-- First drug candidate discovered based on computer generated GPCR models and
optimized with integrated computational-medicinal chemistry shows biological
activity --
WOBURN, Mass., and RAMAT GAN, Israel, Sept. 14 /PRNewswire/ -- Predix
Pharmaceuticals Inc., a drug discovery and development company, announced
today that its investigational drug PRX-00023 showed clear induction of
surrogate biomarkers and was well tolerated in single and multiple doses among
volunteers in two Phase I clinical studies. PRX-00023 is a proprietary,
potent serotonin 1A (5HT1A) receptor agonist intended to treat a variety of
neuropsychiatric disorders. Based on the safety and on surrogate marker data
obtained in these studies, the company is planning to initiate Phase II trials
for the treatment of anxiety and depression. In addition, the continued
success of the company's drug discovery efforts will enable Predix to expand
its clinical pipeline with two additional Investigational New Drugs within the
next eight months.
"We are very excited about the results of our single and multiple dose
Phase I trials with PRX-00023. Our goal in this program is to develop PRX-
00023 as an anxiolytic and antidepressant with no sexual side effects and with
rapid onset of action," said Michael Kauffman, MD, PhD, president and chief
executive officer of Predix. "Other compounds that target 5HT1A have been
approved for generalized anxiety and have shown efficacy in major depression.
Our 28-day Phase Ib study demonstrated that PRX-00023 has a substantially
longer half-life, improved bioavailability, and apparently superior side-
effect profile than available 5HT1A agents."
PRX-00023 is designed to selectively interact with the 5HT1A receptor in
the brain. It is a highly potent, novel 5HT1A agonist with about 90%
intrinsic activity on its target receptor. This investigational drug
represents a novel, highly selective chemical class of 5HT1A agonists
discovered using PREDICT(TM), the company's proprietary GPCR modeling,
screening and optimization technology.
"We are encouraged by the initial PRX-00023 clinical trial results as
further validation of our technology platform and our ability to forward
integrate into drug development," said Silvia Noiman, PhD., MBA, co-founder,
general manager, and senior vice president of pipeline management at Predix.
"We look forward to leveraging this milestone to pursue a partnering
opportunity with a pharmaceutical company that can assist in bringing this
potential new treatment to patients in need."
Study Findings
In comparison with marketed 5HT1A agonists as well as others in clinical
development, PRX-00023 showed superior metabolic and selectivity profiles in
preclinical studies. These properties were borne out in the Phase I studies.
This investigational drug was very well tolerated in single and 28-days of
dosing, and showed robust induction of surrogate markers of 5HT1A agonist
activity at doses of 30 mg, 40 mg and 60 mg. The terminal half-life was 10-14
hours, consistent with once daily dosing.
Study Design
The primary objectives of the Phase I clinical trials were to evaluate the
safety, tolerability, pharmacokinetics and pharmacodynamics for single and
multiple doses of PRX-00023 among healthy volunteers. In the single dose
study, doses of 10 mg to 60 mg were administered to healthy male volunteers.
In the multiple dose study, doses of 10 to 60 mg were administered to healthy
female and male volunteers once daily for 28 days.
About PREDICT(TM)
PREDICT(TM) is a proprietary, in silico, three-dimensional GPCR modeling
technology that combines the properties of a protein sequence with those of
its membrane environment without relying on x-ray crystallographic or other
structural methodologies. The PREDICT(TM) algorithm searches through the
receptors' conformational space for the most stable 3D structure of the
transmembrane domains of the protein. To ensure the final model represents
the most stable conformation, the method simultaneously optimizes several
thousand alternative conformations of the receptor. Predix Pharmaceuticals
Inc. has an exclusive worldwide license to this technology. Predix has
applied this technology to create highly refined structures of over 10 GPCRs,
and has successfully used these structures for both high throughput in silico
screening and in lead optimization.
About Predix
Predix is a drug development company integrating computational and
medicinal chemistry to rapidly and efficiently create new drugs targeted to
GPCRs and ion channels. Leveraging its proprietary technology, Predix has
created a diverse clinical and pre-clinical stage drug development pipeline
focused on GPCR and ion channel drug targets. The Company's current pipeline
includes the 5HT1A program which has completed Phase I clinical trials, two
programs in late preclinical stages whose INDs will be submitted by mid-2005,
and four additional programs in lead discovery and lead optimization. Predix
expects to retain a minority of its clinical programs in house through Phase 2
and Phase 3 clinical trials, while generating early upfront and milestone
revenues, as well as royalties from partnering some of its novel compounds
following Phase I safety studies.
In addition to the 5HT1A program, Predix is using its proprietary in
silico GPCR models and computational platform for optimizing antagonists of
serotonin 5HT2B for pulmonary hypertension and pulmonary fibrosis and
serotonin 5HT4 agonists for Alzheimer's Disease and irritable bowel syndrome.
The company is also conducting early work on peptide ligand-based GPCRs and
ion channel drug candidates.
Predix was incorporated in December, 2000, and initiated its medicinal
chemistry and development activities, with its headquarters, in Woburn,
Massachusetts, in September, 2002. The Company was founded in Ramat Gan,
Israel, and maintains its computational chemistry division there.
Contact:
Christine Hayden
(781) 376-0821 Ext. 1010
http://www.predixpharm.com
SOURCE Predix Pharmaceuticals Inc.
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Related links:
http://www.predixpharm.com
CONTACT:
Christine Hayden of Predix Pharmaceuticals
Inc., +1-781-376-0821 Ext. 1010
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