San Francisco
December 7, 2012
Destination Europe
POLAND
Chemistry and Biology of Cancer
----------Drug Discovery in Academia
Waldemar Priebe, Ph.D.
Professor of Chemistry and
Professor of Medicinal Chemistry
Importance of Entrepreneurial Scientists to
the Future of the EU and American Economy
Waldemar Priebe
• Professor, Medicinal Chemistry, UT MD Anderson Cancer
Center
• Over 25 years research experience in drug discovery and
development
• Founder or Founding Scientist of 5 Biotech Co.
• Aronex Pharmaceuticals
• Houston Pharmaceuticals
• Reata Pharmaceuticals
• Moleculin, LLC
• IntertechBio
• Licensed 7 compounds to industry with 4 drugs in clinical
studies in humans
2
• Over 180 research papers and 50 patents
TEXAS:
an overview
Population: 23 mln
Labor Force: 11 mln
Unemployment Rate: 4.2 %
2nd Most Populous State
261,797 square miles of land (twice as Germany)
History of The University of Texas
MD Anderson Cancer Center
Monroe Dunaway Anderson
created a charitable
foundation in 1936.
After his death, the
MD Anderson Foundation
provided funding and land
to build a cancer hospital to
serve the citizens of Texas.
LeMaistre Clinic Building
opened in 1996 -- 15,756 sq. m.
Alkek Hospital Building
opened in 1998 -- 70,212 sq. m.
Mays Clinical Building
opened in 2004 --113,112 sq. m.
Texas Medical Center
UT MD Andersons Sister Institution Network
MDACC
Sister Institutions
Breast Awareness and
Research Partnerships
Co-Branded Institutions
Sister Institutions
France
Institut Gustave Roussy, Villejuif
Germany
German Cancer Research Center, Heidelberg
Norway
The Norwegian Cancer Consortium
Poland
The Polish Cancer Consortium
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Structure of the WP631–AC/GTAC/GT Complex
1
WP631 inhibits (at 60 nM) Sp1-activated transcription initiation in vitro
J. Med. Chem., 40: 261-266, 1997
Biochem. Pharmacol. 63, 1251-1258, 2002
Biochemistry, 36: 5940-5946, 1997
Eur. J. Biochem., 270: 764-770, 2003
Biochemistry, 36: 8663-8670, 1997
Biochemistry. 43(23):7584-7592, 2004
Biochemistry, 37: 1743-1753, 1998
Eur. J. Biochem., 271, 3556–3566, 2004
Nucleic Acid Res., 27: 3402-3409, 1999
J. Med. Chem., 48, 8209-8219, 2005
Curr. Med Chem. 8: 1-8, 2001
J. Biol. Chem., 276: 34486, 2001
Methods in Enzymology, Vol. 340, 529-555, 2001
WP631
Kobs = 3 x 1011 M-1
Waldemar Priebe
Patient Examples in Phase I Trial of
WP744 (RTA744, Berubicin)
Patient 119 Achieves Partial Response After 2 Cycles of RTA 744 at a
Dose of 7.5 mg/m2/day x 3
Before RTA 744
Oct 20, 2006
After 2 Cycles
52 Year-old female
Diagnosed with AO December 2000
Previous treatments include resection, RT, resection, Tmz, resection
81% reduction in lesion
Evidence of Clinical Activity of Berubicin
(RTA744/WP744) in Phase I
Patient 104 Achieves Complete Response After 7 Cycles
of RTA 744 at a Dose 2.4 mg/m2/day x 3
Before RTA 744
Jan 20
After 2 Cycles
Mar 7
After 6 Cycles
July 11
52 year-old male
Recurrent GBM progressed from AA
Previous treatments include resection, RT + Tmz,
Tmz + Thalidomide + Accutane + Celebrex (8 cycles)
Complete Response ongoing 3 years later
After 7 Cycles
Aug 1
F18-FDG PET Scan of “Hot” Tumor Treated with 2-DG
F18-FDG PET Baseline Study
24 Hours Repeat F18-FDG PET
Post Treatment with 2-DG