Novel GSTP Inhibitors As Potential Oral Myelostimulants
DESCRIPTION (provided by applicant):
Myelosuppression is a common complication of cancer treatment that limits the
efficacy of conventional chemotherapy. It has been demonstrated that
inhibiting glutathione S-transferase (GST)isozyme P1-1 in animals results in
myelostimulation analogous to the action of the recombinant colony-stimulating
factor G-CSF. This Phase I SBIR project will identify GSTP1-1 inhibitors that
are more potent and isozyme-specific than competing inhibitors, by employing a
novel structural motif in the proposed compound libraries. Screening of the
libraries will be performed using an innovative and proprietary chip
technology that will allow large repertoires to be synthesized and screened
more easily, and with throughputs significantly better than currently
available combinatorial methods. Preliminary experience with the chip
technology and with model compounds suggests feasibility will be demonstrated
for the chip screening technology and the proposed structural motif.
Feasibility in Phase I will provide the basis for scale-up of screening and
biologic testing in Phase II. Low-molecular weight GSTP1-1 inhibitors
identified in Phase II that are both highly potent and isozyme-specific may
lead to oral myelostimulants for treating myelosuppression during cancer
PROPOSED COMMERCIAL APPLICATION:
An oral myelostimulant will capture a significant portion of the market for "injection-only"
factors by providing an oral substitute. The current market for recombinant factors is over
$1 billion. The chip libraries will have commercial potential in the $50M research market
related to drug discovery tools as "off-the-shelf" libraries. Market penetration of products
will be achieved through joint ventures with established corporations.
Small Business Information at Submission:
Principal Investigator:John A. Zebala
SYNTRIX BIOCHIP, INC.
208 207TH AVE NE SAMMAMISH, WA 98053
Number of Employees: