Research Summary

I am a world-renowned pharmacologist with many years of research experience particularly focused on transporter biology and pharmacogenomics. My research is focused on influx transporters, especially influx transporters involved in drug disposition and targeting. In the early 2000s, we began a comprehensive research program focused on the pharmacogenomics of membrane transporters. We published many papers ranging from functional genomics of transporter polymorphisms to clinical studies elucidating the role of transporter polymorphisms on clinical drug response. Our NIH-funded center, the Pharmacogenomics of Membrane Transporters Center, part of the NIH Pharmacogenomics Research Network, is widely recognized as the leading research unit in the world for the discovery, functional characterization and clinical relevance of polymorphisms in drug transporters. We have been leaders in the field of human genetic studies focused on metformin with a particular emphasis on membrane transporters.

Most recently, I am a co-Director of a FDA grant to establish a Center with education, exchange, and collaborative research programs that will greatly advance the ability of the FDA to evaluate and approve safe and effective drugs. This is a collaborative program between Stanford and UCSF that will develop quantitative and computer-based methods for the evaluation of new drug products. Importantly, research will focus on issues of bioequivalence between generic drug products including metformin tablets.

Research Funding

  • September 19, 2023 - June 30, 2028 - Transporter Elucidation Center at the University of California, San Francisco , Co-Investigator . Sponsor: NIH, Sponsor Award ID: UC2HD113474
  • April 1, 2021 - March 31, 2025 - Characterizing the physiological and pharmacological roles of SLC22A24 , Principal Investigator . Sponsor: NIH, Sponsor Award ID: R01GM139875
  • September 25, 2015 - July 31, 2024 - Discovery of Pharmacogenomic Biomarkers for OATP1B1 and OATP1B3 , Principal Investigator . Sponsor: NIH, Sponsor Award ID: R01GM117163
  • September 15, 2016 - August 31, 2023 - UCSF-Stanford Center of Excellence in Regulatory Science and Innovation , Principal Investigator . Sponsor: NIH, Sponsor Award ID: U01FD005978
  • July 15, 2015 - June 30, 2020 - PGRN Administrative Coordination Hub, ACH (PGRN) , Principal Investigator . Sponsor: NIH/NIGMS, Sponsor Award ID: U24GM115370
  • September 20, 2014 - July 31, 2018 - Role of ABCG2 in the disposition and anti-hyperuricemic effects of allopurinol , Principal Investigator . Sponsor: NIH, Sponsor Award ID: R01DK103729
  • April 15, 2014 - March 31, 2017 - UCSF-Stanford Center of Excellence in Regulatory Science and Innovation , Principal Investigator . Sponsor: NIH, Sponsor Award ID: U01FD004979
  • September 30, 2010 - June 30, 2016 - Center for Structure of Membrane Proteins , Co-Investigator . Sponsor: NIH, Sponsor Award ID: U54GM094625
  • April 1, 2000 - June 30, 2015 - Pharmacogenomics of Membrane Transporters , Principal Investigator . Sponsor: NIH, Sponsor Award ID: U19GM061390
  • February 1, 2009 - September 30, 2013 - A Comprehensive Platform for Transporter Mediated Drug-Drug Interaction Studies , Principal Investigator . Sponsor: NIH, Sponsor Award ID: R44GM086970
  • June 1, 1976 - September 14, 2012 - Resource for Biocomputing, Visualization, and Informatics , Co-Investigator . Sponsor: NIH/NCRR, Sponsor Award ID: P41RR001081
  • April 4, 1986 - May 31, 2012 - Cellular Mechanisms of Drug Elimination , Principal Investigator . Sponsor: NIH, Sponsor Award ID: R01GM036780
  • April 1, 2000 - July 14, 2010 - Pharmacogenetics of Membrane Transporters , Principal Investigator . Sponsor: NIH, Sponsor Award ID: U01GM061390
  • December 1, 1974 - March 31, 2009 - General Clinical Research Center , Co-Investigator . Sponsor: NIH, Sponsor Award ID: M01RR000079
  • October 1, 1974 - November 30, 2007 - General Clinical Research Center , Co-Investigator . Sponsor: NIH, Sponsor Award ID: M01RR000083
  • January 1, 1991 - December 31, 2003 - CELLULAR MECHANISMS OF DRUG TRANSPORT IN CHOROID PLEXUS , Principal Investigator . Sponsor: NIH, Sponsor Award ID: R01GM042230
  • August 1, 1997 - July 31, 2001 - MOLECULAR BASIS OF DRUG TRANSPORT IN THE INTESTINE , Principal Investigator . Sponsor: NIH, Sponsor Award ID: R01GM057656
  • August 1, 1979 - July 31, 1998 - PHARMACOKINETICS/PHARMACODYNAMICS , Co-Investigator . Sponsor: NIH, Sponsor Award ID: P50GM026691
  • January 1, 1992 - April 10, 2025 - MOLECULAR MECHANISMS OF DRUG TRANSPORT , Principal Investigator . Sponsor: NIH, Sponsor Award ID: F06TW001776
  • March 1, 1983 - June 30, 1989 - STEREOSELECTIVE PHARMACOKINETICS OF DRUGS IN THE KIDNEY , Principal Investigator . Sponsor: NIH, Sponsor Award ID: R01GM031254

