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Scientist Profile

Cyrus Khojasteh

Senior Scientist
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"My ability to contribute to the discovery of safe and efficacious drugs to treat important unmet medical conditions is what keeps me inspired."

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.

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My Focus

I have worked on a number of projects in oncology and more recently in immunology. I was the Pharmacology Sub-team Leader for GDC-0449, a small molecule hedgehog pathway inhibitor, which is in phase 2/3.

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.

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Publications & Recognition
  • 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 Metab Dispos 2010 Apr 20
  • Wong H, Theil FP, Cui Y, Marsters JC, Khojasteh SC, Vernillet L, La H, Song X, Wang H, Morinello E, Deng Y, Hop CE
  • View Abstract on PubMed
  • Formation of a Quinoneimine Intermediate of 4-Fluoro-N-methylaniline by FMO1: Carbon Oxidation Plus Defluorination
  • Chem Res Toxicol 2010 Apr 6
  • Driscoll JP, Aliagas I, Harris JJ, Halladay JS, Khatib-Shahidi S, Deese A, Segraves N, Khojasteh-Bakht SC
  • View Abstract on PubMed
  • Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor
  • Xenobiotica 2009 Sep 2
  • Wong H, Chen JZ, Chou B, Halladay JS, Kenny JR, La H, Marsters JC, Plise E, Rudewicz PJ, Robarge K, Shin Y, Wong S, Zhang C, Khojasteh SC
  • View Abstract on PubMed
 
