Proteolix, Inc. announced that patient dosing has commenced in a Phase 2 clinical
trial of carfilzomib (PR-171), a selective blocker of proteasome activity,
in relapsed solid tumors. A Phase 1b dose-escalation trial of carfilzomib
in patients with advanced solid tumors has recently been completed.


The Phase 2 trial will evaluate the safety and efficacy of single-agent
carfilzomib in patients with recurrent or advanced solid tumors. Subjects
will be enrolled and stratified according to disease type, including
non-small cell lung cancer, small cell lung cancer, ovarian cancer and
renal cancer. The open-label, multi-center clinical trial is a two-stage
design, with pre-determined criteria for continuation after an initial
cohort of patients have been treated. Patients enrolled in the study will
receive carfilzomib twice a week for three weeks with a one week rest
period.



"We are pleased to advance carfilzomib into Phase 2 in patients with
solid tumors, building on the positive safety data and encouraging signals
of activity observed in our Phase 1b trial," said Lori Kunkel, M.D.,
Proteolix' Chief Medical Officer. "In addition to its demonstrated
anti-tumor activity against hematologic malignancies, carfilzomib's unique
profile points to its potential as a new treatment for solid tumor cancers.
Carfilzomib exhibits a highly selective mechanism of action for the
proteasome, an important therapeutic target for cancer, and we believe this
selectivity may reduce or eliminate toxicities seen with other proteasome
inhibitors."



"Targeted agents with novel mechanisms of action can complement current
treatment regimens and improve outcomes. Carfilzomib has demonstrated
tolerability and anti-tumor activity in early studies and these Phase 2
trials in patients with solid tumors are an exciting step forward in the
clinical development of the drug," said Kyri Papadopoulos, M.D., a
principal investigator on the study from South Texas Accelerated Research
Therapeutics (START).



In preclinical models of solid tumors, carfilzomib demonstrates
activity and induces apoptosis of cancer cells when administered on a
consecutive day dose schedule (day 1, day 2). Proteolix completed a
14-patient Phase 1b clinical trial designed to assess the safety of
escalating doses of carfilzomib administered intravenously on this schedule
to patients with a variety of solid tumors. This trial established a
maximum-tolerated dose of 36 mg/m2 for carfilzomib in relapsed patients
with solid tumor malignancies. Proteolix expects to present data from the
Phase 1b trial in a peer-review forum in the second half of this year.



About Carfilzomib



Carfilzomib is a structurally- and mechanistically-novel proteasome
inhibitor that exhibits a high level of selectivity for a single active
site in the proteasome, as well as minimal cross reactivity to other
protease classes. In addition to the Phase 2 trial in solid tumors,
carfilzomib is currently being evaluated in two Phase 2 single-agent trials
in multiple myeloma and a Phase 1 study in lymphoma. Phase 1 clinical
studies have shown that patients with hematologic malignancies who have
relapsed or progressed following multiple therapies can achieve durable
anti-tumor responses with carfilzomib.



About Proteolix



Proteolix, Inc. is a privately-held biopharmaceutical company,
headquartered in South San Francisco, dedicated to discovering, developing
and commercializing pharmaceutical therapies that target certain cancers
and immunological conditions by inhibiting the proteasome and thereby
disrupting protein turnover in cells. Proteolix' lead product, carfilzomib
(PR-171), is currently in clinical studies to evaluate its safety and
efficacy in multiple myeloma, lymphoma and solid tumor malignancies.
Proteolix is also developing a pipeline of next-generation proteasome
inhibitors, including an oral proteasome inhibitor and a selective
immunoproteasome inhibitor. For additional information on Proteolix, please
visit http://www.proteolix.com.


Proteolix, Inc.

http://www.proteolix.com