After a couple of years in the Biotransformation Group at Pfizer, I joined Genentech as a Scientist in 2000. At the time, Genentech was known for its large molecule therapeutics and not the small molecule projects. I understood that Genentech is a place where one can do good science and the scientists are empowered to make a difference, which leads to a 'can-do' attitude. In the past 10 years, this has translated in a state-of-the-art small molecule organization with a strong pipeline.

People ask me if this attitude has changed since we are now a much larger organization. I maintain that the spirit and the culture of Genentech has not changed. The passion to work hard to discover new therapeutic agents is still very strong.

• My Focus

  I have worked on a number of projects in oncology and immunology. I was the Pharmacology Sub-team Leader for Vismodegib (trade name Erivedge), a small molecule hedgehog pathway inhibitor, which is got FDA approval January 30, 2012.

  Scientists from my field, Drug Metabolism and Pharmacokinetics, interface with a large number of disciplines from discovery to development: Medicinal Chemistry, Pharmacology, Toxicology, Clinical Pharmacology, Pharmaceutical Sciences, etc. There are many opportunities to work together to solve very complicated problems.

• Publications

  • An 'all-inclusive' 96-well cytochrome P450 induction method: Measuring enzyme: Activity, mrna levels, protein levels, and cytotoxicity from one well using: Cryopreserved human hepatocytes

    Journal of Pharmacological and Toxicological Methods, 2012, ISSN: 1056-8719

    Halladay, Jason S.; Wong, Susan; Cyrus Khojasteh, S.; Grepper, Susan

     View on PubMed

  • Evaluation of time-dependent cytochrome P450 inhibition in a high-throughput, automated assay: Introducing a novel area under the curve shift approach

    Drug Metabolism Letters, 2012, ISSN: 1872-3128

    Mukadam, Sophie; Tay, Suzanne; Tran, Daniel; Wang, Leslie; Delarosa, Erlie M.; Khojasteh, S. Cyrus; Halladay, Jason S.; Kenny, Jane R.

  • Evaluation of Metabolism and Disposition of GDC-0152 in Rats Using 14C Labeling Strategy at Two Different Positions: A Novel Formation of Hippuric Acid from 4-Phenyl-5-amino-1,2,3-thiadiazole

    Drug Metabolism and Disposition, 2012, ISSN: 0090-9556

    Yue, Qin; Mulder, Teresa; Rudewicz, Patrick J; Solon, Eric; Budha, Nageshwar; Ware, Joseph A; Lyssikatos, Joseph; Hop, Cornelis E C A; Wong, Harvey; Khojasteh, S Cyrus

     View on PubMed

  • Characterization of rat liver proteins adducted by reactive metabolites of menthofuran

    Chemical Research in Toxicology, 2012, ISSN: 0893-228X

    Khojasteh, S. Cyrus; Hartley, Dylan P.; Ford, Kevin A.; Uppal, Hirdesh; Oishi, Shimako; Nelson, Sidney D.

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  • Drug-Drug Interaction Potential of Marketed Oncology Drugs: In Vitro Assessment of Time-Dependent Cytochrome P450 Inhibition, Reactive Metabolite Formation and Drug-Drug Interaction Prediction

    Pharmaceutical Research, 2012, ISSN: 0724-8741

    Kenny, Jane R; Mukadam, Sophie; Zhang, Chenghong; Tay, Suzanne; Collins, Carol; Galetin, Aleksandra; Khojasteh, S. Cyrus;

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  • Novel Mechanism for Dehalogenation and Glutathione Conjugation of Dihalogenated Anilines in Human Liver Microsomes: Evidence for ipso Glutathione Addition.

    Chemical Research in Toxicology, 9 Sep 2011, ISSN: 1520-5010.

    Zhang, Chenghong; Kenny, Jane R; Le, Hoa; Deese, Alan; Ford, Kevin A; Lightning, Luke K; Fan, Peter W; Driscoll, James P; Halladay, Jason S; Hop, Cornelis E C A; Khojasteh, S Cyrus

     View on PubMed

  • High-Throughput, 384-Well, LC-MS/MS CYP Inhibition Assay Using Automation, Cassette-Analysis Technique, and Streamlined Data Analysi

    Drug Metabolism Letters, 9 Aug 2011, ISSN: 1872-3128.

    Halladay, Jason S; Delarosa, Erlie Marie; Tran, Daniel; Wang, Leslie; Wong, Susan; Khojasteh, S Cyrus

     View on PubMed

  • Significant Species Difference in Amide Hydrolysis of GDC-0834, a Novel Potent and Selective Bruton's Tyrosine Kinase (BTK) Inhibitor.

