Publications

•  Jason J Zoeller, Ravinder Tammali, Roger B Dodd, Neki V Patel, Alma Andoni, Ina Bisha, Shane Cronin, Ana De Almeida, Nancy Lee, John H Meekin, Isabella Tilmont, Diana Gasper, Lingyun Lan, Megan Cox, Tima Thomas, Christopher Ward, Jon Chesebrough, Judith Anderton, Frances Neal, Zenon Zenonos 7, Harini Shandilya 1, K Phin Chooi 8, Kathryn Pugh 8, Ali Saleh 2, Jixin Wang 1, Pat Mitchell, Humaira Naseer, Kevin Beaumont, John Hood, Claire Myers, Simon Christ, Iris Dino, Xhenifer Guza, Tillmann Falck, Michael Lehmann, Rebecca Sargeant, Lisa Godfrey, Benedicte Recolin, Tim Brier, Simon Turner, Edward Rosfjord, Paula G Fraenkel, Sabina Cosulich, Marco Gymnopoulos, Elaine Hurt, Puja Sapra. Derivation of AZD5335, a novel FRα-targeted TOP1i-loaded ADC, for the treatment of FRα-expressing cancers. Clin Cancer Res. (2025), OF1–OF15.

​

• Simon C. C. Lucas,* J. Henry Blackwell, Ulf Börjesson, David Hargreaves, Alexander G. Milbradt,Mark J. Bostock, Samiyah Ahmed, Kevin Beaumont, Tony Cheung, Sylvain Demanze, Andrea Gohlke, Carine Guerot, Afreen Haider, Vasudev Kantae, Gregory W. Kauffman, Olaf Kinzel, Lea Kupcova, Michael D. Lainchbury, Michelle L. Lamb, Leonardo Leon, Adeline Palisse, Claudia Sacchetto, R. Ian Storer, Nancy Su, Clare Thomson, John Vales, Yunhua Chen, and Xiaolong Hu. Structure-Based Optimization of a Series of Covalent, Cell Active Bfl‑1 Inhibitors. J. Med. Chem. 2024, 67, 16455−16479.

​

• Gopalsamy, Ariamala; Aulabaugh, Ann E.; Barakat, Amey; Beaumont, Kevin C.; Cabral, Shawn; Canterbury, Daniel P.; Casimiro-Garcia, Agustin; Chang, Jeanne S.; Chen, Ming Z.; Choi, Chulho; et al. PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease. Journal of Medicinal Chemistry (2021), 64(1), 326-342.

​

• Limberakis, Chris; Boehm, Markus; Beaumont, Kevin; Jones, Rhys; Kalgutkar, Amit; Zhang, Liying; Atkinson, Karen; Bai, Guoyun; Brown, Janice; Eng, Heather; et al. Identification of novel cyclic peptide-peptoid hybrid CXCR7 modulators. From Abstracts of Papers, 256th ACS National Meeting & Exposition, Boston, MA, United States, August 19-23, 2018 (2018), MEDI-151.

 

• Menhaji-Klotz, Elnaz; Hesp, Kevin D.; Londregan, Allyn Timothy; Kalgutkar, Amit S.; Piotrowski, David W.; Boehm, Markus; Song, Kun; Ryder, Tim; Beaumont, Kevin; Jones, Rhys M.; et al Discovery of a Novel Small Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis. Journal of Medicinal Chemistry (2018), 61(8), 3685-3696.

​

• McClure, Kim F.; Piotrowski, David W.; Petersen, Donna; Wei, Liuqing; Xiao, Jun; Londregan, Allyn T.; Kamlet, Adam S.; Dechert-Schmitt, Anne-Marie; Raymer, Brian; Ruggeri, Roger B.; Beaumont, Kevin et al. Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis. Angewandte Chemie, International Edition (2017), 56(51), 16218-16222.

​

• Gosset, James R.; Beaumont, Kevin; Matsuura, Tomomi; Winchester, Wendy; Attkins, Neil; Glatt, Sophie; Lightbown, Ian; Ulrich, Kristina; Roberts, Sonia; Harris, Jolie; et al. A cross-species translational pharmacokinetic-pharmacodynamic evaluation of core body temperature reduction by the TRPM8 blocker PF-05105679. European Journal of Pharmaceutical Sciences (2017), 109(Suppl.), S161-S167.

 

• Boehm, Markus; Beaumont, Kevin; Jones, Rhys M.; Kalgutkar, Amit S.; Zhang, Liying; Atkinson, Karen; Bai, Guoyun; Brown, Janice A.; Eng, Heather; Goetz, Gilles H.; et al. Discovery of potent and orally bioavailable macrocyclic peptide-peptoid hybrid CXCR7 modulators. Journal of Medicinal Chemistry (2017), 60(23), 9653-9663.

