PHARMACOLOGY

Kathleen GIACOMINI

SITE

Drug Metab Dispos. 2021 ;In press. Emerging roles of the Human Solute Carrier 22 family. Yee SW, Giacomini KM. PubMed

Pharm Res. 2022 ;In press. High throughput screening of a prescription drug library for inhibitors of Organic Cation Transporter 3, OCT3. Chen EC, Matsson P, Azimi M, Zhou X, Handin N, Yee SW, Artursson P, Giacomini KM. PubMed

Clin Pharmacol Ther. 2022 ;In press. The Clinical Pharmacogenetics Implementation Consortium Guideline for SLCO1B1, ABCG2, and CYP2C9 genotypes and statin-associated musculoskeletal symptoms. Cooper-DeHoff RM, Niemi M, Ramsey LB, Luzum JA, Tarkiainen EK, Straka RJ, Gong L, Tuteja S, Wilke RA, Wadelius M, Larson EA, Roden DM, Klein TE, Yee SW, Krauss RM, Turner RM, Palaniappan L, Gaedigk A, Giacomini KM, Caudle KE, Voora D. PubMed

Diabetes Care. 2021;44:2673-2682. Genome-Wide Meta-analysis identifies genetic variants associated with glycemic response to Sulfonylureas.  Dawed AY, Yee SW, Zhou K, van Leeuwen N, Zhang Y, Siddiqui MK, Etheridge A, Innocenti F, Xu F, Li JH, Beulens JW, van der Heijden AA, Slieker RC, Chang YC, Mercader JM, Kaur V, Witte JS, Lee MTM, Kamatani Y, Momozawa Y, Kubo M, Palmer CNA, Florez JC, Hedderson MM, 't Hart LM, Giacomini KM, Pearson ER. PubMed

AAPS J. 2021;23:106. Interaction of commonly used oral molecular excipients with P-glycoprotein. Bajaj R, Chong LB, Zou L, Tsakalozou E, Ni Z, Giacomini KM, Kroetz DL. PubMed

Clin Pharmacol Ther. 2021;110:559-562. Advancing precision medicine through the new Pharmacogenomics Global Research Network. Giacomini KM, Karnes JH, Crews KR, Monte AA, Murphy WA, Oni-Orisan A, Ramsey LB, Yang JJ, Whirl-Carrillo M. PubMed

Clin Transl Sci. 2021;14:1431-1443. Oxypurinol pharmacokinetics and pharmacodynamics in healthy volunteers: Influence of BCRP Q141K polymorphism and patient characteristics. Vora B, Brackman DJ, Zou L, Garcia-Cremades M, Sirota M, Savic RM, Giacomini KM. PubMed

Am J Hum Genet. 2021;108:535-548. Opportunities and challenges for the computational interpretation of rare variation in clinically important genes. McInnes G, Sharo AG, Koleske ML, Brown JEH, Norstad M, Adhikari AN, Wang S, Brenner SE, Halpern J, Koenig BA, Magnus DC, Gallagher RC, Giacomini KM, Altman RB. PubMed

Clin Pharmacol Ther. 2021;In press. Drugs in COVID19 clinical trials: Predicting transporter-mediated drug-drug interactions using in vitro assays and real-world data. Yee SW, Vora B, Oskotsky TT, Zou L, Jakobsen S, Enogieru OJ, Koleske ML, Kosti I, Rödin M, Sirota M, Giacomini KM. PubMed

Br J Pharmacol. 2021;178:1459-1474. Characterization of cytochrome P450 (CYP) 2D6 drugs as substrates of human organic cation transporters and multidrug and toxin extrusion proteins. Neul C, Hofmann U, Schaeffeler E, Winter S, Klein K, Giacomini KM, Eichelbaum M, Schwab M, Nies AT. PubMed 

FASEB J. 2020;34:15734-15752. Deorphaning a solute carrier 22 family member, SLC22A15, through functional genomic studies. Yee SW, Buitrago D, Stecula A, Ngo HX, Chien HC, Zou L, Koleske ML, Giacomini KM. PubMed

J Pharm Sci. 2021;110:2-11. Matsson P, Baranczewski P, Giacomini KM, Andersson TB, Palm J, Palm K, Charman WN, Bergström CAS. A Tribute to Professor Per Artursson - Scientist, explorer, mentor, innovator, and giant in Pharmaceutical Research. PubMed

J Pharm Sci. 2021;110:347-353. Drug metabolites potently inhibit renal Organic Anion Transporters, OAT1 and OAT3. Zou L, Matsson P, Stecula A, Ngo HX, Zur AA, Giacomini KM. PubMed

