First-in-Human Phase I Study to Evaluate the Brain-Penetrant PI3K/mTOR Inhibitor GDC-0084 in Patients with Progressive or Recurrent High-Grade Glioma
Wen, Patrick Y, Cloughesy, Timothy F, Olivero, Alan G, Morrissey, Kari M, Wilson, Timothy R, Lu, Xuyang, Mueller, Lars U, Coimbra, Alexandre F, Ellingson, Benjamin M, Gerstner, Elizabeth, Lee, Eudocia Q, Rodon, Jordi
Published in Clinical cancer research (15.04.2020)
Published in Clinical cancer research (15.04.2020)
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Preclinical characterization of the absorption and disposition of the brain penetrant PI3K/mTOR inhibitor paxalisib and prediction of its pharmacokinetics and efficacy in human
Salphati, Laurent, Pang, Jodie, Alicke, Bruno, Plise, Emile G, Cheong, Jonathan, Jaochico, Allan, Olivero, Alan G, Sampath, Deepak, Wong, Susan, Zhang, Xiaolin
Published in Xenobiotica (07.02.2024)
Published in Xenobiotica (07.02.2024)
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GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway
Wallin, Jeffrey J, Edgar, Kyle A, Guan, Jane, Berry, Megan, Prior, Wei Wei, Lee, Leslie, Lesnick, John D, Lewis, Cristina, Nonomiya, Jim, Pang, Jodie, Salphati, Laurent, Olivero, Alan G, Sutherlin, Daniel P, O'Brien, Carol, Spoerke, Jill M, Patel, Sonal, Lensun, Letitia, Kassees, Robert, Ross, Leanne, Lackner, Mark R, Sampath, Deepak, Belvin, Marcia, Friedman, Lori S
Published in Molecular cancer therapeutics (01.12.2011)
Published in Molecular cancer therapeutics (01.12.2011)
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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy
Song, Kyung W, Edgar, Kyle A, Hanan, Emily J, Hafner, Marc, Oeh, Jason, Merchant, Mark, Sampath, Deepak, Nannini, Michelle A, Hong, Rebecca, Phu, Lilian, Forrest, William F, Stawiski, Eric, Schmidt, Stephen, Endres, Nicholas, Guan, Jane, Wallin, Jeffrey J, Cheong, Jonathan, Plise, Emile G, Lewis Phillips, Gail D, Salphati, Laurent, Heffron, Timothy P, Olivero, Alan G, Malek, Shiva, Staben, Steven T, Kirkpatrick, Donald S, Dey, Anwesha, Friedman, Lori S
Published in Cancer discovery (01.01.2022)
Published in Cancer discovery (01.01.2022)
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Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity
Ndubaku, Chudi O, Heffron, Timothy P, Staben, Steven T, Baumgardner, Matthew, Blaquiere, Nicole, Bradley, Erin, Bull, Richard, Do, Steven, Dotson, Jennafer, Dudley, Danette, Edgar, Kyle A, Friedman, Lori S, Goldsmith, Richard, Heald, Robert A, Kolesnikov, Aleksandr, Lee, Leslie, Lewis, Cristina, Nannini, Michelle, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Wallin, Jeffery J, Wang, Lan, Wei, BinQing, Sampath, Deepak, Olivero, Alan G
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
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The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer
Folkes, Adrian J, Ahmadi, Khatereh, Alderton, Wendy K, Alix, Sonia, Baker, Stewart J, Box, Gary, Chuckowree, Irina S, Clarke, Paul A, Depledge, Paul, Eccles, Suzanne A, Friedman, Lori S, Hayes, Angela, Hancox, Timothy C, Kugendradas, Arumugam, Lensun, Letitia, Moore, Pauline, Olivero, Alan G, Pang, Jodie, Patel, Sonal, Pergl-Wilson, Giles H, Raynaud, Florence I, Robson, Anthony, Saghir, Nahid, Salphati, Laurent, Sohal, Sukhjit, Ultsch, Mark H, Valenti, Melanie, Wallweber, Heidi J.A, Wan, Nan Chi, Wiesmann, Christian, Workman, Paul, Zhyvoloup, Alexander, Zvelebil, Marketa J, Shuttleworth, Stephen J
Published in Journal of medicinal chemistry (25.09.2008)
Published in Journal of medicinal chemistry (25.09.2008)
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The Rational Design of Selective Benzoxazepin Inhibitors of the α‑Isoform of Phosphoinositide 3‑Kinase Culminating in the Identification of (S)‑2-((2-(1-Isopropyl‑1H‑1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)