​

• Sanhueza, Carlos A.; Baksh, Michael M.; Thuma, Benjamin; Roy, Marc D.; Dutta, Sanjay; Preville, Cathy; Chrunyk, Boris A.; Beaumont, Kevin; Dullea, Robert; Ammirati, Mark et al. Efficient Liver Targeting by Polyvalent Display of a Compact Ligand for the Asialoglycoprotein Receptor. Journal of the American Chemical Society (2017), 139(9), 3528-3536.

 

• Trapa, Patrick E.; Beaumont, Kevin; Atkinson, Karen; Eng, Heather; King-Ahmad, Amanda; Scott, Dennis O.; Maurer, Tristan S.; Di, Li. In Vitro-In Vivo Extrapolation of Intestinal Availability for Carboxylesterase Substrates Using Portal Vein-Cannulated Monkey. Journal of Pharmaceutical Sciences (2017), 106 (3), 898-905.

​

• Jones, Hannah M.; Butt, Richard P.; Webster, Rob W.; Gurrell, Ian; Dzygiel, Pawel; Flanagan, Neil; Fraier, Daniela; Hay, Tanya; Iavarone, Laura Else; Luckwell, Jacquelynn; Pearce, Hannah; Phipps, Alex; Segelbacher, Jill; Speed, Bill; Beaumont, Kevin. Clinical Micro-Dose Studies to Explore the Human Pharmacokinetics of Four Selective Inhibitors of Human Nav1.7 Voltage-Dependent Sodium Channels. Clinical Pharmacokinetics (2016), 55(7), 875-887.

 

• Andrews, Mark D.; af Forselles, Kerry; Beaumont, Kevin; Galan, Sebastien R. G.; Glossop, Paul A.; Grenie, Mathilde; Jessiman, Alan; Kenyon, Amy S.; Lunn, Graham; Maw, Graham; et al. Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain. ACS Medicinal Chemistry Letters (2015), 6(4), 419-424.

 

• Winchester, W., Gore, K., Glatt, S., Petit, W., Gardiner, J., Conlon, K., Postlethwaite, M., Saintot, Pierre-Philippe., Roberts, Sonia, Gosset, J., Matsuura, T., Andrews, M., Glossop, P., Palmer, M., Clear, N., Collins, S., Beaumont, K. and Reynolds, D. Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. Journal of Pharmacology and Experimental Therapeutics (2014), 351(2), 259-269.

 

• Beaumont, K.; Gosset, J. R. and Keefer, C. E. Integrated assessment of drug clearance and cross-species scalability. From "Predictive ADMET: Integrative approaches in drug discovery and development" (2014), Chapter 14, 291-318.

 

• Rawson, D.; Ballard, S.; Barber, C.; Barker, L.; Beaumont, K.; Bunnage, M.; Cole, S.; Corless, M.; Denton, S.; Ellis, D. The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics. Bioorganic & Medicinal Chemistry (2012), 20(1), 498-509.

 

• Harrison, A.; Gardner, I.; Hay, T.; Dickins, M.; Beaumont, K.; Phipps, A.; Purkins, L.; Allan, G.; Christian, R.; Duckworth, J. Case studies addressing human pharmacokinetic uncertainty using a combination of pharmacokinetic simulation and alternative first in human paradigms. Xenobiotica (2012), 42(1), 57-74.

 

• Hay, Tanya; Jones, Rhys; Beaumont, Kevin; Kemp, Mark. Modulation of the partition coefficient between octanol and buffer at pH 7.4 and pKa to achieve the optimum balance of blood clearance and volume of distribution for a series of tetrahydropyran histamine type 3 receptor antagonists. Drug Metabolism and Disposition (2009), 37(9), 1864-1870.

​

• Hosea, Natilie A.; Collard, Wendy T.; Cole, Susan; Maurer, Tristan S.; Fang, Rick X.; Jones, Hannah; Kakar, Shefali M.; Nakai, Yasuhiro; Smith, Bill J.; Webster, Rob; Beaumont, Kevin. Prediction of human pharmacokinetics from preclinical information: comparative accuracy of quantitative prediction approaches. Journal of Clinical Pharmacology (2009), 49(5), 513-533.

 

• Blagg, Julian; Mowbray, Charles; Pryde, David; Salmon, Gary; Fairman, David; Schmid, Esther; Beaumont, Kevin. Small, non-peptide C5a receptor antagonists: Part 2. Bioorganic & Medicinal Chemistry Letters (2008), 18(20), 5605-5608.

 

• Blagg, Julian; Mowbray, Charles; Pryde, David C.; Salmon, Gary; Schmid, Esther; Fairman, David; Beaumont, Kevin. Small, non-peptide C5a receptor antagonists: Part 1. Bioorganic & Medicinal Chemistry Letters (2008), 18(20), 5601-5604.