    Drug metabolism and disposition: the biological fate of chemicals, {Drug-Metab-Dispos}, 8 Jul 2011 (epub: 8 7 2011), ISSN: 1521-009X.

    Liu, Lichuan; Halladay, Jason; Shin, Young; Wong, Susan; Coraggio, Melis; La, Hank; Baumgardner, Matthew; Le, Hoa; Gopaul, Sashi; Boggs, Jason; Kuebler, Peter; Davis, John; Liao, Charlene; Lubach, Joseph; Deese, Alan; Sowell, Gregory; Currie, Kevin; Young, Wendy; Khojasteh, Cyrus; Hop, Cornelis; Wong, Harvey

     View on PubMed

  • Absorption, Distribution, Metabolism, and Excretion of [¹⁴C]GDC-0449 (Vismodegib), an Orally Active Hedgehog Pathway Inhibitor, in Rats and Dogs: A Unique Metabolic Pathway via Pyridine Ring Opening.

    Drug Metabolism and Disposition, {Drug-Metab-Dispos}, June 2011, vol. 39, no. 6, p. 952-965, 22 refs, CODEN: DMDSA, eISSN: 1521-009X, ISSN: 0090-9556. Publisher: American Society for Pharmacology and Experimental Therapy, 9650 Rockville Pike, Bethesda, MD 20814, USA.

    Yue, Qin; Chen, Yung Hsiang; Mulder, Teresa; Deese, Alan; Takahashi, Ryan; Rudewicz, Patrick J; Reynolds, Mark; Solon, Eric; Hop, Cornelis ECA; Wong, Harvey; Khojasteh, S Cyrus

     View on PubMed

  • Influence of Fluorine Substitution at the C-3 Position on Oxidative Metabolism of N-Ethylpiperidine Analogs.

    Drug Metabolism Reviews, 2010, ISSN: 0360-2532

    Liederer, B.M.; Dinkel, V.; Gaudino, J.; Gopaul, S.; Le, H.; Liu, X.; Sutherlin, D.; Wong, S.; Khojasteh, C.

  • Investigation of Metabolism in Mice, Rats, Monkeys, Dogs and Humans of a Novel Met Kinase Inhibitor for Species Selection for Preclinical Toxicology Studies.

    Drug Metabolism Reviews, 2010, ISSN: 0360-2532

    Liederer, B.M.; Baumgardner, M.; Dean, B.; Dinkel, V.; Gaudino, J.; Gopaul, S.; Le, H.; Liu, X.; Sutherlin, D.; Khojasteh, C.

  • Mechanism Studies for Determining the Loss of Nitrile Moiety and Formation of Primary Alcohol by CYP.

    Drug Metabolism Reviews, 2010, ISSN: 0360-2532

    Le, H.; Wong, S.; Driscoll, J.; Hop, C.; Khojasteh, C.

  • Significant Species Difference of Amide Hydrolysis of GDC-0834, a Novel Potent and Selective Bruton's Tyrosine Kinase Inhibitor.

    Drug Metabolism Reviews, 2010, ISSN: 0360-2532

    Liu, L.; Halladay, J.; Shin, Y.; Wong, S.; Coraggio, M.; La, H.; Baumgardner, M.; Le, H.; Kuebler, P.; Davis, J.C.; Liao, X.C.; Lubach, J.; Deese, A.; Sowell, C.G.; Currie, K.S.; Young, W.B.; Khojasteh, C.; Hop, C.; Wong, H.

  • Metabolism and Toxicity of Menthofuran in Rat Liver Slices and in Rats.

    Chemical Research in Toxicology, 2010, ISSN: 1520-5010

    Khojasteh, S.C.; Oishi, S.; Nelson, S.

  • Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway.

    Bioorganic & Medicinal Chemistry Letters, 2010, ISSN: 1464-3405

    Castanedo, G.; Wang, S.; Robarge, K.; Blackwood, E.; Burdick, D.; Chang, C.; Dijkgraaf, G.; Gould, S.; Gunzner, J.; Guichert, O.; Halladay, J.; Khojasteh, C.; Lee, L.; Marsters, J.; Murray, L.; Peterson, D.; Plise, E.; Salphati, L.; de Sauvage, F.; Wong, S.; Sutherlin, D.