Sci Transl Med. 2020;12:eaax2550. Scientific considerations for global drug development. Wilson JL, Cheung KWK, Lin L, Green EAE, Porrás AI, Zou L, Mukanga D, Akpa PA, Darko DM, Yuan R, Ding S, Johnson WCN, Lee HA, Cooke E, Peck CC, Kern SE, Hartman D, Hayashi Y, Marks PW, Altman RB, Lumpkin MM, Giacomini KM, Blaschke TF. PubMed

Proc Natl Acad Sci USA. 2020;117:16009-16018. Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Zou L, Spanogiannopoulos P, Pieper LM, Chien HC, Cai W, Khuri N, Pottel J, Vora B, Ni Z, Tsakalozou E, Zhang W, Shoichet BK, Giacomini KM, Turnbaugh PJ. PubMed

Clin Pharmacol Ther. 2020;107:1045-1047. Novel technologies enable mechanistic understanding and modeling of drug exposure and response. Giacomini KM. PubMed

Mol Pharm. 2020;17:748-756. Interactions of oral molecular excipients with Breast Cancer Resistance Protein, BCRP. Zou L, Pottel J, Khuri N, Ngo HX, Ni Z, Tsakalozou E, Warren MS, Huang Y, Shoichet BK, Giacomini KM. PubMed

Clin Pharmacol Ther. 2020;107:96-101. Expanding precompetitive multisector collaborations to advance drug development and pharmacogenomics. Yee SW, Do TP, Huang SM, Krauss RM, Kusuhara H, Sugiyama Y, Unadkat JD, Giacomini KM. PubMed

Am J Clin Nutr. 2020;111:110-121. Drug-nutrient interactions: discovering prescription drug inhibitors of the thiamine transporter ThTR-2 (SLC19A3). Vora B, Green EAE, Khuri N, Ballgren F, Sirota M, Giacomini KM. PubMed

Clin Pharmacol Ther. 2020;107:57-61. Global pharmacogenomics within Precision Medicine: Challenges and opportunities. Chenoweth MJ, Giacomini KM, Pirmohamed M, Hill SL, van Schaik RHN, Schwab M, Shuldiner AR, Relling MV, Tyndale RF. PubMed

PLoS Genet. 2019;15:e1008208. Unraveling the functional role of the orphan solute carrier, SLC22A24 in the transport of steroid conjugates through metabolomic and genome-wide association studies. Yee SW, Stecula A, Chien HC, Zou L, Feofanova EV, van Borselen M, Cheung KWK, Yousri NA, Suhre K, Kinchen JM, Boerwinkle E, Irannejad R, Yu B, Giacomini KM. PubMed

Clin Pharmacol Ther. 2019;106:1083-1092. A comprehensive analysis of ontogeny of renal drug transporters: mRNA analyses, quantitative proteomics and localization. Wun Kathy Cheung K, van Groen BD, Spaans E, van Borselen MD, C J M de Bruijn A, Simons-Oosterhuis Y, Tibboel D, Samsom JN, Verdijk RM, Smeets B, Zhang L, Huang SM, Giacomini KM, de Wildt SN. PubMed

Clin Transl Sci. 2019;12:388-399. Organic Anion Transporter Polypeptide 1B1 polymorphism modulates the extent of Drug-Drug Interaction and associated biomarker levels in healthy volunteers. Yee SW, Giacomini MM, Shen H, Humphreys WG, Horng H, Brian W, Lai Y, Kroetz DL, Giacomini KM. PubMed

Hum Mutat. 2019;40:983-995. Functional and structural analysis of rare SLC2A2 variants associated with Fanconi-Bickel syndrome and metabolic traits. Enogieru OJ, Ung PMU, Yee SW, Schlessinger A, Giacomini KM. PubMed

Clin Pharmacol Ther. 2019;106:623-631. Genome-Wide Association and Functional Studies Reveal Novel Pharmacological Mechanisms for Allopurinol. Brackman DJ, Yee SW, Enogieru OJ, Shaffer C, Ranatunga D, Denny JC, Wei WQ, Kamatani Y, Kubo M, Roden DM, Jorgenson E, Giacomini KM. PubMed

Clin Pharmacol Ther. 2019;105:815-818. Research projects supported by the University of California, San Francisco-Stanford Center of Excellence in regulatory science and innovation. Giacomini KM, Lin L, Altman RB. PubMed