Education

University of Houston, Houston, TX, B.S., 1973, Pharmacy
State University of New York at Buffalo, Buffalo, NY, Ph.D., 1979, Pharmaceutical Sciences
Stanford University, Stanford, CA, Postdoc, 1979-81, Pharmacology /Clinical Pharmacology

Honors & Awards

  • 2021
    Distinguished Pharmaceutical Scientist Award, American Association of Pharmaceutical Scientists (AAPS)
  • 2020
    Inaugural President, Pharmacogenomics Global Research Network (PGRN)
  • 2020
    Bernard B. Brodie Award in Drug Metabolism and Disposition Lecture, American Society for Pharmacology and Experimental Therapeutics (ASPET)
  • 2019
    Faculty Research Lecture Award in Translational Science, Academic Senate, UCSF
  • 2018
    Outstanding Mentor of the Year Award, American Foundation for Pharmaceutical Education (AFPE)
  • 2018
    Volwiler Research Achievement Award, American Association of Colleges of Pharmacy (AACP)
  • 2016
    Honorary Doctorate Degree Uppsala University (UU)
  • 2011
    Scheele Award, Swedish Academy of Pharmaceutical Sciences (SPS)
  • 2009
    Rawls-Palmer Progress in Medicine Award, American Society for Clinical Pharmacology and Therapeutics (ASCPT)
  • 2006
    Elected Member, National Academy of Medicine (NAM)

