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Paul G Pearson

Explore the profile of Paul G Pearson including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 21
Citations 671
Followers 0
Related Specialties
Pharmacology
Chemistry
Science
Top 10 Co-Authors
Thomas A Baillie
Jiunn H Lin
Konstantin Petrukhin
Boglarka Racz
Christopher L Cioffi
Punam Sandhu
Graham Johnson
Keith D Barnes
Andras Varadi
Bradley K Wong
Published In
Drug Metab Dispos
J Pharmacol Exp Ther
J Med Chem
Antimicrob Agents Chemother
Chem Res Toxicol
Affiliations
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Recent Articles
1.
Identification and Characterization of ACP-5862, the Major Circulating Active Metabolite of Acalabrutinib: Both Are Potent and Selective Covalent Bruton Tyrosine Kinase Inhibitors 
Podoll T, Pearson P, Kaptein A, Evarts J, de Bruin G, Emmelot-van Hoek M, et al.
J Pharmacol Exp Ther . 2022 Oct; 384(1):173-186. PMID: 36310034
Acalabrutinib is a covalent Bruton tyrosine kinase (BTK) inhibitor approved for relapsed/refractory mantle cell lymphoma and chronic lymphocytic leukemia/small lymphocytic lymphoma. A major metabolite of acalabrutinib (M27, ACP-5862) was observed...
2.
Comparative pharmacokinetics and pharmacodynamics of the advanced Retinol-Binding Protein 4 antagonist in dog and cynomolgus monkey
Racz B, Varadi A, Pearson P, Petrukhin K
PLoS One . 2020 Jan; 15(1):e0228291. PMID: 31978148
Accumulation of lipofuscin bisretinoids in the retina contributes to pathogenesis of macular degeneration. Retinol-Binding Protein 4 (RBP4) antagonists reduce serum retinol concentrations thus partially reducing retinol delivery to the retina...
3.
Design, Synthesis, and Preclinical Efficacy of Novel Nonretinoid Antagonists of Retinol-Binding Protein 4 in the Mouse Model of Hepatic Steatosis
Cioffi C, Racz B, Varadi A, Freeman E, Conlon M, Chen P, et al.
J Med Chem . 2019 May; 62(11):5470-5500. PMID: 31079449
Retinol-binding protein 4 (RBP4) serves as a transporter for all- trans-retinol (1) in the blood, and it has been proposed to act as an adipokine. Elevated plasma levels of the...
4.
Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans
Podoll T, Pearson P, Evarts J, Ingallinera T, Bibikova E, Sun H, et al.
Drug Metab Dispos . 2018 Nov; 47(2):145-154. PMID: 30442651
Acalabrutinib
5.
A non-retinoid antagonist of retinol-binding protein 4 rescues phenotype in a model of Stargardt disease without inhibiting the visual cycle
Racz B, Varadi A, Kong J, Allikmets R, Pearson P, Johnson G, et al.
J Biol Chem . 2018 Jun; 293(29):11574-11588. PMID: 29871924
A primary pathological defect in the heritable eye disorder Stargardt disease is excessive accumulation of cytotoxic lipofuscin bisretinoids in the retina. Age-dependent accumulation of lipofuscin in the retinal pigment epithelium...
6.
ATR-101, a selective ACAT1 inhibitor, decreases ACTH-stimulated cortisol concentrations in dogs with naturally occurring Cushing's syndrome
Langlois D, Fritz M, Schall W, Olivier N, Smedley R, Pearson P, et al.
BMC Endocr Disord . 2018 May; 18(1):24. PMID: 29720169
Background: Cushing's syndrome in humans shares many similarities with its counterpart in dogs in terms of etiology (pituitary versus adrenal causes), clinical signs, and pathophysiologic sequelae. In both species, treatment...
7.
Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile
Barf T, Covey T, Izumi R, van de Kar B, Gulrajani M, van Lith B, et al.
J Pharmacol Exp Ther . 2017 Sep; 363(2):240-252. PMID: 28882879
Several small-molecule Bruton tyrosine kinase (BTK) inhibitors are in development for B cell malignancies and autoimmune disorders, each characterized by distinct potency and selectivity patterns. Herein we describe the pharmacologic...
8.
Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease
Cioffi C, Racz B, Freeman E, Conlon M, Chen P, Stafford D, et al.
J Med Chem . 2015 Jul; 58(15):5863-88. PMID: 26181715
Antagonists of retinol-binding protein 4 (RBP4) impede ocular uptake of serum all-trans retinol (1) and have been shown to reduce cytotoxic bisretinoid formation in the retinal pigment epithelium (RPE), which...
9.
Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease
Cioffi C, Dobri N, Freeman E, Conlon M, Chen P, Stafford D, et al.
J Med Chem . 2014 Sep; 57(18):7731-57. PMID: 25210858
Accumulation of lipofuscin in the retina is associated with pathogenesis of atrophic age-related macular degeneration and Stargardt disease. Lipofuscin bisretinoids (exemplified by N-retinylidene-N-retinylethanolamine) seem to mediate lipofuscin toxicity. Synthesis of...
10.
Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor
Basavapathruni A, Olhava E, Daigle S, Therkelsen C, Jin L, Boriack-Sjodin P, et al.
Biopharm Drug Dispos . 2014 Jan; 35(4):237-52. PMID: 24415392
(2R,3R,4S,5R)-2-(6-Amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol (EPZ-5676) is a novel DOT1L histone methyltransferase inhibitor currently in clinical development for the treatment of MLL-rearranged leukemias. This report describes the preclinical pharmacokinetics and metabolism of EPZ-5676, an...