PLoS Biol. 2019;17:e2006571. Organic cation transporter 3 (Oct3) is a distinct catecholamines clearance route in adipocytes mediating the beiging of white adipose tissue. Song W, Luo Q, Zhang Y, Zhou L, Liu Y, Ma Z, Guo J, Huang Y, Cheng L, Meng Z, Li Z, Zhang B, Li S, Yee SW, Fan H, Li P, Giacomini KM, Chen L. PubMed

Clin Pharmacol Ther. 2019;105:323-325. Impact of pharmaceutical excipients on oral drug absorption: A focus on intestinal drug transporters. Zou L, Ni Z, Tsakalozou E, Giacomini KM. PubMed

Clin Pharmacol Ther. 2018;104:836-864. Clinical probes and endogenous biomarkers as substrates for transporter Drug-Drug Interaction evaluation: Perspectives from the International Transporter Consortium. Chu X, Liao M, Shen H, Yoshida K, Zur AA, Arya V, Galetin A, Giacomini KM, Hanna I, Kusuhara H, Lai Y, Rodrigues D, Sugiyama Y, Zamek-Gliszczynski MJ, Zhang L; International Transporter Consortium. PubMed

Clin Pharmacol Ther. 2018;104:766-771. The International Transporter Consortium: Summarizing advances in the role of transporters in drug development. Giacomini KM, Galetin A, Huang SM. PubMed

Clin Pharmacol Ther. 2018;104:890-899. Transporters in drug development: 2018 ITC recommendations for transporters of emerging clinical importance. Zamek-Gliszczynski MJ, Taub ME, Chothe PP, Chu X, Giacomini KM, Kim RB, Ray AS, Stocker SL, Unadkat JD, Wittwer MB, Xia C, Yee SW, Zhang L, Zhang Y; International Transporter Consortium. PubMed

Adv Pharmacol. 2018;83:361-389. Pharmacogenetics of antidiabetic drugs. Srinivasan S, Yee SW, Giacomini KM. PubMed

Clin Pharmacol Ther. 2018;104:781-784. ITC Commentary on Metformin clinical drug-drug interaction study design that enables an efficacy- and safety-based dose adjustment decision. Zamek-Gliszczynski MJ, Chu X, Cook JA, Custodio JM, Galetin A, Giacomini KM, Lee CA, Paine MF, Ray AS, Ware JA, Wittwer MB, Zhang L; International Transporter Consortium. PubMed

Mol Pharmacol. 2018;94:689-699. Molecular mechanisms for species differences in Organic Anion Transporter 1, OAT1: Implications for renal drug toxicity.Zou L, Stecula A, Gupta A, Prasad B, Chien HC, Yee SW, Wang L, Unadkat JD, Stahl SH, Fenner KS, Giacomini KM. PubMed

Clin Pharmacol Ther. 2018;104:803-817. Influence of transporter polymorphisms on drug disposition and response: A perspective from the International Transporter Consortium. Yee SW, Brackman DJ, Ennis EA, Sugiyama Y, Kamdem LK, Blanchard R, Galetin A, Zhang L, Giacomini KM. PubMed

Clin Pharmacol Ther. 2018;103:758-760. Emerging clinical importance of hepatic Organic Cation Transporter 1 (OCT1) in drug pharmacokinetics, dynamics, pharmacogenetic variability, and drug interactions. Zamek-Gliszczynski MJ, Giacomini KM, Zhang L. PubMed

Clin Pharmacol Ther. 2018;103:233-242. Reverse translational research of ABCG2 (BCRP) in human disease and drug response. Brackman DJ, Giacomini KM. PubMed

Pharmacogenet Genomics. 2017;27:420-427. PharmGKB summary: very important pharmacogene information for ABCG2. Fohner AE, Brackman DJ, Giacomini KM, Altman RB, Klein TE. PubMed

Clin Pharmacol Ther. 2017;102:897-902. New Pharmacogenomics Research Network: An open community catalyzing research and translation in precision medicine. Relling MV, Krauss RM, Roden DM, Klein TE, Fowler DM, Terada N, Lin L, Riel-Mehan M, Do TP, Kubo M, Yee SW, Johnson GT, Giacomini KM. PubMed

Clin Pharmacol Ther. 2018;103:485-492. PBPK modeling of the effect of reduced kidney function on the pharmacokinetics of drugs excreted renally by Organic Anion Transporters. Hsueh CH, Hsu V, Zhao P, Zhang L, Giacomini KM, Huang SM. PubMed

