Proteolix Presents Solid Tumor Clinical Trial Results for Carfilzomib at EORTC-NCI-AACR...

Proteolix Presents Solid Tumor Clinical Trial Results for Carfilzomib at
EORTC-NCI-AACR International Conference
Preliminary Evidence of Anti-Tumor Activity Observed in Heavily Pre-Treated
Patients

SOUTH SAN FRANCISCO, Oct. 23 /PRNewswire/ -- Proteolix, Inc., a leader in
the discovery and development of novel therapeutics that target protein
degradation pathways in cancer and autoimmune diseases, today presented
positive data from a Phase 1 clinical trial of carfilzomib (PR-171) in
patients with advanced solid tumors at the 20th EORTC-NCI-AACR symposium on
"Molecular Targets and Cancer Therapeutics" in Geneva, Switzerland.
The Phase 1 clinical trial was designed to assess the safety,
pharmacokinetics and pharmacodynamics of carfilzomib among patients with
advanced solid tumors who had previously failed at least two rounds of prior
treatment with approved chemotherapies. Patients received carfilzomib
administered for two consecutive days for each of the first three weeks on a
four week cycle. Dosing commenced at 20 mg/m2 and escalated thereafter to a
dose of 36 mg/m2.
A total of fourteen patients were enrolled in the study. Of those, one
renal cell (clear cell) patient who had previously failed three prior rounds
of treatment achieved a partial response and remains on the study after eight
months of treatment. One small cell lung cancer patient achieved stable
disease and is continuing on study after six months, and a mesothelioma
patient achieved stable disease for five months.
"Carfilzomib is a highly specific inhibitor of the proteasome and the
results observed in this Phase 1 clinical trial are very encouraging," said
Kyri Papadopoulos, M.D., principal investigator on the study from South Texas
Accelerated Research Therapeutics (START). "Novel agents that positively
impact patient outcomes without adding significant toxicities are desperately
needed to complement and improve existing cancer treatment regimens. I look
forward to the results from further clinical evaluation of the activity of
carfilzomib in a variety of tumor types."
Carfilzomib was generally well tolerated with a low incidence of Grade 3
or higher adverse events. The most common adverse events were reversible
and/or transient fatigue, headache, diarrhea, nausea and constipation.
Notably, incidence of peripheral neuropathy was rare and did not require dose
discontinuation or reduction.
"We are pleased by the promising response results and the solid safety
profile observed in our Phase 1 clinical trial of carfilzomib in patients with
advanced solid tumors. These results demonstrate that carfilzomib appears to
be highly targeted and generally well tolerated at active doses without
resulting in the dose-limiting peripheral neuropathy that typically occurs
with other proteasome inhibitors," said Lori Kunkel, M.D., Proteolix's Chief
Medical Officer. "We believe carfilzomib exhibits strong potential in diverse
cancer indications. Based on these encouraging results, we recently initiated
a Phase 2 clinical trial evaluating carfilzomib's activity in four types of
solid tumor cancers. In addition, we look forward to reporting data from our
ongoing trials of carfilzomib in hematologic malignancies later this year."
Carfilzomib is the first in a new class of highly specific proteasome
inhibitors. Carfilzomib produces specific and sustained inhibition of the
proteasome, leading to apoptosis in cancer cells with minimal off-target
effects. Based on the safety and efficacy observed in this Phase 1 study,
Proteolix initiated a Phase 2 clinical trial of single-agent carfilzomib in
selected solid tumors (non-small cell lung, ovarian, small cell lung, and
renal cell cancers) in May 2008. Carfilzomib is also being studied in
relapsed/refractory multiple myeloma patients as a single agent in two Phase 2
clinical trials and as part of a combination regimen with lenalidomide and
dexamethasone in a Phase 1b trial. For more information on the ongoing
clinical trials with carfilzomib, please visit http://www.clinicaltrials.gov.
Clinical data from Proteolix's Phase 1 clinical trial of carfilzomib were
presented today in a poster titled "A Phase 1 safety, pharmacokinetic and
pharmacodynamic study of carfilzomib, a selective proteasome inhibitor, in
subjects with advanced solid tumors" during the Phase 1 session during the
20th EORTC-NCI-AACR symposium on "Molecular Targets and Cancer Therapeutics"
in Geneva, Switzerland.
About Proteolix
Proteolix, Inc. is a privately-held biopharmaceutical company,
headquartered in South San Francisco, dedicated to discovering, developing and
commercializing novel therapeutics that target protein degradation pathways
for cancer and autoimmune diseases. Proteolix's lead product, carfilzomib
(PR-171), the first in a new class of highly specific proteasome inhibitors,
is currently in multiple Phase 2 clinical studies to evaluate its safety and
efficacy in hematologic and solid tumor malignancies. Proteolix is also
developing a pipeline of novel proteasome inhibitors, including an oral
proteasome inhibitor and a selective immunoproteasome inhibitor. For
additional information on Proteolix, please visit http://www.proteolix.com.
Contact information

Investors: Media Inquiries:
Matthew Ferguson BCC Partners
Chief Financial Officer Karen L. Bergman or Michelle Corral
650-266-2825 650-575-1509 or 415-794-8662
investors@proteolix.com

SOURCE Proteolix, Inc.

Investors, Matthew Ferguson, Chief Financial Officer of Proteolix, Inc.,
+1-650-266-2825, investors@proteolix.com; or Media Inquiries, Karen L.
Bergman, +1-650-575-1509 or Michelle Corral, +1-415-794-8662, both of BCC
Partners for Proteolix, Inc.