A First-Time-in-Human Study of GSK2636771, a Phosphoinositide 3 Kinase Beta-Selective Inhibitor, in Patients with Advanced Solid Tumors.

@article{Mateo2017AFS,
  title={A First-Time-in-Human Study of GSK2636771, a Phosphoinositide 3 Kinase Beta-Selective Inhibitor, in Patients with Advanced Solid Tumors.},
  author={Joaqu{\'i}n Ezpeleta Mateo and Gopinath Ganji and Charlotte R. Lemech and Howard A. Burris and Songjun Han and Karen Elizabeth. Swales and Shaun Decordova and M Phillip Deyoung and Deborah Anne Smith and Shanker Kalyana-Sundaram and Jiuhua Wu and Monica Motwani and Rakesh Kumar and Jerry M. Tolson and Sun Young Rha and Hyun Cheol Chung and Joseph Paul Eder and Sunil Dutta Sharma and Yung-Jue Bang and Jeffrey R. Infante and Li Yan and Johann S de Bono and Hendrik-Tobias Arkenau},
  journal={Clinical cancer research : an official journal of the American Association for Cancer Research},
  year={2017},
  volume={23 19},
  pages={
          5981-5992
        }
}
Background: The PI3K/protein kinase B (AKT) pathway is commonly activated in several tumor types. Selective targeting of p110β could result in successful pathway inhibition while avoiding the on- and off-target effects of pan-PI3K inhibitors. GSK2636771 is a potent, orally bioavailable, adenosine triphosphate-competitive, selective inhibitor of PI3Kβ.Methods: We evaluated the safety, pharmacokinetics, pharmacodynamics and antitumor activity of GSK2636771 to define the recommended phase II dose… CONTINUE READING
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