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Nigel J Waters
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Journal Articles

The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia

Free
Clinical Trials & Observations
Eytan M. Stein, Guillermo Garcia-Manero, David A. Rizzieri, Raoul Tibes, Jesus G. Berdeja, Michael R. Savona, Mojca Jongen-Lavrenic, Jessica K. Altman, Blythe Thomson, Stephen J. Blakemore, Scott R. Daigle, Nigel J. Waters, A. Benjamin Suttle, Alicia Clawson, Roy Pollock, Andrei Krivtsov, Scott A. Armstrong, Jorge DiMartino, Eric Hedrick, Bob Löwenberg, Martin S. Tallman
Journal: Blood
Blood (2018) 131 (24): 2661–2669.
https://doi.org/10.1182/blood-2017-12-818948
Published: 2018
Includes: Supplemental data
Journal Articles

Early Results from a Biomarker-Directed Phase 2 Trial of Sy-1425 in Acute Myeloid Leukemia (AML) and Myelodysplastic Syndrome (MDS) Demonstrate DHRS3 Induction and Myeloid Differentiation Following Sy-1425 Treatment

Free
Joseph G. Jurcic, MD, Azra Raza, MD, George Vlad, PhD, Eytan M. Stein, MD, Mikhail Roshal, MDPhD, Dale L. Bixby, Daniel F. Boyer, MD PhD, Carlos Enrique Vigil, MD, Sergei Syrbu, MD PhD, Mikkael A. Sekeres, MD MS, Heesun J. Rogers, MD PhD, David A. Rizzieri, MD, Anand Shreeram Lagoo, MD PhD, Gail J. Roboz, MD, Robert L. Redner, MD, David P. Steensma, MD, Rachel J. Cook, MD, Tamara Moyo, MD PhD, Michael McKeown, PhD, Nigel J. Waters, PhD, Kristin Stephens, Angela Volkert, Emmanuelle Di Tomaso, PhD, David A. Roth, MD, Jorge E. Cortes, MD
Journal: Blood
Blood (2017) 130 (Supplement 1): 2633.
https://doi.org/10.1182/blood.V130.Suppl_1.2633.2633
Published: 2017
Journal Articles

Final Report of Phase 1 Study of the DOT1L Inhibitor, Pinometostat (EPZ-5676), in Children with Relapsed or Refractory MLL-r Acute Leukemia

Free
Neerav Shukla, MD, Cynthia Wetmore, MD PhD, Maureen M O'Brien, MD, Lewis B. Silverman, MD, Patrick Brown, MD, Todd M Cooper, DO, Blythe Thomson, MD, Stephen J. Blakemore, PhD, Scott Daigle, Ben Suttle, Nigel J. Waters, PhD, Andrei V Krivstov, PhD, Scott A. Armstrong, MD PhD, Peter T Ho, PhD MD, Lia Gore, MD
Journal: Blood
Blood (2016) 128 (22): 2780.
https://doi.org/10.1182/blood.V128.22.2780.2780
Published: 2016
Journal Articles

Preliminary Report of the Phase 1 Study of the DOT1L Inhibitor, Pinometostat, EPZ-5676, in Children with Relapsed or Refractory MLL-r Acute Leukemia: Safety, Exposure and Target Inhibition

Free
Neerav Shukla, MD, Maureen M. O'Brien, MD, Lewis B. Silverman, MD, Melinda Pauly, MD, Cynthia Wetmore, MD PhD, Mignon L. Loh, MD, James A. Whitlock, MD, Patrick Brown, MD, Blythe Thomson, MD, Stephen J. Blakemore, PhD, Scott Daigle, Patricia Pimentel, Nigel J. Waters, PhD, Andrei V Krivstov, PhD, Richard Koche, PhD, Scott A. Armstrong, MD PhD, Peter T Ho, PhD MD, Lia Gore, MD
Journal: Blood
Blood (2015) 126 (23): 3792.
https://doi.org/10.1182/blood.V126.23.3792.3792
Published: 2015
Journal Articles

A Phase 1 Study of the DOT1L Inhibitor, Pinometostat (EPZ-5676), in Adults with Relapsed or Refractory Leukemia: Safety, Clinical Activity, Exposure and Target Inhibition

