August 2017
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Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors
Ken A. Brameld, Timothy D. Owens, Erik Verner, Eleni Venetsanakos, J. Michael Bradshaw, Vernon T. Phan, Danny Tam, Kwan Leung, Jin Shu, Jacob LaStant, David G. Loughhead, Tony Ton, Dane E. Karr, Mary E. Gerritsen, David M. Goldstein, and Jens Oliver Funk.
J Med Chem, August 2017
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June 2017
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A phase 1, multicenter, dose-escalation Study of PRN1371, an irreversible covalent FGFR1-4 kinase inhibitor, in patients with advanced solid tumors, followed by expansion cohorts in patients with FGFR genetic alterations
Sarina Anne Piha-Paul, Cinta Hierro, Valentino Boni, Victor Moreno, Noah Hahn, Rhonda Bitting, Todd Bauer, Rahul Raj Aggarwal, Steven Gourlay, Patrick Smith, Funda Meric-Bernstam, Dane Karr, Stefani Wolff, Farhad Kazazi, Steve Murray, Josep Tabernero.
Presented at 2017 American Society of Clinical Oncology (ASCO) Annual Meeting, Chicago, IL, June 2017
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May 2017
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A Pilot Study of the Efficacy of a Bruton’s Tyrosine Kinase Inhibitor in the Treatment of Dogs with Pemphigus Foliaceus
Murrell D.F, Gourlay S, Francesco M, Hill R.J, Bisconte A, Smith P, Karr D, Outerbridge C, Varjonen K, Goodale E.C, Borjesson D, Werth V.P, Nunn P, White S.
Presented at The Australasian College of Dermatologists – 2017 Annual Scientific Meeting, May 2017
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April 2017
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PRN1371, an irreversible, covalent inhibitor of FGFR1-4 exhibits sustained pathway inhibition in cancer cell lines
Yan Xing, Natalie Loewenstein, J.Michael Bradshaw, David M. Goldstein, Dane Karr, Jacob LaStant, Philip Nunn, Jin Shu, Abha Bommireddi, Jens Oliver Funk, Ken A. Brameld, Stefani Wolff, Steven G. Gourlay, Eleni Venetsanakos.
Presented at American Association for Cancer Research Annual Meeting, April 2017
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April 2016
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PRN1371, an irreversible, covalent inhibitor of FGFR1, 2, 3 and 4 is highly efficacious in preclinical tumor models
Venetsanakos E, Bradshaw JM, Goldstein DM, Leung K, Karr D, Gerritsen ME, Xing Y, LaStant J, Nunn PA, Shu J, Bommireddi A, Gourlay SG, Funk JO, Brameld KA.
Presented at American Association for Cancer Research Annual Meeting, New Orleans, LA, April 2016
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March 2016
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A New Treatment for Autoimmune Blistering Diseases: Efficacy of the Bruton’s Tyrosine Kinase (BTK) Inhibitor PRN473 in Canine Pemphigus Foliaceus
Outerbridge C, Goodale E, Varjonen K, Borjesson D, Murrell D, Bisconte A, Hill R, Masjedizadeh M, Gourlay SG, White S.
Presented at AAD 2016, Washington, DC, March 5, 2016
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March 2016
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Development of PRN1008, a novel, reversible covalent BTK inhibitor in clinical development for pemphigus
Murrell DF, Gourlay SG, Hill RJ, Bisconte A, Francesco M, Smith P, Karr D, Outerbridge C, Varjonen K, Goodale EC, Borjesson D, Werth VP, Nunn PA, White SD.
Presented at Medicinal Dermatology Society Annual Meeting, Washington, DC, March 3, 2016
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March 2016
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A New Treatment for Autoimmune Blistering Diseases: Efficacy of the Bruton’s Tyrosine Kinase (BTK) Inhibitor PRN473 in Canine Pemphigus Foliaceus
Outerbridge C, Goodale E, Varjonen K, Borjesson D, Murrell D, Bisconte A, Hill R, Masjedizadeh M, Gourlay SG, White S.
Presented at AAD 2016, Washington, DC, March 5, 2016
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