TAS-116, a Novel, Orally Bioavailable HSP90a/β Selective Inhibitor Demonstrates Highly Potent Antitumor Activity in Preclinical Models with a Favorable PK Profile

被引:3
|
作者
Ohkubo, S. [1 ]
Muraoka, H. [1 ]
Hashimoto, A. [1 ]
Ito, S. [1 ]
Ito, K. [1 ]
Shibata, Y. [1 ]
Kanoh, A. [1 ]
Kitade, M. [1 ]
Yonekura, K. [1 ]
Utsugi, T. [1 ]
机构
[1] Taiho Pharmaceut Co LTD, Tsukuba Res Ctr, Tsukuba, Ibaraki, Japan
关键词
D O I
10.1016/S0959-8049(12)72089-0
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
291
引用
收藏
页码:89 / 89
页数:1
相关论文
共 50 条
  • [41] DS-1062a, a novel TROP2-targeting antibody-drug conjugate with a novel DNA topoisomerase I inhibitor DXd, demonstrates potent antitumor activity in preclinical models
    Okajima, Daisuke
    Yamaguchi, Junko
    Kitamura, Michiko
    Kamei, Reiko
    Maejima, Takanori
    Shibutani, Tomoko
    Yasuda, Satoru
    Toki, Tadashi
    Karibe, Tsuyoshi
    Fujitani, Tomomichi
    Nakada, Takashi
    Goto, Riki
    Noguchi, Yutaka
    Abe, Yuki
    Agatsuma, Toshinori
    MOLECULAR CANCER THERAPEUTICS, 2019, 18 (12)
  • [42] DS-6000a, a novel CDH6-targeting antibody-drug conjugate with a novel DNA topoisomerase I inhibitor DXd, demonstrates potent antitumor activity in preclinical models
    Suzuki, H.
    Nagase, S.
    Saito, C.
    Nagata, M.
    Kaneda, Y.
    Honda, K.
    Nishiya, Y.
    Honda, T.
    Nakada, T.
    Goto, R.
    Ishizaka, T.
    Myobatake, Y.
    Abe, Y.
    Agatsuma, T.
    ANNALS OF ONCOLOGY, 2021, 32 : S363 - S364
  • [43] CEP-7055: A novel, orally active pan inhibitor of vascular endothelial growth factor receptor tyrosine kinases with potent antiangiogenic activity and antitumor efficacy in preclinical models
    Ruggeri, B
    Singh, J
    Gingrich, D
    Angeles, T
    Albom, M
    Chang, H
    Robinson, C
    Hunter, K
    Dobrzanski, P
    Jones-Bolin, S
    Aimone, L
    Klein-Szanto, A
    Herbert, JM
    Bono, F
    Schaeffer, P
    Casellas, P
    Bourie, B
    Pili, R
    Isaacs, J
    Ator, M
    Hudkins, R
    Vaught, J
    Mallamo, J
    Dionne, C
    CANCER RESEARCH, 2003, 63 (18) : 5978 - 5991
  • [44] Discovery of a novel and highly selective CDK9 kinase inhibitor (JS']JSH-009) with potent antitumor efficacy in preclinical acute myeloid leukemia models
    Wang, Li
    Hu, Chen
    Wang, Aoli
    Chen, Cheng
    Wu, Jiaxin
    Jiang, Zongru
    Zou, Fengming
    Yu, Kailin
    Wu, Hong
    Liu, Juan
    Wang, Wenliang
    Wang, Zuowei
    Wang, Beilei
    Qi, Ziping
    Liu, Qingwang
    Wang, Wenchao
    Li, Lili
    Ge, Jian
    Liu, Jing
    Liu, Qingsong
    INVESTIGATIONAL NEW DRUGS, 2020, 38 (05) : 1272 - 1281
  • [45] RMC-5127, a first-in-class, orally bioavailable mutant- selective RASG12V( ON) inhibitor is central nervous system (CNS)-penetrant and demonstrates antitumor activity in a preclinical intracranial xenograft model
    Chen, Zhe
    Eriksson, Andre
    Lee, Bianca
    Dinglasan, Jay
    Montazer, Nilufar
    Cregg, Jim
    Edwards, Anne
    Sanders, Kate
    Smith, Jacqueline A.