Heffron, Timothy P, Heald, Robert A, Ndubaku, Chudi, Wei, BinQing, Augistin, Martin, Do, Steven, Edgar, Kyle, Eigenbrot, Charles, Friedman, Lori, Gancia, Emanuela, Jackson, Philip S, Jones, Graham, Kolesnikov, Aleksander, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, McLean, Neville, Mörtl, Mario, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Staben, Steven T, Steinbacher, Stefan, Tsui, Vickie, Wallin, Jeffrey, Sampath, Deepak, Olivero, Alan G
Published in Journal of medicinal chemistry (11.02.2016)
Published in Journal of medicinal chemistry (11.02.2016)
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Multiparametric MR-PET Imaging Predicts Pharmacokinetics and Clinical Response to GDC-0084 in Patients with Recurrent High-Grade Glioma
Ellingson, Benjamin M, Yao, Jingwen, Raymond, Catalina, Nathanson, David A, Chakhoyan, Ararat, Simpson, Jeremy, Garner, James S, Olivero, Alan G, Mueller, Lars U, Rodon, Jordi, Gerstner, Elizabeth, Cloughesy, Timothy F, Wen, Patrick Y
Published in Clinical cancer research (01.07.2020)
Published in Clinical cancer research (01.07.2020)
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Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR
Heffron, Timothy P, Ndubaku, Chudi O, Salphati, Laurent, Alicke, Bruno, Cheong, Jonathan, Drobnick, Joy, Edgar, Kyle, Gould, Stephen E, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, Nonomiya, Jim, Pang, Jodie, Plise, Emile G, Sideris, Steve, Wallin, Jeffrey, Wang, Lan, Zhang, Xiaolin, Olivero, Alan G
Published in ACS medicinal chemistry letters (14.04.2016)
Published in ACS medicinal chemistry letters (14.04.2016)
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A Selective, Slow Binding Inhibitor of Factor VIIa Binds to a Nonstandard Active Site Conformation and Attenuates Thrombus Formation in Vivo
Olivero, Alan G., Eigenbrot, Charles, Goldsmith, Richard, Robarge, Kirk, Artis, Dean R., Flygare, John, Rawson, Thomas, Sutherlin, Daniel P., Kadkhodayan, Saloumeh, Beresini, Maureen, Elliott, Linda O., DeGuzman, Geralyn G., Banner, David W., Ultsch, Mark, Marzec, Ulla, Hanson, Stephen R., Refino, Canio, Bunting, Stuart, Kirchhofer, Daniel
Published in The Journal of biological chemistry (11.03.2005)
Published in The Journal of biological chemistry (11.03.2005)
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Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma
Salphati, Laurent, Alicke, Bruno, Heffron, Timothy P, Shahidi-Latham, Sheerin, Nishimura, Merry, Cao, Tim, Carano, Richard A, Cheong, Jonathan, Greve, Joan, Koeppen, Hartmut, Lau, Shari, Lee, Leslie B, Nannini-Pepe, Michelle, Pang, Jodie, Plise, Emile G, Quiason, Cristine, Rangell, Linda, Zhang, Xiaolin, Gould, Stephen E, Phillips, Heidi S, Olivero, Alan G
Published in Drug metabolism and disposition (01.12.2016)
Published in Drug metabolism and disposition (01.12.2016)
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Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging
Salphati, Laurent, Shahidi-Latham, Sheerin, Quiason, Cristine, Barck, Kai, Nishimura, Merry, Alicke, Bruno, Pang, Jodie, Carano, Richard A, Olivero, Alan G, Phillips, Heidi S
Published in Drug metabolism and disposition (01.07.2014)
Published in Drug metabolism and disposition (01.07.2014)
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The Design and Identification of Brain Penetrant Inhibitors of Phosphoinositide 3‑Kinase α
Heffron, Timothy P, Salphati, Laurent, Alicke, Bruno, Cheong, Jonathan, Dotson, Jennafer, Edgar, Kyle, Goldsmith, Richard, Gould, Stephen E, Lee, Leslie B, Lesnick, John D, Lewis, Cristina, Ndubaku, Chudi, Nonomiya, Jim, Olivero, Alan G, Pang, Jodie, Plise, Emile G, Sideris, Steve, Trapp, Sean, Wallin, Jeffrey, Wang, Lan, Zhang, Xiaolin
Published in Journal of medicinal chemistry (27.09.2012)
Published in Journal of medicinal chemistry (27.09.2012)
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Targeting the PI3K Pathway in the Brain-Efficacy of a PI3K Inhibitor Optimized to Cross the Blood―Brain Barrier
