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

  • 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


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. Venkatakrishnan K, Brown KE, Giacomini KM, van der Graaf PH. Diversity, Equity, and Inclusion: Translating Clinical Pharmacology for All. Clin Pharmacol Ther. 2023 Mar; 113(3):457-461.  View on PubMed
  2. Li JH, Perry JA, Jablonski KA, Srinivasan S, Chen L, Todd JN, Harden M, Mercader JM, Pan Q, Dawed AY, Yee SW, Pearson ER, Giacomini KM, Giri A, Hung AM, Xiao S, Williams LK, Franks PW, Hanson RL, Kahn SE, Knowler WC, Pollin TI, Florez JC, Diabetes Prevention Program Research Group. Identification of Genetic Variation Influencing Metformin Response in a Multi-Ancestry Genome-Wide Association Study in the Diabetes Prevention Program (DPP). Diabetes. 2022 Dec 16.  View on PubMed
  3. Koleske ML, McInnes G, Brown JEH, Thomas N, Hutchinson K, Chin MY, Koehl A, Arkin MR, Schlessinger A, Gallagher RC, Song YS, Altman RB, Giacomini KM. Functional genomics of OCTN2 variants informs protein-specific variant effect predictor for Carnitine Transporter Deficiency. Proc Natl Acad Sci U S A. 2022 Nov 16; 119(46):e2210247119.  View on PubMed
  4. Giacomini KM, Huang SM. More Than Pharmacokinetics: Transporters in Clinical Pharmacology. Clin Pharmacol Ther. 2022 09; 112(3):423-426.  View on PubMed
  5. Giacomini KM, Yee SW, Koleske ML, Zou L, Matsson P, Chen EC, Kroetz DL, Miller MA, Gozalpour E, Chu X. New and Emerging Research on Solute Carrier and ATP Binding Cassette Transporters in Drug Discovery and Development: Outlook From the International Transporter Consortium. Clin Pharmacol Ther. 2022 09; 112(3):540-561.  View on PubMed
  6. Martinez MN, Sinko B, Wu F, Flanagan T, Borbás E, Tsakalozou E, Giacomini KM. A Critical Overview of the Biological Effects of Excipients (Part I): Impact on Gastrointestinal Absorption. AAPS J. 2022 05 02; 24(3):60.  View on PubMed
  7. 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, for MetGen Plus, for the DIRECT Consortium. Response to Comment on Dawed et al. Genome-Wide Meta-analysis Identifies Genetic Variants Associated With Glycemic Response to Sulfonylureas. Diabetes Care 2021;44:2673-2682. Diabetes Care. 2022 04 01; 45(4):e82-e83.  View on PubMed
  8. 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. The Clinical Pharmacogenetics Implementation Consortium Guideline for SLCO1B1, ABCG2, and CYP2C9 genotypes and Statin-Associated Musculoskeletal Symptoms. Clin Pharmacol Ther. 2022 05; 111(5):1007-1021.  View on PubMed
  9. Giacomini KM, van der Graaf PH. The Pandemic as a Catalyst for Disruptive Innovation in Clinical Pharmacology. Clin Pharmacol Ther. 2022 03; 111(3):529-532.  View on PubMed
  10. Chen EC, Matsson P, Azimi M, Zhou X, Handin N, Yee SW, Artursson P, Giacomini KM. High Throughput Screening of a Prescription Drug Library for Inhibitors of Organic Cation Transporter 3, OCT3. Pharm Res. 2022 Jul; 39(7):1599-1613.  View on PubMed
  11. Yee SW, Giacomini KM. Emerging Roles of the Human Solute Carrier 22 Family. Drug Metab Dispos. 2021 Dec 17.  View on PubMed
  12. 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, for MetGen Plus, for the DIRECT Consortium, MetGen Plus investigators:. Genome-Wide Meta-analysis Identifies Genetic Variants Associated With Glycemic Response to Sulfonylureas. Diabetes Care. 2021 12; 44(12):2673-2682.  View on PubMed
  13. Bajaj R, Chong LB, Zou L, Tsakalozou E, Ni Z, Giacomini KM, Kroetz DL. Interaction of Commonly Used Oral Molecular Excipients with P-glycoprotein. AAPS J. 2021 09 15; 23(5):106.  View on PubMed
  14. Giacomini KM, Karnes JH, Crews KR, Monte AA, Murphy WA, Oni-Orisan A, Ramsey LB, Yang JJ, Whirl-Carrillo M. Advancing Precision Medicine Through the New Pharmacogenomics Global Research Network. Clin Pharmacol Ther. 2021 09; 110(3):559-562.  View on PubMed
  15. Yee SW, Vora B, Oskotsky T, Zou L, Jakobsen S, Enogieru OJ, Koleske ML, Kosti I, R?din M, Sirota M, Giacomini KM. Drugs in COVID-19 Clinical Trials: Predicting Transporter-Mediated Drug-Drug Interactions Using In Vitro Assays and Real-World Data. Clin Pharmacol Ther. 2021 07; 110(1):108-122.  View on PubMed
  16. Vora B, Brackman DJ, Zou L, Garcia-Cremades M, Sirota M, Savic RM, Giacomini KM. Oxypurinol pharmacokinetics and pharmacodynamics in healthy volunteers: Influence of BCRP Q141K polymorphism and patient characteristics. Clin Transl Sci. 2021 07; 14(4):1431-1443.  View on PubMed
  17. 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. Opportunities and challenges for the computational interpretation of rare variation in clinically important genes. Am J Hum Genet. 2021 04 01; 108(4):535-548.  View on PubMed
  18. Enogieru OJ, Koleske ML, Vora B, Ngo H, Yee SW, Chatad D, Sirota M, Giacomini KM. The Effects of Genetic Mutations and Drugs on the Activity of the Thiamine Transporter, SLC19A2. AAPS J. 2021 03 01; 23(2):35.  View on PubMed
  19. Lavertu A, Vora B, Giacomini KM, Altman R, Rensi S. A New Era in Pharmacovigilance: Toward Real-World Data and Digital Monitoring. Clin Pharmacol Ther. 2021 05; 109(5):1197-1202.  View on PubMed
  20. Neul C, Hofmann U, Schaeffeler E, Winter S, Klein K, Giacomini KM, Eichelbaum M, Schwab M, Nies AT. Characterization of cytochrome P450 (CYP) 2D6 drugs as substrates of human organic cation transporters and multidrug and toxin extrusion proteins. Br J Pharmacol. 2021 03; 178(6):1459-1474.  View on PubMed

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