University of California San Francisco
Helen Diller Family Comprehensive Cancer Center
Kathleen Giacomini, PhD

Kathleen Giacomini, PhD

Professor and Co-Chair, Department of Bioengineering and Therapeutic Sciences; Professor, Departments of Biopharmaceutical Sciences, Pharmaceutical Chemistry, and Cellular & Molecular Pharmacology, UCSF

Cancer Center Program Memberships

Cancer Genetics

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.

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


Professional Experience

  • 1981-87
    Assistant Professor of Pharmacy/ Pharmaceutical Chem. & Pharmacology
  • 1987-91
    Associate Professor of Pharmacy/ Pharmaceutical Chem. & Pharmacology
  • 1998-2009
    Chair of the Department of Biopharmaceutical Sciences
  • 1992-present
    Professor of Biopharmaceutical Sciences, Pharmaceutical Chemistry, and Cellular & Molecular Pharmacology, UCSF
  • 2009-present
    Co-chair, Department of Bioengineering and Therapeutic Sciences, UCSF

Honors & Awards

  • 1973
    Rho Chi, Honorary Pharmacy Fraternity
  • 1983-84
    Long Foundation Award for Excellence in Teaching, School of Pharmacy, UCSF
  • 1984-85
    UCSF Nominee, Recognition Award for Young Scholars, American Association of University Women
  • 1985-86
    Distinguished Teaching Award, UCSF, Academic Senate
  • 1990
    Leon Goldberg Young Investigator Award, American Society for Clinical Pharmacology and Therapeutics
  • 1990-94
    Member of Pharmacological Science Review Committee; National Institutes of Health (GM)
  • 1990-94
    Member of Generic Drugs Advisory Committee; Food and Drug Administration
  • 1992
    Recipient, Fogarty International Fellowship; National Institutes of Health
  • 1993
    Elected Fellow, American Association of Pharmaceutical Scientists
  • 1994
    UCSF, Dr. Martin Luther King, Jr. Award for the Advancement of Women and Minorities
  • 1996-97
    Vice President, American Society for Clinical Pharmacology and Therapeutics
  • 1996-97
    UCSF, Chancellor's Award for the Advancement of Women
  • 1999
    Recognition Award for Distinguished Achievement of Filipino at UCSF
  • 1999
    International Pharmaceutical Federation (FIP), Pharmaceutical Scientist of the Year
  • 2001
    Elected Fellow, American Association for the Advancement of Science
  • 2002
    Distinguished Bill Abram's Lectureship (FDA)
  • 2002
    First Distinguished Gerhard Levy Lectureship (SUNY Buffalo)
  • 2002
    Speaker: State Legislative Presentation 'The Impact of the Human Genome Pronect on Drug Development and Use: Tailoring Drugs to Individuals'
  • 2005
    Paul Dawson Biotechnology Award, American Association of College of Pharmacy
  • 2006
    Distinguished Scientist in Drug Metabolism, American Association of Pharmaceutical Scientists
  • 2006
    Elected Member, Institute of Medicine
  • 2007
    International Pharmaceutical Sciences World Congress (PSWC) Research Achievement Award
  • 2007
    International Woman Scientist Award, Academy of Pharmaceutical Sciences and Technology, Japan
  • 2008
    Japan Society for the Promotion of Sciences (JSPS) Invitation Fellowship Program for Research in Japan
  • 2009
    Rawls-Palmer Progress in Medicine Award, American Society for Clinical Pharmacology and Therapeutics (ASCPT)
  • 2009
    UCSF Postdoctoral Scholars Association Outstanding Mentor Award
  • 2010
    American College of Clinical Pharmacy Therapeutic Frontiers Lecture Award
  • 2011
    Scheele Award, Swedish Academy of Pharmaceutical Sciences

