Advanced search
Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 41, 2011 - Issue 12
Submit an article Journal homepage
772
Views
20
CrossRef citations to date
0
Altmetric
Animal Pharmacokinetics and Metabolism

Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human

Laurent SalphatiDepartment of Drug Metabolism and Pharmacokinetics, Genentech, Inc., South San Francisco, USACorrespondence[email protected]
,
Jodie PangDepartment of Drug Metabolism and Pharmacokinetics, Genentech, Inc., South San Francisco, USA
,
Emile G. PliseDepartment of Drug Metabolism and Pharmacokinetics, Genentech, Inc., South San Francisco, USA
,
Bilin ChouDepartment of Drug Metabolism and Pharmacokinetics, Genentech, Inc., South San Francisco, USA
,
Jason S. HalladayDepartment of Drug Metabolism and Pharmacokinetics, Genentech, Inc., South San Francisco, USA
,
Alan G. OliveroDepartment of Chemistry, Genentech, Inc., South San Francisco, USA
,
Patrick J. RudewiczDepartment of Drug Metabolism and Pharmacokinetics, Genentech, Inc., South San Francisco, USA
,
Qingping TianDepartment of Small Molecule Process Chemistry, Genentech, Inc., South San Francisco, USA
,
Susan WongDepartment of Drug Metabolism and Pharmacokinetics, Genentech, Inc., South San Francisco, USA
&
Xiaolin ZhangDepartment of Drug Metabolism and Pharmacokinetics, Genentech, Inc., South San Francisco, USA
 show all
Pages 1088-1099 | Received 29 Apr 2011, Accepted 04 Jul 2011, Published online: 13 Aug 2011

Citations (20)

Keep up to date with the latest research on this topic with citation updates for this article.

Subscribe to citation updates

Read on this site (1)

Qin Yue, S. Cyrus Khojasteh, Sungjoon Cho, Shuguang Ma, Teresa Mulder, John Chen, Jodie Pang, Xiao Ding, Alan Deese, Jackson D. Pellet, Nicholas Siebers, Lori Joas, Laurent Salphati & Joseph A. Ware. (2021) Absorption, metabolism and excretion of pictilisib, a potent pan-class I phosphatidylinositol-3-Kinase (PI3K) inhibitor, in rats, dogs, and humans. Xenobiotica 51:7, pages 796-810.
Read now

Articles from other publishers (19)

