JZP815, a potent and selective pan-RAF inhibitor, demonstrates efficacy in RAF and RAS mutant tumor pre-clinical models

被引：0
|
作者：
Hauptschein, Robert [1 ]
Woodcock, Simon [2 ]
Belfield, Andrew [2 ]
Mason, Helen [2 ]
Keppel, Dorottya [2 ]
Markova, Svetlana [1 ]
Kim, Kyuri [1 ]
Roller, Shane [1 ]
Phillips, Caroline [2 ]
Jones, Clifford D. [2 ]
Humphreys, Robin C. [1 ]
机构：
[1] Jazz Pharmaceut, Palo Alto, CA USA
[2] Redx Pharma, Manchester, Lancs, England
来源：
CANCER RESEARCH | 2022年 / 82卷 / 12期
关键词：
D O I：
暂无
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
2677
引用
收藏
页数：1
相关论文
共 50 条
  • [1] A selective and potent pan-RAF inhibitor, HM95573 exhibits high therapeutic potential as a next-generation RAF inhibitor by direct inhibition of RAF kinase activity in BRAF or RAS mutant cancers
    Namgoong, G.
    Kim, S. H.
    Song, T. H.
    Bae, I. H.
    Ahn, Y. G.
    Lee, J. H.
    Choi, K.
    Lee, K. H.
    Kim, Y. H.
    Lee, Y. M.
    Suh, K. H.
    EUROPEAN JOURNAL OF CANCER, 2016, 69 : S127 - S127
  • [2] Antitumor activity of KIN-2787, a next-generation pan-RAF inhibitor, in preclinical models of human RAF/RAS mutant melanoma
    Miller, Nichol L. G.
    Wang, Tim S.
    Severson, Paul
    Jiang, Ping
    Perez, Michelle
    Timple, Noel
    Kanouni, Toufike
    Franovic, Aleksandra
    Martin, Eric S.
    Murphy, Eric
    CANCER RESEARCH, 2022, 82 (12)
  • [3] Discovery of a novel pan-RAF inhibitor with potent anti-tumor activity in preclinical models of BRAFV600E mutant cancer
    Hong, Sung Pyo
    Ahn, Soon Kil
    LIFE SCIENCES, 2017, 183 : 37 - 44
  • [4] Exarafenib (KIN-2787) is a potent, selective pan-RAF inhibitor with activity in preclinical models of BRAF class II/III mutant and NRAS mutant melanoma
    Wang, Tim S.
    Lee, Catherine
    Severson, Paul
    Pelham, Robert J.
    Williams, Richard
    Miller, Nichol L. G.
    CANCER RESEARCH, 2023, 83 (07)
  • [5] Development of a dual inhibitor of pan-RAF and angiogenesis for the treatment of metastatic colorectal cancer with mutant K-RAS
    Hong, Sungpyo
    Choi, Younghoon
    Kwon, Ho-Seok
    Park, Yong Bin
    Ki, Min-Hyo
    Shin, Hee Jong
    Lee, Michael
    Ahn, Soon Kil
    CANCER RESEARCH, 2017, 77
  • [6] Discovery of TAK-632: A selective kinase inhibitor of pan-RAF with potent antitumor activity against BRAF and NRAS mutant melanomas
    Okaniwa, Masanori
    Hirose, Masaaki
    Arita, Takeo
    Yabuki, Masato
    Nakamura, Akita
    Takagi, Terufumi
    Kawamoto, Tomohiro
    Uchiyama, Noriko
    Sumita, Akihiko
    Tsutsumi, Shunichirou
    Tottori, Tsuneaki
    Inui, Yoshitaka
    Sang, Bi-Ching
    Yano, Jason
    Aertgeerts, Kathleen
    Yoshida, Sei
    Ishikawa, Tomoyasu
    MOLECULAR CANCER THERAPEUTICS, 2013, 12 (11)
  • [7] Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF
    Shao, Wenlin
    Mishina, Yuji M.
    Feng, Yun
    Caponigro, Giordano
    Cooke, Vesselina G.
    Rivera, Stacy
    Wang, Yingyun
    Shen, Fang
    Korn, Joshua M.
    Griner, Lesley A. Mathews
    Nishiguchi, Gisele
    Rico, Alice
    Tellew, John
    Haling, Jacob R.
    Aversa, Robert
    Polyakov, Valery
    Zang, Richard
    Hekmat-Nejad, Mohammad
    Amiri, Payman
    Singh, Mallika
    Keen, Nicholas
    Dillon, Michael P.
    Lees, Emma
    Ramurthy, Savithri
    Sellers, William R.
    Stuart, Darrin D.
    CANCER RESEARCH, 2018, 78 (06) : 1537 - 1548
  • [8] Development of a dual inhibitor of pan-RAF and VEGFR2 for the treatment of metastatic colorectal cancer with mutant K-RAS
    Hong, Sungpyo
    Choi, Young-Il
    Choi, Jihye
    Kim, Wonyoung
    Kwon, Ho-Seok
    Park, Yong Bin
    Ki, Min-Hyo
    Shin, Hee Jong
    Lee, Michael
    Ahn, Soon Kil
    CANCER RESEARCH, 2016, 76
  • [9] Development of REDX05358, a novel highly selective and potent pan RAF inhibitor and a potential therapeutic for BRAF and RAS mutant tumors
    Mason, Helen
    Scrace, Simon
    Testar, Richard
    Rainard, Julie
    Talab, Fatima
    Poonawala, Ryaka
    Smith, Philippa
    Brooke, Harriet
    Frith, Sarah
    Ahmet, Jonathan
    Hall, Jonathan
    Sorrell, David
    Moore, Jon
    Phillips, Caroline
    France, Dennis
    Bingham, Matilda
    Armer, Richard
    CANCER RESEARCH, 2017, 77
  • [10] XL518, a potent selective orally bioavailable MEK1 inhibitor, downregulates the RAS/RAF/MEK/ERK pathway in vivo, resulting in tumor growth inhibition and regression in pre-clinical models
    Johnston, Stuart
    MOLECULAR CANCER THERAPEUTICS, 2007, 6 (12) : 3595S - 3595S
12345