Selected Publications

  1. Brackman DJ, Giacomini KM. Reverse Translational Research of ABCG2 (BCRP) in Human Disease and Drug Response. Clin Pharmacol Ther. 2018 Feb; 103(2):233-242.
    View on PubMed
  2. Fohner AE, Brackman DJ, Giacomini KM, Altman RB, Klein TE. PharmGKB summary: very important pharmacogene information for ABCG2. Pharmacogenet Genomics. 2017 11; 27(11):420-427.
    View on PubMed
  3. 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. New Pharmacogenomics Research Network: An Open Community Catalyzing Research and Translation in Precision Medicine. Clin Pharmacol Ther. 2017 Dec; 102(6):897-902.
    View on PubMed
  4. Hsueh CH, Hsu V, Zhao P, Zhang L, Giacomini KM, Huang SM. PBPK Modeling of the Effect of Reduced Kidney Function on the Pharmacokinetics of Drugs Excreted Renally by Organic Anion Transporters. Clin Pharmacol Ther. 2018 Mar; 103(3):485-492.
    View on PubMed
  5. Stecula A, Schlessinger A, Giacomini KM, Sali A. Human Concentrative Nucleoside Transporter 3 (hCNT3, SLC28A3) Forms a Cyclic Homotrimer. Biochemistry. 2017 07 11; 56(27):3475-3483.
    View on PubMed
  6. Khuri N, Zur AA, Wittwer MB, Lin L, Yee SW, Sali A, Giacomini KM. Computational Discovery and Experimental Validation of Inhibitors of the Human Intestinal Transporter OATP2B1. J Chem Inf Model. 2017 06 26; 57(6):1402-1413.
    View on PubMed
  7. Liang X, Giacomini KM. Transporters Involved in Metformin Pharmacokinetics and Treatment Response. J Pharm Sci. 2017 Sep; 106(9):2245-2250.
    View on PubMed
  8. Cheung KWK, Hsueh CH, Zhao P, Meyer TW, Zhang L, Huang SM, Giacomini KM. The Effect of Uremic Solutes on the Organic Cation Transporter 2. J Pharm Sci. 2017 Sep; 106(9):2551-2557.
    View on PubMed
  9. Chen EC, Khuri N, Liang X, Stecula A, Chien HC, Yee SW, Huang Y, Sali A, Giacomini KM. Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1). J Med Chem. 2017 Apr 13; 60(7):2685-2696.
    View on PubMed
  10. Dujic T, Zhou K, Yee SW, van Leeuwen N, de Keyser CE, Javorský M, Goswami S, Zaharenko L, Hougaard Christensen MM, Out M, Tavendale R, Kubo M, Hedderson MM, van der Heijden AA, Klimcáková L, Pirags V, Kooy A, Brøsen K, Klovins J, Semiz S, Tkác I, Stricker BH, Palmer C, 't Hart LM, Giacomini KM, Pearson ER. Variants in Pharmacokinetic Transporters and Glycemic Response to Metformin: A Metgen Meta-Analysis. Clin Pharmacol Ther. 2017 Jun; 101(6):763-772.
    View on PubMed
  11. Luizon MR, Eckalbar WL, Wang Y, Jones SL, Smith RP, Laurance M, Lin L, Gallins PJ, Etheridge AS, Wright F, Zhou Y, Molony C, Innocenti F, Yee SW, Giacomini KM, Ahituv N. Genomic Characterization of Metformin Hepatic Response. PLoS Genet. 2016 Nov; 12(11):e1006449.
    View on PubMed
  12. Giacomini KM, Yee SW, Mushiroda T, Weinshilboum RM, Ratain MJ, Kubo M. Genome-wide association studies of drug response and toxicity: an opportunity for genome medicine. Nat Rev Drug Discov. 2017 Jan; 16(1):1.
    View on PubMed
  13. Giacomini KM. The use of drug transporters as therapeutic targets. Clin Adv Hematol Oncol. 2016 Nov; 14(11):869-871.
    View on PubMed
  14. Irwin JJ, Pottel J, Zou L, Wen H, Zuk S, Zhang X, Sterling T, Shoichet BK, Lionberger R, Giacomini KM. A Molecular Basis for Innovation in Drug Excipients. Clin Pharmacol Ther. 2017 Mar; 101(3):320-323.
    View on PubMed
  15. Goswami S, Yee SW, Xu F, Sridhar SB, Mosley JD, Takahashi A, Kubo M, Maeda S, Davis RL, Roden DM, Hedderson MM, Giacomini KM, Savic RM. A Longitudinal HbA1c Model Elucidates Genes Linked to Disease Progression on Metformin. Clin Pharmacol Ther. 2016 Nov; 100(5):537-547.
    View on PubMed
  16. Yee SW, Giacomini MM, Hsueh CH, Weitz D, Liang X, Goswami S, Kinchen JM, Coelho A, Zur AA, Mertsch K, Brian W, Kroetz DL, Giacomini KM. Metabolomic and Genome-wide Association Studies Reveal Potential Endogenous Biomarkers for OATP1B1. Clin Pharmacol Ther. 2016 Nov; 100(5):524-536.
    View on PubMed
  17. Zur AA, Chien HC, Augustyn E, Flint A, Heeren N, Finke K, Hernandez C, Hansen L, Miller S, Lin L, Giacomini KM, Colas C, Schlessinger A, Thomas AA. LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates. Bioorg Med Chem Lett. 2016 10 15; 26(20):5000-5006.
    View on PubMed
  18. Hsueh CH, Yoshida K, Zhao P, Meyer TW, Zhang L, Huang SM, Giacomini KM. Identification and Quantitative Assessment of Uremic Solutes as Inhibitors of Renal Organic Anion Transporters, OAT1 and OAT3. Mol Pharm. 2016 09 06; 13(9):3130-40.
    View on PubMed
  19. Zhou K, Yee SW, Seiser EL, van Leeuwen N, Tavendale R, Bennett AJ, Groves CJ, Coleman RL, van der Heijden AA, Beulens JW, de Keyser CE, Zaharenko L, Rotroff DM, Out M, Jablonski KA, Chen L, Javorský M, Židzik J, Levin AM, Williams LK, Dujic T, Semiz S, Kubo M, Chien HC, Maeda S, Witte JS, Wu L, Tkác I, Kooy A, van Schaik RHN, Stehouwer CDA, Logie L. Variation in the glucose transporter gene SLC2A2 is associated with glycemic response to metformin. Nat Genet. 2016 09; 48(9):1055-1059.
    View on PubMed
  20. Yee SW, Momozawa Y, Kamatani Y, Tyndale RF, Weinshilboum RM, Ratain MJ, Giacomini KM, Kubo M. Genomewide Association Studies in Pharmacogenomics: Meeting Report of the NIH Pharmacogenomics Research Network-RIKEN (PGRN-RIKEN) Collaboration. Clin Pharmacol Ther. 2016 Nov; 100(5):423-426.
    View on PubMed

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