Fangyao Hu, Sara F. Santagostino, Dimitry M. Danilenko, Min Tseng, Jochen Brumm, Philip Zehnder & Kai Connie Wu. (2022) Assessment of Skin Toxicity in an in Vitro Reconstituted Human Epidermis Model Using Deep Learning. The American Journal of Pathology 192:4, pages 687-700.
Crossref
Kyung W. Song, Kyle A. Edgar, Emily J. Hanan, Marc Hafner, Jason Oeh, Mark Merchant, Deepak Sampath, Michelle A. Nannini, Rebecca Hong, Lilian Phu, William F. Forrest, Eric Stawiski, Stephen Schmidt, Nicholas Endres, Jane Guan, Jeffrey J. Wallin, Jonathan Cheong, Emile G. Plise, Gail D. Lewis Phillips, Laurent Salphati, Timothy P. Heffron, Alan G. Olivero, Shiva Malek, Steven T. Staben, Donald S. Kirkpatrick, Anwesha Dey & Lori S. Friedman. (2022) RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy. Cancer Discovery 12:1, pages 204-219.
Crossref
Ricarda Ziegler, Fabian Häusermann, Stephan Kirchner & Liudmila Polonchuk. (2021) Cardiac Safety of Kinase Inhibitors – Improving Understanding and Prediction of Liabilities in Drug Discovery Using Human Stem Cell-Derived Models. Frontiers in Cardiovascular Medicine 8.
Crossref
David Olayinka Kamson, Harmon Singh Khela & John Laterra. 2021. Glioblastoma Resistance to Chemotherapy: Molecular Mechanisms and Innovative Reversal Strategies. Glioblastoma Resistance to Chemotherapy: Molecular Mechanisms and Innovative Reversal Strategies 31 77 .
Diren Beyoğlu & Jeffrey R. Idle. (2020) Metabolomic insights into the mode of action of natural products in the treatment of liver disease. Biochemical Pharmacology 180, pages 114171.
Crossref
Walaa I. El-Sofany, Dalia Ahmed A. Othman, Asma M. Mahran, El-Manawaty A. May & Wael A. El-Sayed. (2020) Synthesis and Anticancer Activity of Functionalized Thieno[2,3-d]pyrimidine Compounds and Their Triazinyl and Tetrazinyl Derivatives. Russian Journal of Bioorganic Chemistry 46:3, pages 393-402.
Crossref
Bouhari Altine, Yongkang Gai, Na Han, Yaqun Jiang, Hao Ji, Hanyi Fang, Alexandre Niyonkuru, Khamis Hassan Bakari, Maher Mohamad Rajab Arnous, Qingyao Liu, Yongxue Zhang & Xiaoli Lan. (2019) Preclinical Evaluation of a Fluorine-18 ( 18 F)-Labeled Phosphatidylinositol 3-Kinase Inhibitor for Breast Cancer Imaging . Molecular Pharmaceutics 16:11, pages 4563-4571.
Crossref
Eslam M.H. Ali, Mohammed S. Abdel-Maksoud & Chang-Hyun Oh. (2019) Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances. Bioorganic & Medicinal Chemistry 27:7, pages 1159-1194.
Crossref
Kelli M. Wilson, Lesley A. Mathews-Griner, Tara Williamson, Rajarshi Guha, Lu Chen, Paul Shinn, Crystal McKnight, Sam Michael, Carleen Klumpp-Thomas, Zev A. Binder, Marc Ferrer, Gary L. Gallia, Craig J. Thomas & Gregory J. Riggins. (2019) Mutation Profiles in Glioblastoma 3D Oncospheres Modulate Drug Efficacy. SLAS Technology 24:1, pages 28-40.
Crossref
Prashant B. Nigade, Jayasagar Gundu, K. Sreedhara Pai & Kumar V. S. Nemmani. (2017) Prediction of Tissue-to-Plasma Ratios of Basic Compounds in Mice. European Journal of Drug Metabolism and Pharmacokinetics 42:5, pages 835-847.
Crossref
Susan Heavey, Sinead Cuffe, Stephen Finn, Vincent Young, Ronan Ryan, Siobhan Nicholson, Niamh Leonard, Niall McVeigh, Martin Barr, Kenneth O’Byrne & Kathy Gately. (2016) In pursuit of synergy: An investigation of the PI3K/mTOR/MEK co-targeted inhibition strategy in NSCLC. Oncotarget 7:48, pages 79526-79543.
Crossref
Susan Heavey, Kenneth J. O’Byrne & Kathy Gately. (2014) Strategies for co-targeting the PI3K/AKT/mTOR pathway in NSCLC. Cancer Treatment Reviews 40:3, pages 445-456.
Crossref
William A. Denny & Gordon W. Rewcastle. 2014. Cancer Drug Design and Discovery. Cancer Drug Design and Discovery 449 478 .
Emma J. Haagensen, Huw D. Thomas, Ian Wilson, Suzannah J. Harnor, Sara L. Payne, Tommy Rennison, Kate M. Smith, Ross J. Maxwell & David R. Newell. (2013) The Enhanced In Vivo Activity of the Combination of a MEK and a PI3K Inhibitor Correlates with [18F]-FLT PET in Human Colorectal Cancer Xenograft Tumour-Bearing Mice. PLoS ONE 8:12, pages e81763.
Crossref
Qiong Wu, Meng-yao Li, Han-qing Li, Chen-hui Deng, Liang Li, Tian-yan Zhou & Wei Lu. (2013) Pharmacokinetic-pharmacodynamic modeling of the anticancer effect of erlotinib in a human non-small cell lung cancer xenograft mouse model. Acta Pharmacologica Sinica 34:11, pages 1427-1436.
Crossref
Nguyen Tan, Maureen Wong, Michelle A. Nannini, Rebecca Hong, Leslie B. Lee, Stephen Price, Karen Williams, Pierre Pascal Savy, Peng Yue, Deepak Sampath, Jeffrey Settleman, Wayne J. Fairbrother & Lisa D. Belmont. (2013) Bcl-2/Bcl-xL Inhibition Increases the Efficacy of MEK Inhibition Alone and in Combination with PI3 Kinase Inhibition in Lung and Pancreatic Tumor Models. Molecular Cancer Therapeutics 12:6, pages 853-864.
Crossref
Yuhuan Zheng, Jing Yang, Jianfei Qian, Liang Zhang, Yong Lu, Haiyan Li, Heather Lin, Yongsheng Lan, Zhiqiang Liu, Jin He, Sungyoul Hong, Sheeba Thomas, Jatin Shah, Veera Baladandayuthapani, Larry W. Kwak & Qing Yi. (2011) Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone. Journal of Molecular Medicine 90:6, pages 695-706.
Crossref
Edna F. Choo, Marcia Belvin, Jason Boggs, Yuzhong Deng, Klaus P. Hoeflich, Justin Ly, Mark Merchant, Christine Orr, Emile Plise, Kirk Robarge, Jean F. Martini, Robert Kassees, Ron G. Aoyama, Atulkumar Ramaiya & Stuart H. Johnston. (2012) Preclinical Disposition of GDC-0973 and Prospective and Retrospective Analysis of Human Dose and Efficacy Predictions. Drug Metabolism and Disposition 40:5, pages 919-927.
Crossref
David Shahbazian, Joshua Sznol & Harriet M. Kluger. 2012. Current Challenges in Personalized Cancer Medicine. Current Challenges in Personalized Cancer Medicine 1 26 .

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.