Free
Eytan M. Stein, MD, Guillermo Garcia-Manero, MD, David A. Rizzieri, MD, Raoul Tibes, MD PhD, Jesus G. Berdeja, MD, Mojca Jongen-Lavrencic, MD PhD, Jessica K. Altman, MD, Hartmut Dohner, MD, Blythe Thomson, MD, Stephen J. Blakemore, PhD, Scott Daigle, Greg Fine, MS, Nigel J. Waters, PhD, Andrei V Krivstov, PhD, Richard Koche, PhD, Scott A. Armstrong, MD PhD, Peter T Ho, PhD MD, Bob Lowenberg, MD PhD, Martin S Tallman, MD
Journal: Blood
Blood (2015) 126 (23): 2547.
https://doi.org/10.1182/blood.V126.23.2547.2547
Published: 2015
Journal Articles

Identification of a First-in-Class PRMT5 Inhibitor with Potent in Vitro and in Vivo Activity in Preclinical Models of Mantle Cell Lymphoma

Free
Elayne Penebre, PhD, Kristy G Kuplast, Christina R Majer, L. Danielle Johnston, MS, Nathalie Rioux, PhD, Michael Munchhof, PhD, Lei Jin, PhD, P. Ann Boriak-Sjodin, PhD, Tim J Wigle, PhD, Suzanne L Jacques, PhD, Kip A West, PhD, Trupti Lingaraj, Kimberly Stickland, PhD, Scott A Ribich, PhD, Alejandra Raimondi, MS, Margaret Porter-Scott, PhD, Nigel J Waters, PhD, Roy M Pollock, PhD, Jesse J Smith, PhD, Olena Barbash, PhD, Ryan G. Kruger, PhD, Robert A Copeland, PhD, Mikel P Moyer, PhD, Richard Chesworth, DPhil, Kenneth W Duncan, PhD
Journal: Blood
Blood (2014) 124 (21): 438.
https://doi.org/10.1182/blood.V124.21.438.438
Published: 2014
Journal Articles

Pediatric Dose Determinations for the Phase I Study of the DOT1L Inhibitor, EPZ-5676, in MLL-r Acute Leukemia: Leveraging Early Clinical Data in Adults through Physiologically-Based Pharmacokinetic Modeling

Free
Nigel J Waters, PhD, Blythe Thomson, MD, Iain Gardner, PhD, Trevor N Johnson, PhD, Edward J Olhava, PhD, Roy M Pollock, PhD, Michelle Legler, MSHS, Robert A Copeland, PhD, Eric E Hedrick, MD
Journal: Blood
Blood (2014) 124 (21): 3619.
https://doi.org/10.1182/blood.V124.21.3619.3619
Published: 2014
Journal Articles

The DOT1L Inhibitor EPZ-5676: Safety and Activity in Relapsed/Refractory Patients with MLL-Rearranged Leukemia

Free
Eytan M. Stein, Guillermo Garcia-Manero, MD, David A. Rizzieri, MD, Michael Savona, MD, Raoul Tibes, MD, Jessica K Altman, Mojca Jongen-Lavrencic, MD PhD, Hartmut Döhner, Prof., Scott Armstrong, MD PhD, Roy M Pollock, PhD, Nigel J Waters, PhD, Michelle Legler, MSHS, Blythe Thomson, MD, Scott Daigle, Alice McDonald, Carly Campbell, Ed Olhava, Eric E Hedrick, MD, Bob Lowenberg, MDPhD, Robert A Copeland, PhD, Martin S. Tallman, MD
Journal: Blood
Blood (2014) 124 (21): 387.
https://doi.org/10.1182/blood.V124.21.387.387
Published: 2014
Journal Articles

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

Free
Scott R. Daigle, Edward J. Olhava, Carly A. Therkelsen, Aravind Basavapathruni, Lei Jin, P. Ann Boriack-Sjodin, Christina J. Allain, Christine R. Klaus, Alejandra Raimondi, Margaret Porter Scott, Nigel J. Waters, Richard Chesworth, Mikel P. Moyer, Robert A. Copeland, Victoria M. Richon, Roy M. Pollock
Journal: Blood
Blood (2013) 122 (6): 1017–1025.
https://doi.org/10.1182/blood-2013-04-497644
Published: 2013
Includes: Supplemental data