SALPHATI, Laurent, HEFFRON, Timothy P, KOEPPEN, Hartmut, LAU, Shari, LEE, Leslie B, PANG, Jodie, PLISE, Emile G, POKORNY, Jenny L, BOU RESLAN, Hani, SARKARIA, Jann N, WALLIN, Jeffrey J, XIAOLIN ZHANG, ALICKE, Bruno, GOULD, Stephen E, OLIVERO, Alan G, PHILLIPS, Heidi S, NISHIMURA, Merry, BARCK, Kai, CARANO, Richard A, CHEONG, Jonathan, EDGAR, Kyle A, GREVE, Joan, KHARBANDA, Samir
Published in Clinical cancer research (15.11.2012)
Published in Clinical cancer research (15.11.2012)
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Preclinical assessment of the absorption and disposition of the phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor GDC-0980 and prediction of its pharmacokinetics and efficacy in human
Salphati, Laurent, Pang, Jodie, Plise, Emile G, Lee, Leslie B, Olivero, Alan G, Prior, Wei Wei, Sampath, Deepak, Wong, Susan, Zhang, Xiaolin
Published in Drug metabolism and disposition (01.09.2012)
Published in Drug metabolism and disposition (01.09.2012)
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Journal Article
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform
Staben, Steven T., Ndubaku, Chudi, Blaquiere, Nicole, Belvin, Marcia, Bull, Richard J., Dudley, Danette, Edgar, Kyle, Gray, Daniel, Heald, Robert, Heffron, Timothy P., Jones, Graham E., Jones, Mark, Kolesnikov, Aleks, Lee, Leslie, Lesnick, John, Lewis, Cristina, Murray, Jeremy, McLean, Neville J., Nonomiya, Jim, Olivero, Alan G., Ord, Rachel, Pang, Jodie, Price, Stephen, Prior, Wei Wei, Rouge, Lionel, Salphati, Laurent, Sampath, Deepak, Wallin, Jeff, Wang, Lan, Wei, BinQing, Weismann, Christian, Wu, Ping
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
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Journal Article
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase
Staben, Steven T, Siu, Michael, Goldsmith, Richard, Olivero, Alan G, Do, Steven, Burdick, Daniel J, Heffron, Timothy P, Dotson, Jenna, Sutherlin, Daniel P, Zhu, Bing-Yan, Tsui, Vickie, Le, Hoa, Lee, Leslie, Lesnick, John, Lewis, Cristina, Murray, Jeremy M, Nonomiya, Jim, Pang, Jodie, Prior, Wei Wei, Salphati, Laurent, Rouge, Lionel, Sampath, Deepak, Sideris, Steve, Wiesmann, Christian, Wu, Ping
Published in Bioorganic & medicinal chemistry letters (01.07.2011)
Published in Bioorganic & medicinal chemistry letters (01.07.2011)
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Journal Article
Cis-Amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase
Staben, Steven T., Blaquiere, Nicole, Tsui, Vickie, Kolesnikov, Aleksandr, Do, Steven, Bradley, Erin K., Dotson, Jenna, Goldsmith, Richard, Heffron, Timothy P., Lesnick, John, Lewis, Cristina, Murray, Jeremy, Nonomiya, Jim, Olivero, Alan G., Pang, Jodie, Rouge, Lionel, Salphati, Laurent, Wei, BinQing, Wiesmann, Christian, Wu, Ping
Published in Bioorganic & medicinal chemistry letters (01.02.2013)
Published in Bioorganic & medicinal chemistry letters (01.02.2013)
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Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human
Salphati, Laurent, Pang, Jodie, Plise, Emile G., Chou, Bilin, Halladay, Jason S., Olivero, Alan G., Rudewicz, Patrick J., Tian, Qingping, Wong, Susan, Zhang, Xiaolin
Published in Xenobiotica (01.12.2011)
Published in Xenobiotica (01.12.2011)
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Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase
Staben, Steven T., Heffron, Timothy P., Sutherlin, Daniel P., Bhat, Seema R., Castanedo, Georgette M., Chuckowree, Irina S., Dotson, Jenna, Folkes, Adrian J., Friedman, Lori S., Lee, Leslie, Lesnick, John, Lewis, Cristina, Murray, Jeremy M., Nonomiya, Jim, Olivero, Alan G., Plise, Emile, Pang, Jodie, Prior, Wei Wei, Salphati, Laurent, Rouge, Lionel, Sampath, Deepak, Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Weismann, Christian, Wu, Ping, Zhu, Bing-Yan
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
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