J Chem Inf Model. 2017;57:1402-1413. Computational Discovery and Experimental Validation of Inhibitors of the Human Intestinal Transporter OATP2B1. Khuri N1, Zur AA, Wittwer MB, Lin L, Yee SW, Sali A2, Giacomini KM. PubMed

J Pharm Sci. 2017;106:2245-2250. Transporters involved in Metformin pharmacokinetics and treatment response. Liang X, Giacomini KM. PubMed

J Med Chem. 2017;60:2685-2696. Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A). Chen EC, Khuri N, Liang X, Stecula A, Chien HC, Yee SW, Huang Y, Sali A, Giacomini KM. PubMed

Clin Adv Hematol Oncol. 2016;14:869-871. The use of drug transporters as therapeutic targets. Giacomini KM. PubMed

PLoS Genet. 2016;12:e1006449. Genomic characterization of Metformin hepatic response. Luizon MR, Eckalbar WL, Wang Y, Jones SL, Smith RP, Laurance M, Lin, Gallins PJ, Etheridge AS, Wright F, Zhou Y, Molony C, Innocenti F, Yee SW, Giacomini KM, Ahituv N. PubMed

Nat Rev Drug Discov. 2017;16:1. Genome-wide association studies of drug response and toxicity: an opportunity for genome medicine. Giacomini KM, Yee SW, Mushiroda T, Weinshilboum RM, Ratain MJ, Kubo M. PubMed

J Pharm Sci. 2017 May; in press. The effect of uremic solutes on the Organic Cation Transporter 2, OCT2. Kathy Cheung KW, Hsueh CH, Zhao P, Meyer TW, Zhang L, Huang SM, Giacomini KM. PubMed

J Med Chem. 2017;60:2685-2696. Discovery of competitive and noncompetitive ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1). Chen EC, Khuri N, Liang X, Stecula A, Chien HC, Yee SW, Huang Y, Sali A, Giacomini KM. PubMed

Mol Pharm. 2016;13:3130-40. Identification and quantitative assessment of uremic solutes as inhibitors of renal Organic Anion Transporters, OAT1 and OAT3. Hsueh CH, Yoshida K, Zhao P, Meyer TW, Zhang L, Huang SM, Giacomini KM. PubMed

Clin Pharmacol Ther. 2016;100:524-536. Metabolomic and genome-wide association studies reveal potential endogenous biomarkers for OATP1B1. Yee SW, Giacomini MM, Hsueh CH1, Weitz D, Liang X, Goswami S, Kinchen JM, Coelho A, Zur AA, Mertsch K, Brian W, Kroetz DL, Giacomini KM. PubMed

Drug Metab Dispos. 2016;44:356-64. Rapid method to determine intracellular drug concentrations in cellular uptake assays: application to Metformin in Organic CationTransporter 1-transfected Human Embryonic Kidney 293 Cells. Chien HC, Zur AA, Maurer TS, Yee SW, Tolsma J, Jasper P, Scott DO, Giacomini KM. PubMed

Mol Pharm. 2015;12:4301-10. Metformin Is a substrate and Inhibitor of the Human Thiamine Transporter, THTR-2 (SLC19A3). Liang X, Chien HC, Yee SW, Giacomini MM, Chen EC, Piao M, Hao J, Twelves J, Lepist EI, Ray AS, Giacomini KM. PubMed

Clin Pharmacokinet. 2016;55:495-506. The effect of Nizatidine, a MATE2K selective inhibitor, on the pharmacokinetics and harmacodynamics of Metformin in healthy volunteers. Morrissey KM, Stocker SL, Chen EC, Castro RA, Brett CM, Giacomini KM. PubMed

J Pharmacokinet Pharmacodyn. 2015;42:463-75. Prediction and validation of enzyme and transporter off-targets for metformin. Yee SW, Lin L, Merski M, Keiser MJ, Gupta A, Zhang Y, Chien HC, Shoichet BK, Giacomini KM. PubMed

Nat Rev Drug Discov. 2015;14:543-60. SLC transporters as therapeutic targets: emerging opportunities. Lin L, Yee SW, Kim RB, Giacomini KM. PubMed

Clin Pharmacol Ther. 2015;97:518-25. Genome-wide association study identifies ABCG2 (BCRP) as an allopurinol transporter and a determinant of drug response. Wen CC, Yee SW, Liang X, Hoffmann TJ, Kvale MN, Banda Y, Jorgenson E, Schaefer C, Risch N, Giacomini KM. PubMed