 

• Bunnage, Mark E.; Blagg, Julian; Steele, John; Owen, Dafydd R.; Allerton, Charlotte; McElroy, Andrew B.; Miller, Duncan; Ringer, Tracy; Butcher, Ken; Beaumont, Kevin; Evans, Karen; Gray, Andrew J.; Holland, Stephen J.; Feeder, Neil; Moore, Robert S.; Brown, David G. Discovery of Potent & Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor for the Treatment of Thrombosis. Journal of Medicinal Chemistry (2007), 50(24), 6095-6103.

​

• Meng, Xiaoli; Maggs, James L.; Pryde, David C.; Planken, Simon; Jenkins, Rosalind E.; Peakman, Torren M.; Beaumont, Kevin; Kohl, Christopher; Park, B. Kevin; Stachulski, Andrew V. Cyclization of the Acyl Glucuronide Metabolite of a Neutral Endopeptidase Inhibitor to an Electrophilic Glutarimide: Synthesis, Reactivity, and Mechanistic Analysis. Journal of Medicinal Chemistry (2007), 50(24), 6165-6176.

 

• Betts, Alison; Atkinson, Fidelma; Gardner, Iain; Fox, David; Webster, Rob; Beaumont, Kevin; Morgan, Paul. Impact of physicochemical and structural properties on the pharmacokinetics of a series of a1L-adrenoceptor antagonists. Drug Metabolism and Disposition (2007), 35(8), 1435-1445.

 

• Pryde, David C.; Cook, Andrew S.; Burring, Denise J.; Jones, Lyn H.; Foll, Stephanie; Platts, Michelle Y.; Sanderson, Vivienne; Corless, Martin; Stobie, Alan; Middleton, Donald S.; Foster, Laura; Barker, Laura; Van Der Graaf, Piet; Stacey, Peter; Kohl, Christopher; Coggon, Sara; Beaumont, Kevin. Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder. Bioorganic & Medicinal Chemistry (2007), 15(1), 142-159.

 

• Pryde, David C.; Maw, Graham N.; Planken, Simon; Platts, Michelle Y.; Sanderson, Vivienne; Corless, Martin; Stobie, Alan; Barber, Christopher G.; Russell, Rachel; Foster, Laura; Barker, Laura; Wayman, Christopher; Van Der Graaf, Piet; Stacey, Peter; Morren, Debbie; Kohl, Christopher; Beaumont, Kevin; Coggon, Sara; Tute, Michael. Novel Selective Inhibitors of Neutral Endopeptidase for the Treatment of Female Sexual Arousal Disorder. Synthesis and Activity of Functionalized Glutaramides. Journal of Medicinal Chemistry (2006), 49(14), 4409-4424.

 

• Allerton, Charlotte M. N.; Barber, Christopher G.; Beaumont, Kevin C.; Brown, David G.; Cole, Susan M.; Ellis, David; Lane, Charlotte A. L.; Maw, Graham N.; Mount, Natalie M.; Rawson, David J.; Robinson, Colin M.; Street, Stephen D. A.; Summerhill, Nicholas W. A Novel Series of Potent and Selective PDE5 Inhibitors with Potential for High and Dose-Independent Oral Bioavailability. Journal of Medicinal Chemistry (2006), 49(12), 3581-3594.

​

• Maw, Graham N.; Stobie, Alan; Planken, Simon; Pryde, David C.; Sanderson, Vivienne; Platts, Michelle Y.; Corless, Martin; Stacey, Peter; Wayman, Christopher; Van Der Graaf, Piet; Kohl, Christopher; Coggon, Sara; Beaumont, Kevin. The discovery of small molecule inhibitors of neutral endopeptidase. Structure-activity studies on functionalized glutaramides. Chemical Biology & Drug Design (2006), 67(1), 74-77.

​

• Beaumont, Kevin; Schmid, Esther; Smith, Dennis A. Oral delivery of G protein-coupled receptor modulators: An explanation for the observed class difference. Bioorganic & Medicinal Chemistry Letters (2005), 15(16), 3658-3664.

​

• Bunnage, Mark E.; Mathias, John P.; Street, Stephen D. A.; Wood, Anthony; Ballard, Stephen A.; Beaumont, Kevin C.. Highly selective chiral PDE5 inhibitors for treatment of MED. Abstracts of Papers, 227th ACS National Meeting, Anaheim, CA, United States, March 28-April 1, 2004.

​

• Harrison, Anthony; Betts, Alison; Fenner, Katherine; Beaumont, Kevin; Edgington, Alan; Roffey, Sarah; Davis, John; Comby, Pierre; Morgan, Paul. Nonlinear oral pharmacokinetics of the a -antagonist 4-amino-5-(4-fluorophenyl)-6,7-dimethoxy-2-[4-(morpholinocarbonyl)perhydro-1,4-diazepin-1-yl]quinoline in humans: Use of preclinical data to rationalize clinical observations. Drug Metabolism and Disposition (2004), 32(2), 197-204.

