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Pico Pharmaceuticals Inc. is developing powerful therapeutics to treat
cancer and infectious diseases with novel methods of inhibitor design
called transition state inhibitors, or TSIs. Pico Pharmaceuticals’ products
are orally available, druggable small molecule compounds which utilize
Transition State Quantum Chemistry.

Compounds in Pico Pharmaceuticals’ cancer and anti-infective programs
have demonstrated unprecedented binding affinity and specificity for their
targets in preclinical studies. Pico Pharmaceuticals’ TSIs:
I Access medically validated but previously intractable drug targets
I Achieve picomolar or greater binding affinity
I Maintain ultimate enzyme-target binding
I Function through natural cellular mechanisms
I Are orally available

These features may yield compounds with multiple therapeutic advantages
including minimal off-target interactions and low predicted toxicity,
conforming to the clinical dictum of “first, do no harm.”

Applying TSQC for Development of Therapeutic Compounds

Pico Pharmaceuticals is able to capture a blueprint of an enzyme in a
dynamic moment of transition and, using this model, can create inhibitors
specific to the enzymes’transition state conformation — a new method to
selectively access and bind to previously intractable targets.

                                                  Initial blueprint
                                                  Captures enzyme’s transition
                                                  state energetic information
                                                  Bond energy model
                                                  Created using calculated values
                                                  Molecular structure
                                                  Enables synthesis of a transition
                                                  state inhibitor drug compound
                                                                                                              MANAGEMENT TEAM AND
PICO PHARMACEUTICALS TRANSITION                                                                               BOARD OF DIRECTORS
                                                                                                              Tim Boyd, JD, MBT
                                                                                                              President and Chief Executive Officer
                                          Transition State   Transition State
                                             Mapping       Inhibitor Synthesis    Pre-IND       IND/Phase 1   Bert Liang, MD, MBA
  PC8608 − Lung                                                                                     *         Doug Wilson, MB, ChB, PhD
                                                                                                    *         Director
  PC8608 − Prostate

  PC8608 − Head & neck                                                                              *
  PC8608 − Colon Cancer                                                                             *         SCIENTIFIC ADVISORY BOARD
 Lead indication
                                                                                                              Vern Schramm, PhD
Anti-infectives                                                                                               Albert Einstein College of Medicine
  PC0208 – Hospital acquired infections
                                                                                                              Chandan Guha, MD, PhD
  PC4708 – Implantable devices                                                                                Albert Einstein College of Medicine

             Current                      Projected YE09                    Lead cancer indication YE09       John Kozarich, PhD
                                                                                                              ACTIVX Pharmaceuticals
*Lead indication to be chosen for IND in 2009
                                                                                                              Ashley Dunn, PhD
                                                                                                              AR Dunn & Associates
Lead compound poised for clinical stage trials
Pico Pharmaceuticals is developing PC8608, a novel once-a-day
transition state inhibitor, to treat multiple cancer types. PC8608 targets
MTAP, an enzyme critical for cancer cell proliferation, and is also
believed to have an epigenetic mechanism that exploits the genomic
instability of cancer cells. PC8608 has shown significant anti-tumor
activity in human cancer models of prostate, lung, colon, cervical and
head and neck cancers. Pico Pharmaceuticals plans to complete
IND-enabling studies in 2009.

Two compounds for multiple hospital acquired infections
Pico Pharmaceuticals is developing PC0208 and PC4708, novel
transition state inhibitors to suppress pathogenic traits in microbial
infections. The lead compounds in this program, PC0208 and PC4708
target MTAN, a key enzyme in the bacterial quorum sensing pathway,
to create a feedback signal and disrupt bacterial aggregation, preventing
infection. An important feature of this mechanism is that it is expected
to be slow to induce antibiotic resistance in pathogens such as Vibrio                                        Corporate Headquarters
cholera, Staphylococcus aureus, Streptococcus pneumaniae, Neisseria                                           Suite 206
meningitidis and Escherichia coli therefore providing long use profiles.                                      4510 Executive Drive
Pico Pharmaceuticals plans to conclude pre-IND studies and nominate                                           San Diego, CA 92121 USA
a lead compound in the anti-infectives program by the end of 2009.
                                                                                                              phone: +1 858 866 9319
                                                                                                              fax: +1 858 408 2652

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