  • Interplay of Dissolution, Solubility and Non-Sink Permeation Determines the Oral Absorption of the Hedgehog Pathway Inhibitor, GDC-0449, in Dogs: An Investigation using Preclinical Studies and Physiologically- Based Pharmacokinetic Modeling.

    Drug Metabolism and Disposition, 2010, ISSN: 0090-9556

    Wong, H.; Theil, F.-P; Cui, Y; Marsters, J.; Khojasteh S.C.; Vernillet, L.; La, H.; Song, X.; Wang, H.; Morinello, E.; Deng, Y.; Hop, C.

  • Formation of a Quinoneimine Intermediate of 4-Fluoro-N-methylaniline by FMO1: Carbon Oxidation Plus Defluroination.

    Chemical Research in Toxicology, 2010, ISSN: 1520-5010

    Driscoll, J.P.; Aliagas, I.; Harris, J.J.; Halladay, J.S.; Khatib-Shahidi, S.; Deese, A.; Segraves, N.; Khojasteh-Bakht, S.C.

  • Corrigendum to "GDC-0449-A potent inhibitor of the hedgehog pathway" [Bioorg. Med. Chem. Lett. 19 (2009) 5576]

    Bioorganic and Medicinal Chemistry Letters, 2010, ISSN: 0960-894X

    Robarge, K.; Brunton, S.; Castanedo, G.; Cui, Y.; Dina, M.; Goldsmith, R.; Gould, S.; Guichert, O.; Gunzner, J.; Halladay, J.; Jia, W.; Khojasteh, C.; Koehler, M.; Kotkow, K.; La, H.; LaLonde, R.; Lau, K.; Lee, L.; Marshall, D.; Marsters, Jr., J.; Murray, L.; Qian, C.; Rubin, L.; Salphati, L.; Stanley, M.S.; Stibbard, J.; Sutherlin, D.; Ubhayaker, S.; Wang, S.; Wong, S.; Xie M.

  • Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl) -4-(methylsulfonyl)benz amide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor.

    Xenobiotica, 2009, ISSN: 1366-5928

    Wong, H.; Chen, J.Z.; Chou, B.; Halladay, J.S.; Kenny, J.R.; La, H.; Marsters, J.C.; Plise, E.; Rudewicz, P.J.; Robarge, K.; Shin, Y.; Wong S.; Zhang, C.; Khojasteh, S.C.

  • GDC-0449-a potent inhibitor of the hedgehog pathway.

    Bioorganic & Medicinal Chemistry Letters, 2009, ISSN: 1464-3405

    Robarge, K.D.; Brunton, S.A.; Castanedo, G.M.; Cui, Y.; Dina, M.S.; Goldsmith, R.; Gould, S.E.; Guichert, O.; Gunzner, J.L.; Halladay, J.; Jia, W.; Khojasteh, C.; Koehler, M.F.; Kotkow, K.; La, H.; Lalonde, R.L.; Lau, K.; Lee, L.; Marshall, D.; Marsters, J.C. Jr.; Murray, L.J.; Qian, C.; Rubin, L.L.; Salphati, L.; Stanley, M.S.; Stibbard, J.H.; Sutherlin, D.P.; Ubhayaker, S.; Wang, S.; Wong, S.; X

  • Inhibitory properties of trapping agents: glutathione, potassium cyanide, and methoxylamine, against major human cytochrome p450 isoforms.

    Drug Metabolism Letters, 2009, ISSN: 1872-3128

    Zhang, C.; Wong, S.; Delarosa, E.M.; Kenny, J.R.; Halladay, J.S.; Hop, C.E.; Khojasteh-Bakht, S.C.

  • On the prediction of hepatic clearance using the diluted plasma in metabolic stability assay.

    Journal of Pharmaceutical Sciences, 2009, ISSN: 1520-6017

    Berezhkovskiy, L.M.; Khojasteh, S.C.; Halladay, J.S.; Hop, C.E.

• Education
  • University of Washington, Medicinal Chemistry, Ph.D. – 1998
  • California State University, Sacramento, Organic Chemistry, M.S. – 1991
  • University of California, Berkeley, Chemistry, B.A. – 1988
• Awards & Honors
  • Member of the International Society for Studying Xenobiotics Abstract Review Committee – 2009
  • Member of the International Society for Studying Xenobiotics Exhibitors Committee – 2008-2011
  • Predoctoral National Institutes of Health Grant Awardee, University of Washington – 1998
  • Travel Award from American Society for Pharmacology and Experimental Therapeutics – 1998