Cell Cycle. 2015;14:283-4. OCT1 in hepatic steatosis and thiamine disposition. Chen L, Yee SW, Giacomini KM. PubMed

Clin Pharmacokinet. 2014;53:283-293. Towards quantitation of the effects of renal impairment and probenecid inhibition on kidney uptake and efflux transporters, using physiologically based pharmacokinetic modelling and simulations. Hsu V, de L T Vieira M, Zhao P, Zhang L, Zheng JH, Nordmark A, Berglund EG, Giacomini KM, Huang SM. PubMed

Clin Pharmacol Ther. 2013;94:636-9. Profiling solute carrier transporters in the human blood-brain barrier. Geier EG, Chen EC, Webb A, Papp AC, Yee SW, Sadee W, Giacomini KM. PubMed

Clin Pharmacol Ther. 2013;94:23-6. International Transporter Consortium commentary on clinically important transporter polymorphisms. Giacomini KM, Balimane PV, Cho SK, Eadon M, Edeki T, Hillgren KM, Huang SM, Sugiyama Y, Weitz D, Wen Y, Xia CQ, Yee SW, Zimdahl H, Niemi M; International Transporter Consortium. PubMed

Clin Pharmacol Ther. 2013;94:19-23. SLC classification: an update. Schlessinger A, Yee SW, Sali A, Giacomini KM. PubMed

Clin Pharmacol Ther. 2013;94:3-9. doi: 10.1038/clpt.2013.86. Transporters in drug development and clinical pharmacology. Giacomini KM, Huang SM. PubMed

J Pharm Sci. 2013;102:3451-7. Reduced renal clearance of cefotaxime in asians with a low-frequency polymorphism of OAT3 (SLC22A8). Yee SW, Nguyen AN, Brown C, Savic RM, Zhang Y, Castro RA, Cropp CD, Choi JH, Singh D, Tahara H, Stocker SL, Huang Y, Brett CM, Giacomini KM. PubMed

Clin Pharmacol Ther. 2013;94:52-63. Emerging transporters of clinical importance: an update from the International Transporter Consortium. Hillgren KM, Keppler D, Zur AA, Giacomini KM, Stieger B, Cass CE, Zhang L; International Transporter Consortium. PubMed

Curr Top Med Chem. 2013;13:843-56. Molecular modeling and ligand docking for solute carrier (SLC) transporters. Schlessinger A, Khuri N, Giacomini KM, Sali A. PubMed

Proc Natl Acad Sci U S A. 2013;110:5480-5. Structure-based ligand discovery for the Large-neutral Amino Acid Transporter 1, LAT-1. Geier EG, Schlessinger A, Fan H, Gable JE, Irwin JJ, Sali A, Giacomini KM. PubMed

Mol Pharm. 2013;10:650-63. Gene expression profiling of transporters in the solute carrier and ATP-binding cassette superfamilies in human eye substructures. Dahlin A, Geier E, Stocker SL, Cropp CD, Grigorenko E, Bloomer M, Siegenthaler J, Xu L, Basile AS, Tang-Liu DD, Giacomini KM. PubMed

Clin Pharmacol Ther. 2013;93:186-94. The effect of novel promoter variants in MATE1 and MATE2 on the pharmacokinetics and pharmacodynamics of metformin. Stocker SL, Morrissey KM, Yee SW, Castro RA, Xu L, Dahlin A, Ramirez AH, Roden DM, Wilke RA, McCarty CA, Davis RL, Brett CM, Giacomini KM. PubMed

Annu Rev Pharmacol Toxicol. 2013;53:503-29. Renal transporters in drug development. Morrissey KM, Stocker SL, Wittwer MB, Xu L, Giacomini KM. PubMed

Clin Pharmacol Ther. 2012;92:553-6. Highlights from the International Transporter Consortium second workshop. Zamek-Gliszczynski MJ, Hoffmaster KA, Tweedie DJ, Giacomini KM, Hillgren KM. PubMed

Clin Pharmacol Ther. 2012;92:545-6. The UCSF-FDA TransPortal: a public drug transporter database. Morrissey KM1, Wen CC, Johns SJ, Zhang L, Huang SM, Giacomini KM. PubMed

Nat Rev Drug Discov. 2010;9:215-36. Membrane transporters in drug development. International Transporter Consortium, Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, Hoffmaster KA, Ishikawa T, Keppler D, Kim RB, Lee CA, Niemi M, Polli JW, Sugiyama Y, Swaan PW, Ware JA, Wright SH, Yee SW, Zamek-Gliszczynski MJ, Zhang L. PubMed