2023, 21 (05)
  • [5] ASP3082, a First-in-class novel KRAS G12D degrader, exhibits remarkable anti-tumor activity in KRAS G12D mutated cancer models
    Nagashima, T.
    Inamura, K.
    Nishizono, Y.
    Suzuki, A.
    Tanaka, H.
    Yoshinari, T.
    Yamanaka, Y.
    EUROPEAN JOURNAL OF CANCER, 2022, 174 : S30 - S30
  • [6] GFH375 (VS-7375): An oral, selective KRAS G12D (ON/ OFF) inhibitor with potent anti-tumor efficacy
    Yan, Feng
    Jiang, Tao
    Liang, Tao
    Cai, Lijian
    Zhang, Leitao
    Xu, Xiaoming
    Zhao, Yanhui
    Lan, Xiaoling
    Zhang, Xiaohui
    Liu, Meng
    Liu, Qiang
    Gao, Jinting
    Xie, Fubo
    Gao, Xueyan
    Wang, Li
    Zhang, Jingyang
    Ren, Hongcan
    Liu, Dong
    Le, Siyuan
    Tang, Lili
    Coma, Silvia
    Cheng, Yaofeng
    Sanburn, Nathan
    Pachter, Jonathan A.
    Zhou, Fusheng
    Lan, Jiong
    Lu, Qiang
    CANCER RESEARCH, 2024, 84 (06)
  • [7] Mutant-selective, covalent inhibitors of K-Ras(G12D)
    Zheng, Qinheng
    Zhang, Ziyang
    Guiley, Keelan
    Shokat, Kevan
    CANCER RESEARCH, 2024, 84 (02)
  • [8] Discovery of SHR1127, an orally bioavailable, highly potent and selective KRAS G12D inhibitor
    Li, Xin
    Shen, Feng
    Zhang, Limin
    Wang, Wei
    Kong, Luyao
    Bao, Yong
    Mao, Yuchang
    Wang, Zaiyong
    Lin, Sophie
    Zhang, Zhe
    Feng, Jun
    Hu, Min
    He, Feng
    CANCER RESEARCH, 2024, 84 (06)
  • [9] ALTA3263: an oral, KRAS isoform-selective, dual ON/OFF state, non-covalent inhibitor induces regressions across KRAS G12V, G12D, and G12C cancer models
    Wang, T.
    Ibanez, M.
    Yu, K.
    Fan, K.
    Juan, J.
    Perez, M.
    Smith, T.
    Walsh, B.
    Kang, V.
    Tyhonas, J.
    Alvarez, N.
    Tran, J.
    Moorefield, K. S.
    Phimister, A.
    Zhu, X.
    Chi, A.
    Bartberger, M. D.
    Murphy, E.
    EUROPEAN JOURNAL OF CANCER, 2024, 211 : S5 - S6
  • [10] Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors
    Cheng, Hengmiao
    Li, Puhui
    Chen, Ping
    Irimia, Adriana
    Bae, Jae Hyun
    Brooun, Alexei
    Fagan, Patrick
    Lam, Richard
    Lin, Bingzhen
    Zhang, Jingchuan
    Zhan, Xuejun
    Wu, Xu
    Xie, Nan
    Chiang, Gary
    Shoemaker, Robert
    Vernier, Jean-Michel
    ACS MEDICINAL CHEMISTRY LETTERS, 2023, 14 (10): : 1351 - 1357