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. Hall C, Wolfe H, Wells A, Chien HC, Colas C, Schlessinger A, Giacomini KM, Thomas AA. l-Type amino acid transporter 1 activity of 1,2,3-triazolyl analogs of l-histidine and l-tryptophan. Bioorg Med Chem Lett. 2019 Jun 20.
    View on PubMed
  2. Cheung KWK, van Groen BD, Spaans E, van Borselen MD, de Bruijn ACJM, Simons-Oosterhuis Y, Tibboel D, Samsom JN, Verdijk RM, Smeets B, Zhang L, Huang SM, Giacomini KM, de Wildt SN. A Comprehensive Analysis of Ontogeny of Renal Drug Transporters: mRNA Analyses, Quantitative Proteomics, and Localization. Clin Pharmacol Ther. 2019 May 25.
    View on PubMed
  3. Yee SW, Giacomini MM, Shen H, Humphreys WG, Horng H, Brian W, Lai Y, Kroetz DL, Giacomini KM. Organic Anion Transporter Polypeptide 1B1 Polymorphism Modulates the Extent of Drug-Drug Interaction and Associated Biomarker Levels in Healthy Volunteers. Clin Transl Sci. 2019 Apr 13.
    View on PubMed
  4. Enogieru OJ, Ung PMU, Yee SW, Schlessinger A, Giacomini KM. Functional and structural analysis of rare SLC2A2 variants associated with Fanconi-Bickel syndrome and metabolic traits. Hum Mutat. 2019 Apr 05.
    View on PubMed
  5. Brackman DJ, Yee SW, Enogieru OJ, Shaffer C, Ranatunga D, Denny JC, Wei WQ, Kamatani Y, Kubo M, Roden DM, Jorgenson E, Giacomini KM. Genome-Wide Association and Functional Studies Reveal Novel Pharmacological Mechanisms for Allopurinol. Clin Pharmacol Ther. 2019 Mar 28.
    View on PubMed
  6. Giacomini KM, Lin L, Altman RB. Research Projects Supported by the University of California, San Francisco-Stanford Center of Excellence in Regulatory Science and Innovation. Clin Pharmacol Ther. 2019 Apr; 105(4):815-818.
    View on PubMed
  7. Zou L, Ni Z, Tsakalozou E, Giacomini KM. Impact of Pharmaceutical Excipients on Oral Drug Absorption: A Focus on Intestinal Drug Transporters. Clin Pharmacol Ther. 2019 Feb; 105(2):323-325.
    View on PubMed
  8. 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. Organic cation transporter 3 (Oct3) is a distinct catecholamines clearance route in adipocytes mediating the beiging of white adipose tissue. PLoS Biol. 2019 Jan; 17(1):e2006571.
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  9. 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. Clinical Probes and Endogenous Biomarkers as Substrates for Transporter Drug-Drug Interaction Evaluation: Perspectives From the International Transporter Consortium. Clin Pharmacol Ther. 2018 Nov; 104(5):836-864.
    View on PubMed
  10. Giacomini KM, Galetin A, Huang SM. The International Transporter Consortium: Summarizing Advances in the Role of Transporters in Drug Development. Clin Pharmacol Ther. 2018 Nov; 104(5):766-771.
    View on PubMed
  11. Chien HC, Colas C, Finke K, Springer S, Stoner L, Zur AA, Venteicher B, Campbell J, Hall C, Flint A, Augustyn E, Hernandez C, Heeren N, Hansen L, Anthony A, Bauer J, Fotiadis D, Schlessinger A, Giacomini KM, Thomas AA. Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1). J Med Chem. 2018 Aug 23; 61(16):7358-7373.
    View on PubMed
  12. 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. Transporters in Drug Development: 2018 ITC Recommendations for Transporters of Emerging Clinical Importance. Clin Pharmacol Ther. 2018 Nov; 104(5):890-899.
    View on PubMed
  13. Yee SW, Brackman DJ, Ennis EA, Sugiyama Y, Kamdem LK, Blanchard R, Galetin A, Zhang L, Giacomini KM. Influence of Transporter Polymorphisms on Drug Disposition and Response: A Perspective From the International Transporter Consortium. Clin Pharmacol Ther. 2018 Nov; 104(5):803-817.
    View on PubMed
  14. 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. ITC Commentary on Metformin Clinical Drug-Drug Interaction Study Design That Enables an Efficacy- and Safety-Based Dose Adjustment Decision. Clin Pharmacol Ther. 2018 Nov; 104(5):781-784.
    View on PubMed
  15. Srinivasan S, Yee SW, Giacomini KM. Pharmacogenetics of Antidiabetic Drugs. Adv Pharmacol. 2018; 83:361-389.
    View on PubMed
  16. Zou L, Stecula A, Gupta A, Prasad B, Chien HC, Yee SW, Wang L, Unadkat JD, Stahl SH, Fenner KS, Giacomini KM. Molecular Mechanisms for Species Differences in Organic Anion Transporter 1, OAT1: Implications for Renal Drug Toxicity. Mol Pharmacol. 2018 07; 94(1):689-699.
    View on PubMed
  17. Liang X, Yee SW, Chien HC, Chen EC, Luo Q, Zou L, Piao M, Mifune A, Chen L, Calvert ME, King S, Norheim F, Abad J, Krauss RM, Giacomini KM. Organic cation transporter 1 (OCT1) modulates multiple cardiometabolic traits through effects on hepatic thiamine content. PLoS Biol. 2018 04; 16(4):e2002907.
    View on PubMed
  18. Rotroff DM, Yee SW, Zhou K, Marvel SW, Shah HS, Jack JR, Havener TM, Hedderson MM, Kubo M, Herman MA, Gao H, Mychaleckyi JC, McLeod HL, Doria A, Giacomini KM, Pearson ER, Wagner MJ, Buse JB, Motsinger-Reif AA. Genetic Variants in CPA6 and PRPF31 Are Associated With Variation in Response to Metformin in Individuals With Type 2 Diabetes. Diabetes. 2018 07; 67(7):1428-1440.
    View on PubMed
  19. Zamek-Gliszczynski MJ, Giacomini KM, Zhang L. Emerging Clinical Importance of Hepatic Organic Cation Transporter 1 (OCT1) in Drug Pharmacokinetics, Dynamics, Pharmacogenetic Variability, and Drug Interactions. Clin Pharmacol Ther. 2018 May; 103(5):758-760.
    View on PubMed
  20. Brackman DJ, Giacomini KM. Reverse Translational Research of ABCG2 (BCRP) in Human Disease and Drug Response. Clin Pharmacol Ther. 2018 02; 103(2):233-242.
    View on PubMed

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