Pharmaceuticals, Inc. is a drug discovery and development company offering
unique value for both todays biotech investor and tomorrows
medical patient. By tightly integrating our proprietary 3D computational
chemistry technologies with traditional medicinal chemistry, we have created
a drug discovery platform that dramatically accelerates the generation
of new drugs associated with G-protein coupled receptors (GPCRs) and ion
channels. Our innovative drug discovery platform allows us to readily
work on any of the more than 400 non-olfactory GPCRs as well as ion channels
that are related to major diseases and drive nearly 50% of all pharmaceutical
Predix is focused on GPCRs and ion channels because even though they comprise
only 2% to 3% of the human genome, they are involved in a very wide range
of body functions and processes, including cardiovascular, nervous, endocrine,
and immune systems; and are related to major diseases such as hypertension,
cardiac dysfunction, depression, eating disorders (obesity), certain types
of cancer, pain, schizophrenia, and viral infection. GPCRs and ion channels
are also of great interest to the pharmaceutical industry because they are
currently associated with nearly 50% of all pharmaceutical sales, including
the majority of the best selling drugs on the market such as antihistamines
(e.g., Claritin®, Allegra®), antihypertensives (e.g., Losartan®),
bronchodilators, beta-blockers, and anti-migraine drugs.
Our drug discovery platform uses proprietary 3-dimensional modeling technology
(PREDICT) together with an integrated in silico screening platform
(RISS) to obtain novel 3D structures of GPCRs, ion channels, and novel
drug candidates. In just the past 24 months, our platform has allowed us
to obtain 3D structures for nearly 50 GPCRs covering 8 different families.
Our proprietary drug discovery platform has also successfully identified
novel drug-like compounds that bind specifically to GPCR targets in affinity
assays. Predix has also used its expertise to model the structure of the
pore-forming portion (named HERG) of the cardiac ion channel called IKr
(i.e., rapidly-activating delayed rectifier potassium channel). Using these
structures in our in silico screening processes, hit rates for novel drug
candidates are as high as 24%, compared to <0.1% with standard High Throughput
Screening or HTS (hits are defined as compounds with <10µM experimentally
determined binding affinity). Most of the computationally driven Predix
hits have affinities of <1µM. Predix has also utilized its unique
ICELR lead optimization algorithms to transform its leads into early
Predix is currently the only company which can generate accurate, validated
3D models of ion channels and any GPCR, carry out rapid in silico screening
of novel drug candidates against these structures, and prioritize the resulting
"computational hits." The highest ranking hits are then evaluated in standard
GPCR binding assays in vitro. The Predix technology platform and novel chemical
entities (NCEs) are protected with a number of pending patents in North
America, Europe, and Israel, and we are rapidly enlarging our patent estate
around our NCEs.
Time to Market
The Predix hit-to-lead and lead-optimization processes (structure-activity
determinations) utilize the computed 3D structure of the protein together
with proprietary algorithms which computationally prioritize hits and leads.
Thus, the speed and accuracy of our drug discovery platform yields dramatic
reductions in cycle times, as efficient as programs where the 3D structure
of the target protein is known. Our goal is to move from initiation of a
new project GPCR sequence up to submission of a regulatory filing (IND or
other) for entry into the clinic within 14-18 months. The integration of
computational and medicinal chemistry also reduces our resource requirements
to levels well below that of traditional processes, since efficiencies are
realized at each step of the drug-discovery process.
As a result of these time and resource efficiencies, Predix has the capacity
to drive 1-2 drug candidates into the clinic each year beginning in 2004.
By exploiting our technology suite and optimization process, Predix is rapidly
developing a diverse pipeline of GPCR targeted drugs for neuropsychiatric
disorders and inflammatory diseases.
Predix has identified novel drug candidates with nanomolar affinity for
its leading in house programs. The Company is focused internally on the
5-HT (serotonin) 1A, 5-HT4, 5-HT2B, and neurokinin 1 (NK1) receptors, as well as on one ion channel target (Ito). The 5-HT1A program entered clinical trials in Q1 2004; 5-HT4 and 5-HT2B are
nearing early development candidate (EDC) status. NK1 and Ito are currently in lead optimization. Modeling and in silico screening is ongoing for vasopressin V2, and other novel GPCR targets.
Collaborations Predix is also exploring collaborations with pharmaceutical and biotechnology companies for co-development of GPCR targeted drugs. In these partnerships, Predix will be responsible for generating 3D GPCR structures and performing in silico screening for de novo drug discovery and/or in lead optimization.
The Company has secured its first such a collaboration
with one of the five largest pharmaceutical companies focusing on a specific
GPCR, and is currently in discussions with several additional U.S. and
European biotech and pharmaceutical companies.
Predix was founded as BioInformation Technologies (BioIT), Ltd., in November,
2000, by Silvi Noiman, Oren Becker, and Haim Aviv after extensive research
conducted over seven years in both Tel Aviv University and Harvard University.
The name of the Company was changed in early 2002 in order to reflect its
move into rational drug discovery, preclinical and early clinical development.
In August of 2003, Predix merged with Physiome Sciences, Inc.
The Companys executive offices, business development, medicinal chemistry
and drug development activities are located in Woburn (near Boston), Massachusetts,
USA; the computational research and development groups are located in Ramat
Gan (near Tel Aviv), Israel.
The company currently employs 32 people: 11 in Israel and 21 in the U.S.