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  • University of Washington, Medicinal Chemistry
  • Ph.D
  • 1993-1998
  • California State University, Sacramento, Organic Chemistry
  • M.S
  • 1989-1991
  • University of California, Berkeley, Chemistry and Chemical Engineering
  • B.S
  • 1984-1988
Publications & Recognition
  • 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 Metab Dispos 2010 Apr 20
  • Wong H, Theil FP, Cui Y, Marsters JC, Khojasteh SC, Vernillet L, La H, Song X, Wang H, Morinello E, Deng Y, Hop CE
  • View Abstract on PubMed
  • Formation of a Quinoneimine Intermediate of 4-Fluoro-N-methylaniline by FMO1: Carbon Oxidation Plus Defluorination
  • Chem Res Toxicol 2010 Apr 6
  • Driscoll JP, Aliagas I, Harris JJ, Halladay JS, Khatib-Shahidi S, Deese A, Segraves N, Khojasteh-Bakht SC
  • View Abstract on PubMed
  • Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor
  • Xenobiotica 2009 Sep 2
  • Wong H, Chen JZ, Chou B, Halladay JS, Kenny JR, La H, Marsters JC, Plise E, Rudewicz PJ, Robarge K, Shin Y, Wong S, Zhang C, Khojasteh SC
  • View Abstract on PubMed
  • GDC-0449-a potent inhibitor of the hedgehog pathway
  • Bioorg Med Chem Lett 2009 Oct 1; 19(19): 5576-81
  • Robarge KD, Brunton SA, Castanedo GM, Cui Y, Dina MS, Goldsmith R, Gould SE, Guichert O, Gunzner JL, Halladay J, Jia W, Khojasteh C, Koehler MF, Kotkow K, La H, Lalonde RL, Lau K, Lee L, Marshall D, Marsters JC Jr, Murray LJ, Qian C, Rubin LL, Salphati L, Stanley MS, Stibbard JH, Sutherlin DP, Ubhayaker S, Wang S, Wong S, Xie M
  • View Abstract on PubMed
  • Inhibitory properties of trapping agents: glutathione, potassium cyanide, and methoxylamine, against major human cytochrome p450 isoforms
  • Drug Metab Lett 2009 Apr; 3(2): 125-9
  • Zhang C, Wong S, Delarosa EM, Kenny JR, Halladay JS, Hop CE, Khojasteh-Bakht SC
  • View Abstract on PubMed
  • On the prediction of hepatic clearance using the diluted plasma in metabolic stability assay
  • J Pharm Sci 2009 Jun; 98(6): 1922-7
  • Berezhkovskiy LM, Khojasteh SC, Halladay JS, Hop CE
  • View Abstract on PubMed
  • Preclinical absorption, distribution, metabolism and excretion (ADME) characterization of ICAM1988, an LFA-1/ICAM antagonist, and its prodrug
  • Xenobiotica 2008 Mar; 38(3): 340-52
  • Khojasteh SC, Leipold DD, Lai F, La H, Baumgardner MJ, Desino KE, Gudmundsson OS, Bloedow DC, Bodary SC, Reynolds ME, Gadek TR, Kenkare-Mitra S
  • View Abstract on PubMed
  • Metabolism, pharmacokinetics, and excretion of a nonpeptidic substance P receptor antagonist, ezlopitant, in normal healthy male volunteers: characterization of polar metabolites by chemical derivatization with dansyl chloride
  • Drug Metab Dispos 2007 Jul; 35(7): 1071-80.
  • Prakash C, O'Donnell J, Khojasteh-Bakht SC
  • View Abstract on PubMed
  • Metabolic stability screen for drug discovery using cassette analysis and column switching
  • Drug Metab Lett 2007 Jan; 1(1): 67-72
  • Halladay JS, Wong S, Jaffer SM, Sinhababu AK, Khojasteh-Bakht SC
  • View Abstract on PubMed
  • Automated online liquid chromatographic/mass spectrometric metabolic study for prodrug stability
  • J Chromatogr B Analyt Technol Biomed Life Sci 2005 Jan 25; 814(2): 225-32
  • Lai F, Khojasteh-Bakht SC
  • View Abstract on PubMed
  • Metabolism, pharmacokinetics, tissue distribution, and excretion of [14C]CP-424391 in rats
  • Drug Metab Dispos 2005 Jan; 33(1): 190-9
  • Khojasteh-Bakht SC, O'donnell JP, Fouda HG, Potchoiba MJ
  • View Abstract on PubMed
  • Identification of the human cytochrome P450s responsible for the in vitro metabolism of a leukotriene B4 receptor antagonist, CP-195,543
  • Xenobiotica 2003 Dec; 33(12): 1201-10
  • Khojasteh-Bakht SC, Rossulek MI, Fouda HG, Prakash C
  • View Abstract on PubMed
  • Biotransformation reactions of five-membered aromatic heterocyclic rings
  • Chem Res Toxicol 2002 Mar; 15(3): 269-99
  • Dalvie DK, Kalgutkar AS, Khojasteh-Bakht SC, Obach RS, O'Donnell JP
  • View Abstract on PubMed
  • Glutathione S-transferase catalyzes the isomerization of (R)-2-hydroxymenthofuran to mintlactones
  • Arch Biochem Biophys 1999 Oct 1; 370(1): 59-65
  • Khojasteh-Bakht SC, Nelson SD, Atkins WM
  • View Abstract on PubMed
  • Metabolism of (R)-(+)-pulegone and (R)-(+)-menthofuran by human liver cytochrome P-450s: evidence for formation of a furan epoxide
  • Drug Metab Dispos 1999 May; 27(5): 574-80
  • Khojasteh-Bakht SC, Chen W, Koenigs LL, Peter RM, Nelson SD
  • View Abstract on PubMed
  • (R)-(+)-Menthofuran is a potent, mechanism-based inactivator of human liver cytochrome P450 2A6
  • Drug Metab Dispos 1998 Jul; 26(7): 701-4
  • Khojasteh-Bakht SC, Koenigs LL, Peter RM, Trager WF, Nelson SD
  • View Abstract on PubMed
  • Pennyroyal toxicity: measurement of toxic metabolite levels in two cases and review of the literature
  • Ann Intern Med 1996 Apr 15; 124(8): 726-34
  • Anderson IB, Mullen WH, Meeker JE, Khojasteh-BakhtSC, Oishi S, Nelson SD, Blanc PD
  • View Abstract on PubMed
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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
  • Travel Award from American Society for Pharmacology and Experimental Therapeutics - 1998
  • Predoctoral National Institutes of Health Grant Awardee, University of Washington - 1995-1998

Ellen Filvaroff, Senior Scientist and Alex Avardo, Receipent of Free Medicine From the Genentech® Access to Care Foundation, on the cover of Genentech's 2006 Annual Report.