Paloma Pharmaceuticals Update on Ocular Clinical and Oncology Programs

By Paloma Pharmaceuticals Inc., PRNE
Monday, February 28, 2011

Through first three cohorts of intravitreal macular degeneration Phase I trial, start of National Eye Institute subconjunctival macular degeneration Phase I trial, publication/submission of cancer studies, presentation at AACR 'Targeting PI3K/mTOR Signaling in Cancer' -

JAMAICA PLAIN, Massachusetts, March 1, 2011 - Paloma Pharmaceuticals, Inc. announced today updates on its age-related
macular degeneration Phase I trials and oncology program. Palomid 529 (P529),
Paloma Pharmaceuticals first-in-class allosteric dual TORC1/TORC2
dissociative inhibitor targeting the PI3K/Akt/mTOR pathway, has successfully
completed the Company's first three cohorts of its Phase I intravitreal
administration trial in patients with age-related macular degeneration (AMD).
In addition, the National Eye Institute has treated its first patient in the
Institute's own Phase I AMD trial administering P529 subconjunctival, "A
Phase I Unmasked Study to Investigate the Safety and Tolerability of
Subconjunctival Injections of Palomid 529 in Patients With Neovascular
Age-Related Macular Degeneration".

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"Relative to our oncology program, we have now completed oral formulation
work to ultimately deliver P529 as a tablet. This final step puts us close to
submitting our oncology IND package to the FDA. Furthermore, we have now
shown activity of P529 in difficult to treat tumors with Brca-1 and PTEN
mutations with a newly published manuscript and the submission of a second
manuscript," said Dr. Sherris.

"Targeting the Akt/mTOR pathway in Brca1-deficient cancers" was published
in the Nature journal Oncogene from the laboratory of Qin Yang, M.D., Ph.D.
of the Department of Radiation Oncology, Washington University School of
Medicine, St. Louis, MO. "Palomid 529 significantly suppressed
Brca1-deficient tumor growth in mice through inhibition of both Akt and mTOR
signaling. Our results indicate that activation of Akt is involved in Brca1-
deficiency mediated tumorigenesis and that the mTOR pathway can be used as a
novel target for treatment of Brca1-deficient cancers," said Dr. Yang.

"The TORC1/TORC2 inhibitor, Palomid 529, reduces tumor growth and
sensitizes to docetaxel and cisplatin in aggressive and hormone refractory
prostate cancer cells" was submitted to the journal Endocrine-related Cancer
from the laboratory of Claudio Festuccia, Ph.D. of the Department of
Experimental Medicine, University of L'aquila, Italy. "The activation of
PI3K/Akt/mTOR pathways is often observed during prostate cancer progression.
Our studies provide preclinical evidence that the inhibition of this pathway
is a very effective approach to treat hormone refractive prostate cancer.
Here, the PI3K/Akt/mTOR pathway was targeted by using P529, an orally
available TORC1/TORC2 inhibitor and showed that this agent results in
synergistic effects with docetaxel and cisplatin in PTEN positive or negative
prostate cancer models. These results provide a rationale for clinical
development with conventional chemotherapy and inhibitors of the
PI3K/Akt/mTOR pathway," said Dr. Festuccia.

Additionally, Paloma Pharmaceuticals presented at the American
Association for Cancer Research (AACR) Special Conference "Targeting
PI3K/mTOR Signaling in Cancer" in San Francisco, CA entitled, "Palomid 529,
an allosteric TORC1/TORC2 inhibitor of the PI3K/Akt/mTOR pathway, shows
differential effects compared to TORC1 inhibition". "Work described here
shows that in a variety of model systems, there is advantage of inhibiting
both TORC1 and TORC2 over that of TORC1. Other TORC1/TORC2 inhibitors are
currently in human Phase I/II studies but differ with P529 in that they are
catalytic inhibitors able to inhibit mTOR within the TORC1/TORC2 complexes.
Although these inhibitors inhibit one protein found within the TORC2
complexes via competitive inhibition, they would not be expected to
dissociate the complexes nor inhibit the activity of the other proteins
within the complexes. As P529 causes the dissociation of the complexes, P529
would be expected to have broader activity over that of the mTOR catalytic
inhibitors," said Dr. Sherris.

About Paloma Pharmaceuticals

Paloma Pharmaceuticals, Inc. is a drug development company using
PI3K/Akt/mTOR inhibitors for cancer, ocular, CNS, fibrotic, antiviral and
skin diseases. Paloma owns intellectual property relating to a library of
novel, proprietary, small molecule drugs created through an integrated design
platform incorporating proprietary, customized and industry standard
computational tools.

CONTACT: David Sherris, Paloma Pharmaceuticals, Inc., +1-617-407-6314

David Sherris, Paloma Pharmaceuticals, Inc., +1-617-407-6314

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