PRECLINICAL DEVELOPMENT OF THE PI3K ALPHA SELECTIVE AND PIK3CA MUTANT SELECTIVE INHIBITOR GDC-0077 AND PREDICTION OF ITS HUMAN PHARMACOKINETICS

被引：0
|
作者：
Pang, Jodie [1 ]
Baumgardner, Matthew [1 ]
Braun, Marie-Gabrielle [1 ]
Cheong, Jonathan [1 ]
Edgar, Kyle [1 ]
Friedman, Lori [1 ]
Hanan, Emily [1 ]
Jaochico, Allan [1 ]
Ma, Shuguang [1 ]
Plise, Emile [1 ]
Schmidt, Stephen [1 ]
Liu, Ning [1 ]
Song, Kyung [1 ]
Staben, Steve [1 ]
Salphati, Laurent [1 ]
机构：
[1] Genentech Inc, San Francisco, CA USA
来源：
DRUG METABOLISM AND PHARMACOKINETICS | 2019年 / 34卷 / 01期
关键词：
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
P56
引用
收藏
页码：S37 / S37
页数：1
相关论文
共 50 条
  • [21] The Selective Class I PI3K Inhibitor CH5132799 Targets Human Cancers Harboring Oncogenic PIK3CA Mutations
    Tanaka, Hiroshi
    Yoshida, Miyuki
    Tanimura, Hiromi
    Fujii, Toshihiko
    Sakata, Kiyoaki
    Tachibana, Yukako
    Ohwada, Jun
    Ebiike, Hirosato
    Kuramoto, Shino
    Morita, Keiichi
    Yoshimura, Yasushi
    Yamazaki, Toshikazu
    Ishii, Nobuya
    Kondoh, Osamu
    Aoki, Yuko
    CLINICAL CANCER RESEARCH, 2011, 17 (10) : 3272 - 3281
  • [22] The PI3K inhibitor, taselisib (GDC-0032), has enhanced potency in PIK3CA mutant models through a unique mechanism of action
    Edgar, Kyle A.
    Song, Kyung
    Schmidt, Stephen
    Kirkpatrick, Don
    Phu, Lilian
    Nannini, Michelle
    Hong, Rebecca
    Cheng, Eric
    Young, Amy
    Sampath, Deepak
    Friedman, Lori S.
    CANCER RESEARCH, 2016, 76
  • [23] Dual PI3K/mTOR inhibition in PIK3CA mutant pancreatic cancers
    Payne, Susan
    Depke, Mitchell
    Yueh, Alex
    Sharick, Joseph T.
    Favreau, Peter F.
    Pasch, Cheri A.
    Clipson, Linda
    Matkowskyj, Kristina A.
    Skala, Melissa
    Deming, Dustin A.
    CANCER RESEARCH, 2018, 78 (13)
  • [24] Discovery of AZD8835, a potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of PIK3CA-dependent cancers
    Barlaam, Bernard
    Cosulich, Sabina
    Delouvrie, Benedicte
    Fitzek, Martina
    Germain, Herve
    Green, Stephen
    Harris, Craig S.
    Hudson, Kevin
    Lambert-van der Brempt, Christine
    Lamorlette, Maryannick
    Antoine, Le Griffon
    Morgentin, Remy
    Ouvry, Gilles
    Page, Ken
    Pasquet, Georges
    Ruston, Linette
    Saleh, Twana
    Vautier, Michel
    Ward, Lara
    CANCER RESEARCH, 2015, 75
  • [25] Differential response to a dual PI3K/mTOR inhibitor in PIK3CA mutant urothelial cancer patient derived xenografts
    Elbanna, May F.
    Ciamporcero, Eric
    Adelaiye, Remi
    Orillion, Ashley
    Chintala, Sreenivasulu
    Pili, Roberto
    CANCER RESEARCH, 2016, 76
  • [26] The PI3K inhibitor, taselisib, has a unique mechanism of action that leads to enhanced potency in PIK3CA mutant models
    Song, Kyung W.
    Edgar, Kyle A.
    Kirkpatrick, Donald S.
    Phu, Lilian
    Schmidt, Stephen
    Nannini, Michelle
    Hong, Rebecca
    Cheng, Eric
    Crocker, Lisa
    Young, Amy
    Sampath, Deepak
    Friedman, Lori
    CANCER RESEARCH, 2017, 77
  • [27] The PI3K inhibitor, taselisib, has enhanced potency in PIK3CA mutant models through a unique mechanism of action
    Friedman, L. S.
    Edgar, K. A.
    Song, K.
    Schmidt, S.
    Kirkpatrick, D. S.
    Phu, L.
    Nannini, M. A.
    Hong, R.
    Cheng, E.
    Crocker, L.
    Young, A.
    Sampath, D.
    CANCER RESEARCH, 2017, 77
  • [28] Phase I Basket Study of Taselisib, an Isoform-Selective PI3K Inhibitor, in Patients with PIK3CA-Mutant Cancers
    Jhaveri, Komal
    Chang, Matthew T.
    Juric, Dejan
    Saura, Cristina
    Gambardella, Valentina
    Melnyk, Anton
    Patel, Manish R.
    Ribrag, Vincent
    Ma, Cynthia X.
    Aljumaily, Raid
    Bedard, Philippe L.
    Sachdev, Jasgit C.
    Dunn, Lara
    Won, Helen
    Bond, John
    Jones, Surai
    Savage, Heidi M.
    Scaltriti, Maurizio
    Wilson, Timothy R.
    Wei, Michael C.
    Hyman, David M.
    CLINICAL CANCER RESEARCH, 2021, 27 (02) : 447 - 459
  • [29] Effective use of PI3K inhibitor BKM120 and PARP inhibitor Olaparib to treat PIK3CA mutant ovarian cancer
    Wang, Dong
    Wang, Min
    Jiang, Nan
    Zhang, Yuan
    Bian, Xing
    Wang, Xiaoqing
    Roberts, Thomas M.
    Zhao, Jean J.
    Liu, Pixu
    Cheng, Hailing
    ONCOTARGET, 2016, 7 (11) : 13153 - 13166
  • [30] Men1611 is a pi3k α/β selective and δ sparing inhibitor with long-lasting antitumor activity in different genetic backgrounds of pik3ca mutant breast cancer models
    Fiascarelli, Alessio
    Carrisi, Corrado
    Merlino, Giuseppe
    Capano, Stefania
    Bisignano, Diego
    Talucci, Simone
    Bressan, Alessandro
    Bellarosa, Daniele
    Bigioni, Mario
    Scaltriti, Maurizio
    Arribas, Joaquin
    Pellacani, Andrea
    Salerno, Massimiliano
    Binaschi, Monica
    CANCER RESEARCH, 2021, 81 (04)
12345