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A Decade in the MIST: Learnings from Investigations of Drug Metabolites in Drug Development under the "Metabolites in Safety Testing" Regulatory Guidance.
Schadt S, Bister B, Chowdhury SK, Funk C, Hop CECA, Humphreys WG, Igarashi F, James AD, Kagan M, Khojasteh SC, Nedderman ANR, Prakash C, Runge F, Scheible H, Spracklin DK, Swart P, Tse S, Yuan J, Obach RS. Schadt S, et al. Among authors: spracklin dk. Drug Metab Dispos. 2018 Jun;46(6):865-878. doi: 10.1124/dmd.117.079848. Epub 2018 Feb 27. Drug Metab Dispos. 2018. PMID: 29487142 Review.
Considerations for Human ADME Strategy and Design Paradigm Shift(s) - An Industry White Paper.
Young GC, Spracklin DK, James AD, Hvenegaard MG, Scarfe G, Wagner DS, Georgi K, Schieferstein H, Bjornsdottir I, van Groen B, Romeo AA, Cassidy KC, Da-Violante G, Bister B, Blech S, Lyer R, Schulz SI, Cuyckens F, Moliner P. Young GC, et al. Among authors: spracklin dk. Clin Pharmacol Ther. 2023 Apr;113(4):775-781. doi: 10.1002/cpt.2691. Epub 2022 Sep 2. Clin Pharmacol Ther. 2023. PMID: 35733280
Non-labelled, Stable Labelled or Radiolabelled Approaches for Provision of Intravenous Pharmacokinetics in Humans: a Discussion Piece.
Young GC, Spracklin DK, James AD, Hvenegaard MG, Pedersen ML, Wagner DS, Georgi K, Schieferstein H, Bjornsdottir I, Romeo AA, Cassidy KC, Da-Violante G, Blech S, Schulz SI, Cuyckens F, Nguyen MA, Scarfe G. Young GC, et al. Among authors: spracklin dk. Clin Pharmacol Ther. 2023 Nov 29. doi: 10.1002/cpt.3121. Online ahead of print. Clin Pharmacol Ther. 2023. PMID: 38018358 Review.
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H1 Receptor Inverse Agonist.
Lall MS, Bassyouni A, Bradow J, Brown M, Bundesmann M, Chen J, Ciszewski G, Hagen AE, Hyek D, Jenkinson S, Liu B, Obach RS, Pan S, Reilly U, Sach N, Smaltz DJ, Spracklin DK, Starr J, Wagenaar M, Walker GS. Lall MS, et al. Among authors: spracklin dk. J Med Chem. 2020 Jul 9;63(13):7268-7292. doi: 10.1021/acs.jmedchem.0c00483. Epub 2020 Jun 8. J Med Chem. 2020. PMID: 32462865
Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764).
Wager TT, Pettersen BA, Schmidt AW, Spracklin DK, Mente S, Butler TW, Howard H, Lettiere DJ, Rubitski DM, Wong DF, Nedza FM, Nelson FR, Rollema H, Raggon JW, Aubrecht J, Freeman JK, Marcek JM, Cianfrogna J, Cook KW, James LC, Chatman LA, Iredale PA, Banker MJ, Homiski ML, Munzner JB, Chandrasekaran RY. Wager TT, et al. Among authors: spracklin dk. J Med Chem. 2011 Nov 10;54(21):7602-20. doi: 10.1021/jm200939b. Epub 2011 Oct 7. J Med Chem. 2011. PMID: 21928839
3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.
Duplantier AJ, Efremov I, Candler J, Doran AC, Ganong AH, Haas JA, Hanks AN, Kraus KG, Lazzaro JT Jr, Lu J, Maklad N, McCarthy SA, O'Sullivan TJ, Rogers BN, Siuciak JA, Spracklin DK, Zhang L. Duplantier AJ, et al. Among authors: spracklin dk. Bioorg Med Chem Lett. 2009 May 1;19(9):2524-9. doi: 10.1016/j.bmcl.2009.03.032. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19328692
Quantitative projection of human brain penetration of the H3 antagonist PF-03654746 by integrating rat-derived brain partitioning and PET receptor occupancy.
Sawant-Basak A, Chen L, Shaffer CL, Palumbo D, Schmidt A, Tseng E, Spracklin DK, Gallezot JD, Labaree D, Nabulsi N, Huang Y, Carson RE, McCarthy T. Sawant-Basak A, et al. Among authors: spracklin dk. Xenobiotica. 2017 Feb;47(2):119-126. doi: 10.3109/00498254.2016.1166531. Epub 2016 Jun 29. Xenobiotica. 2017. PMID: 27353353
24 results