    Wildes, David
    Singh, Mallika
    Wang, Zhican
    Jiang, Jingjing
    CANCER RESEARCH, 2024, 84 (06)
  • [46] BLU-222, a potent and highly selective CDK2 inhibitor, demonstrates antitumor activity as monotherapy and as combination treatment in CCNE1-aberrant endometrial cancer models
    House, Nealia
    Brown, Victoria
    Yuan, Liang
    Chen, Maxine
    Lee, Stephanie
    Wu, Rentian
    Muthuswamy, Lakshmi
    Ribich, Scott
    Ramsden, Philip
    Faia, Kerrie
    CANCER RESEARCH, 2024, 84 (06)
  • [47] JDQ443, a covalent irreversible inhibitor of KRAS G12C, exhibits a novel binding mode and demonstrates potent anti-tumor activity and favorable pharmacokinetic properties in preclinical models
    Brachmann, Saskia M.
    Weiss, Andreas
    Guthy, Daniel A.
    Beyer, Kim
    Voshol, Johannes
    Maira, Michel
    Prahallad, Anirudh
    Porta, Diana Graus
    Schnell, Christian
    Ostermann, Nils
    Vaupel, Andrea
    Gerspacher, Marc
    Leblanc, Catherine
    Erdmann, Dirk
    Sterker, Dario
    Kerr, Grainne
    Jerome, Giovannoni
    Head, Victoria
    Stringer, Rowan
    De Kanter, Ruben
    Jeff, Kearns
    Roman, Danielle
    Widmer, Toni
    Wessels, Peter
    Nunez, Eloisa Jimenez
    Sedrani, Richard
    Zecri, Frederic
    Hofmann, Francesco
    Engleman, Jeff
    Lorthiois, Edwige
    Cotesta, Simona
    MOLECULAR CANCER THERAPEUTICS, 2021, 20 (12)
  • [48] SY-5609, a highly potent and selective oral CDK7 inhibitor, exhibits robust antitumor activity in preclinical models of KRAS mutant cancers as a single agent and in combination with chemotherapy
    Henry, S. H.
    Johannessen, L.
    Sawant, P.
    Lefkovith, A.
    Ke, N.
    Dworakowski, W.
    Hodgson, G.
    ANNALS OF ONCOLOGY, 2021, 32 : S364 - S364
  • [49] Characterization of a novel, orally bioavailable, potent and highly selective small molecule inhibitor of PERK: A tool to probe the biphasic concentration-dependent induction of ER stress in models of multiple myeloma and B-cell lymphoma
    Stansfield, Ian
    Ligny, Yannick
    Simonnet, Yvan
    Demestre, Christophe
    Amblard, Nathalie
    Meyer, Christophe
    Geerts, Tamara
    Van de Ven, Jeroen
    Van den Wyngaert, Ilse
    Vermeulen, Peter
    Beerden, Inge
    Peeters, Danielle
    Liebregts, Johnny
    Van Baelen, Kurt
    Simillion, Cedric
    Janssen, Boudewijn
    Verhulst, Tinne
    Esser, Norbert
    Bischoff, James
    Meerpoel, Lieven
    Versele, Matthias
    CANCER RESEARCH, 2014, 74 (19)
  • [50] TAS0612, a novel and highly potent RSK, AKT, and S6K inhibitor, exhibited strong antitumor effect in preclinical tumor models with deregulated RAS and PI3K pathway activities
    Ichikawa, K.
    Ito, S.
    Machida, T.
    Kato, E.
    Yamada, M.
    Fujita, R.
    Nakatsuru, Y.
    Saito, H.
    Tanaka, G.
    Wakayama, K.
    Jona, H.
    Sugimoto, T.
    Matsuo, K.
    Miyadera, K.
    Utsugi, T.
    Iwasawa, Y.
    EUROPEAN JOURNAL OF CANCER, 2018, 103 : E139 - E140