Selected Publications

  1. Ramamoorthy A, Younis I, Wen YF, Mehanna M, Giacomini KM, van der Graaf PH. Therapeutic Orphan No More: Role for Clinical Pharmacology and Translational Science in Developing Therapeutics for Rare and Neglected Diseases. Clin Pharmacol Ther. 2024 Dec; 116(6):1363-1368.  View on PubMed
  2. Major TJ, Takei R, Matsuo H, Leask MP, Sumpter NA, Topless RK, Shirai Y, Wang W, Cadzow MJ, Phipps-Green AJ, Li Z, Ji A, Merriman ME, Morice E, Kelley EE, Wei WH, McCormick SPA, Bixley MJ, Reynolds RJ, Saag KG, Fadason T, Golovina E, O'Sullivan JM, Stamp LK, Dalbeth N, Abhishek A, Doherty M, Roddy E, Jacobsson LTH, Kapetanovic MC, Melander O, Andrés M, Pérez-Ruiz F, Torres RJ, Radstake T, Jansen TL, Janssen M, Joosten LAB, Liu R, Gaal OI, Crisan TO, Rednic S, Kurreeman F, Huizinga TWJ, Toes R, Lioté F, Richette P, Bardin T, Ea HK, Pascart T, McCarthy GM, Helbert L, Stiburková B, Tausche AK, Uhlig T, Vitart V, Boutin TS, Hayward C, Riches PL, Ralston SH, Campbell A, MacDonald TM, FAST Study Group, Nakayama A, Takada T, Nakatochi M, Shimizu S, Kawamura Y, Toyoda Y, Nakaoka H, Yamamoto K, Matsuo K, Shinomiya N, Ichida K, Japan Gout Genomics Consortium, Lee C, Asia Pacific Gout Consortium, Bradbury LA, Brown MA, Robinson PC, Buchanan RRC, Hill CL, Lester S, Smith MD, Rischmueller M, Choi HK, Stahl EA, Miner JN, Solomon DH, Cui J, Giacomini KM, Brackman DJ, Jorgenson EM, GlobalGout Genetics Consortium, Liu H, Susztak K, 23andMe Research Team, Shringarpure S, So A, Okada Y, Li C, Shi Y, Merriman TR. Publisher Correction: A genome-wide association analysis reveals new pathogenic pathways in gout. Nat Genet. 2024 Nov; 56(11):2577.  View on PubMed
  3. Major TJ, Takei R, Matsuo H, Leask MP, Sumpter NA, Topless RK, Shirai Y, Wang W, Cadzow MJ, Phipps-Green AJ, Li Z, Ji A, Merriman ME, Morice E, Kelley EE, Wei WH, McCormick SPA, Bixley MJ, Reynolds RJ, Saag KG, Fadason T, Golovina E, O'Sullivan JM, Stamp LK, Dalbeth N, Abhishek A, Doherty M, Roddy E, Jacobsson LTH, Kapetanovic MC, Melander O, Andrés M, Pérez-Ruiz F, Torres RJ, Radstake T, Jansen TL, Janssen M, Joosten LAB, Liu R, Gaal OI, Crisan TO, Rednic S, Kurreeman F, Huizinga TWJ, Toes R, Lioté F, Richette P, Bardin T, Ea HK, Pascart T, McCarthy GM, Helbert L, Stiburková B, Tausche AK, Uhlig T, Vitart V, Boutin TS, Hayward C, Riches PL, Ralston SH, Campbell A, MacDonald TM, FAST Study Group, Nakayama A, Takada T, Nakatochi M, Shimizu S, Kawamura Y, Toyoda Y, Nakaoka H, Yamamoto K, Matsuo K, Shinomiya N, Ichida K, Japan Gout Genomics Consortium, Lee C, Asia Pacific Gout Consortium, Bradbury LA, Brown MA, Robinson PC, Buchanan RRC, Hill CL, Lester S, Smith MD, Rischmueller M, Choi HK, Stahl EA, Miner JN, Solomon DH, Cui J, Giacomini KM, Brackman DJ, Jorgenson EM, GlobalGout Genetics Consortium, Liu H, Susztak K, 23andMe Research Team, Shringarpure S, So A, Okada Y, Li C, Shi Y, Merriman TR. A genome-wide association analysis reveals new pathogenic pathways in gout. Nat Genet. 2024 Nov; 56(11):2392-2406.  View on PubMed
  4. Giacomini KM, van der Graaf PH. Is Pharmacogenetic Testing a Vital Tool for Enhancing Therapeutic Management of Patients Worldwide? Clin Pharmacol Ther. 2024 Oct; 116(4):885-889.  View on PubMed
  5. Yee SW, Wang J, Giacomini KM. Rare Diseases Linked to Mutations in Vitamin Transporters Expressed in the Human Blood-Brain Barrier. Clin Pharmacol Ther. 2024 Dec; 116(6):1513-1520.  View on PubMed
  6. Zhou X, Azimi M, Handin N, Riselli A, Vora B, Chun E, Yee SW, Artursson P, Giacomini KM. Proteomic Profiling Reveals Age-Related Changes in Transporter Proteins in the Human Blood-Brain Barrier. bioRxiv. 2024 Jul 27.  View on PubMed
  7. Patterson ME, Ellingrod VL, Feola DJ, Kunda NK, Mei KC, Oestreich JH, Farrell DF, Giacomini KM. Report of the 2023-2024 AACP Research and Graduate Affairs Committee. Am J Pharm Educ. 2024 Aug; 88(8):100745.  View on PubMed
  8. Yee SW, Ferrández-Peral L, Alentorn-Moron P, Fontsere C, Ceylan M, Koleske ML, Handin N, Artegoitia VM, Lara G, Chien HC, Zhou X, Dainat J, Zalevsky A, Sali A, Brand CM, Wolfreys FD, Yang J, Gestwicki JE, Capra JA, Artursson P, Newman JW, Marquès-Bonet T, Giacomini KM. Illuminating the function of the orphan transporter, SLC22A10, in humans and other primates. Nat Commun. 2024 May 23; 15(1):4380.  View on PubMed