​

• Beaumont, Kevin; Webster, Robert; Gardner, Iain; Dack, Kevin. Design of ester prodrugs to enhance oral absorption of poorly permeable compounds: Challenges to the discovery scientist. Current Drug Metabolism (2003), 4(6), 461-485.

​

• Beaumont, Kevin. The importance of gut wall metabolism in determining drug bioavailability. Methods and Principles in Medicinal Chemistry (2003), 18(Drug Bioavailability), 311-328.

​

• Mathias, John P.; Ballard, Stephen A.; Beaumont, Kevin C.; Bunnage, Mark E.; Wood, Anthony; Street, Stephen D. A. Design and synthesis of selective PDE5 inhibitors for the treatment of MED. Abstracts of Papers, 224th ACS National Meeting, Boston, MA, United States, August 18-22, 2002.

​

• Abel, S.; Beaumont, K. C.; Crespi, C. L.; Eve, M. D.; Fox, L.; Hyland, R.; Jones, B. C.; Muirhead, G. J.; Smith, D. A.; Venn, R. F.; Walker, D. K. Potential role for P-glycoprotein in the non-proportional pharmacokinetics of UK-343,664 in man. Xenobiotica (2001), 31(8/9), 665-676.

​

• Walker, D. K.; Beaumont, K. C.; Comby, P.; Evans, K. M.; Gedge, J. I.; Halliday, R. C.; Roffey, S. J.; Wright, P. A. Pharmacokinetics and metabolism of a selective PDE5 inhibitor (UK-343,664) in rat and dog. Xenobiotica (2001), 31(8/9), 651-664.

​

• van de Waterbeemd, Han; Smith, Dennis A.; Beaumont, Kevin; Walker, Don K. Property-based design: optimization of drug absorption and pharmacokinetics. Journal of Medicinal Chemistry (2001), 44(9), 1313-1333.

 

• Webster, R.; Beaumont, K.; Ritzau, M.; Stachulski, A. V. The synthesis of the glucuronide metabolite of UK-157,147 using immobilized uridine 5'-diphosphoglucuronyl transferase and traditional organic chemistry techniques (imidate method). Biocatalysis and Biotransformation (2001), 19(1), 69-83.

​

• Ethell, Brian T.; Beaumont, Kevin; Rance, David J.; Burchell, Brian. Use of cloned and expressed human UDP-glucuronosyltransferases for the assessment of human drug conjugation and identification of potential drug interactions. Drug Metabolism and Disposition (2001), 29(1), 48-53.

 

• Beaumont, K.; Harper, A.; Smith, D. A.; Bennett, J. The role of P-glycoprotein in determining the oral absorption and clearance of the NK2 antagonist, UK-224,671. European Journal of Pharmaceutical Sciences (2000), 12(1), 41-50.

​

• Beaumont, K.; Harper, A.; Smith, D. A.; Abel, S. Pharmacokinetics and metabolism of a sulphamide NK2 antagonist in rat, dog and human. Xenobiotica (2000), 30(6), 627-642.

 

• Amacher, D. E.; Fasulo, L. M.; Charuel, C.; Comby, P.; Beaumont, K.. In vitro toxicity of zamifenacin (UK-76654) and metabolites in primary hepatocyte cultures. Xenobiotica (1998), 28(9), 895-908.

​

• Beaumont, K. C.; Cussans, N. J.; Nichols, D. J.; Smith, D. A. Pharmacokinetics and metabolism of darifenacin in the mouse, rat, dog and man. Xenobiotica (1998), 28(1), 63-75.

​

• Ethell, Brian T.; Anderson, Gail D.; Beaumont, Kevin; Rance, David J.; Burchell, Brian. A universal radiochemical high-performance liquid chromatographic assay for the determination of UDP-glucuronosyltransferase activity. Analytical Biochemistry (1998), 255(1), 142-147.

 

• Walker, D. K.; Beaumont, K. C.; Stopher, D. A.; Smith, D. A. Pharmacokinetics of a series of bis(methanesulfonamido-arylakyl)amines in the beagle dog. Xenobiotica (1996), 26(10), 1101-1111.

​

• Beaumont, K. C.; Causey, A. G.; Coates, P. E.; Smith, D. A. Pharmacokinetics and metabolism of zamifenacin in mouse, rat, dog and man. Xenobiotica (1996), 26(4), 459-71.

​

• Smith, D. A.; Beaumont, K.; Cussans, N. J.; Humphrey, M. J.; Jezequel, S. G.; Rance, D. J.; Stopher, D. A.; Walker, D. K. Bioanalytical data in decision making: discovery and development. Xenobiotica (1992), 22(9-10), 1195-1205.