  9. Silva DB, Trinidad M, Ljungdahl A, Revalde JL, Berguig GY, Wallace W, Patrick CS, Bomba L, Arkin M, Dong S, Estrada K, Hutchinson K, LeBowitz JH, Schlessinger A, Johannesen KM, Møller RS, Giacomini KM, Froelich S, Sanders SJ, Wuster A. Haploinsufficiency underlies the neurodevelopmental consequences of SLC6A1 variants. Am J Hum Genet. 2024 06 06; 111(6):1222-1238.  View on PubMed
  10. Kulkarni CP, Yang J, Koleske ML, Lara G, Alam K, Raw A, Rege B, Zhao L, Lu D, Zhang L, Yu LX, Lionberger RA, Giacomini KM, Kroetz DL, Yee SW. Effect of Antioxidants in Medicinal Products on Intestinal Drug Transporters. Pharmaceutics. 2024 May 10; 16(5).  View on PubMed
  11. Yee SW, Macdonald CB, Mitrovic D, Zhou X, Koleske ML, Yang J, Buitrago Silva D, Rockefeller Grimes P, Trinidad DD, More SS, Kachuri L, Witte JS, Delemotte L, Giacomini KM, Coyote-Maestas W. The full spectrum of SLC22 OCT1 mutations illuminates the bridge between drug transporter biophysics and pharmacogenomics. Mol Cell. 2024 May 16; 84(10):1932-1947.e10.  View on PubMed
  12. Cater RJ, Mukherjee D, Gil-Iturbe E, Erramilli SK, Chen T, Koo K, Santander N, Reckers A, Kloss B, Gawda T, Choy BC, Zhang Z, Katewa A, Larpthaveesarp A, Huang EJ, Mooney SWJ, Clarke OB, Yee SW, Giacomini KM, Kossiakoff AA, Quick M, Arnold T, Mancia F. Structural and molecular basis of choline uptake into the brain by FLVCR2. Nature. 2024 May; 629(8012):704-709.  View on PubMed
  13. Wu B, Yee SW, Xiao S, Xu F, Sridhar SB, Yang M, Hochstadt S, Cabral W, Lanfear DE, Hedderson MM, Giacomini KM, Williams LK. Genome-Wide Association Study Identifies Pharmacogenomic Variants Associated With Metformin Glycemic Response in African American Patients With Type 2 Diabetes. Diabetes Care. 2024 Feb 01; 47(2):208-215.  View on PubMed
  14. Zhao L, Giacomini KM, van der Graaf PH. Progress in Clinical Pharmacology in China: A Randomized Controlled Study to Advance Genotype-Guided Precision Medicine. Clin Pharmacol Ther. 2024 02; 115(2):169-172.  View on PubMed
  15. Galetin A, Brouwer KLR, Tweedie D, Yoshida K, Sjöstedt N, Aleksunes L, Chu X, Evers R, Hafey MJ, Lai Y, Matsson P, Riselli A, Shen H, Sparreboom A, Varma MVS, Yang J, Yang X, Yee SW, Zamek-Gliszczynski MJ, Zhang L, Giacomini KM. Membrane transporters in drug development and as determinants of precision medicine. Nat Rev Drug Discov. 2024 04; 23(4):255-280.  View on PubMed
  16. Ong JCL, Seng BJJ, Law JZF, Low LL, Kwa ALH, Giacomini KM, Ting DSW. Artificial intelligence, ChatGPT, and other large language models for social determinants of health: Current state and future directions. Cell Rep Med. 2024 01 16; 5(1):101356.  View on PubMed
  17. Hunt JP, Dubinsky S, McKnite AM, Cheung KWK, van Groen BD, Giacomini KM, de Wildt SN, Edginton AN, Watt KM. Maximum likelihood estimation of renal transporter ontogeny profiles for pediatric PBPK modeling. CPT Pharmacometrics Syst Pharmacol. 2024 04; 13(4):576-588.  View on PubMed
  18. Smith DM, Minichmayr IK, Standing JF, Giacomini KM, van der Graaf PH, Peck RW. Ensuring Transparency and Quality of Clinical Trial Reporting in Clinical Pharmacology & Therapeutics: Prospective Trial Registration and Compliance with Reporting Guidelines Are Required for all Clinical Trials. Clin Pharmacol Ther. 2023 12; 114(6):1153-1157.  View on PubMed
  19. Yee SW, Ferrández-Peral L, Alentorn P, Fontsere C, Ceylan M, Koleske ML, Handin N, Artegoitia VM, Lara G, Chien HC, Zhou X, Dainat J, Zalevsky A, Sali A, Brand CM, Capra JA, Artursson P, Newman JW, Marques-Bonet T, Giacomini KM. Illuminating the Function of the Orphan Transporter, SLC22A10 in Humans and Other Primates. Res Sq. 2023 Sep 14.  View on PubMed
  20. Michel ME, Wen CC, Yee SW, Giacomini KM, Hamdoun A, Nicklisch SCT. TICBase: Integrated Resource for Data on Drug and Environmental Chemical Interactions with Mammalian Drug Transporters. Clin Pharmacol Ther. 2023 12; 114(6):1293-1303.  View on PubMed

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