Fiscal Year:
2001
Title:
A NEW SUPPORT FOR THE SYNTHESIS OF BIOACTIVE PEPTIDES
Agency:
HHS
Contract:
N/A
Award Amount:
$100,000.00
Abstract:
Description: (Applicant's abstract) Disulfide-bridged cyclic peptides form the
base for many popularly used cancer-treatment drugs and hormones such as
somatostatin, calcitonins, and oxytocin. However, the production of these
peptides is difficult and expensive. One of the main problems faced during the
production of disulfide-bridged peptides is the removal of the oxidant for the
disulfide bond formation from the final product. Extensive subsequent
purification steps lead to increased manufacturing costs and lower yields,
resulting in annual production costs of about $300 million in the US. We
propose a new procedure in which a resin with a directly attached oxidant is
produced. This procedure will ease the synthesis of complex peptides in a very
cost-effective manner by allowing for the final purification of
disulfide-bridged cyclic peptides to involve only simple filtration. The CLEAR
(cross-linked ethoxylate acrylate resin) base support is unique because it is
compatible with both organic solvents (for the reagent linkage) and aqueous
solutions (for the final peptide recovery). CLEAR has been successful as a
support for peptide and organic synthesis and the proposed chemistry for
oxidant linkage has been demonstrated elsewhere utilizing other solid supports.
Our process will be evaluated in discrete steps beginning with the
characterization of the resin-bound oxidant and culminating with its use in the
synthesis of a bioactive drug. The final cyclic peptides will be characterized
to evaluate purity, by-product formation, and yields in comparison with
existing methods. Currently, no such commercial product exists. The commercial
impact for this product could reach as much as $50 million just for the
synthesis of hypothalamic peptides alone. The success of this proposal will
significantly simplify the synthesis process of many cancer-treatment chemicals
and hormones, and reduce medical costs.
PROPOSED COMMERCIAL APPLICATION:
Somatostatin analogs are important anti-cancer products with an estimated $900 million
in annual sales. These and other disulfide bridged cyclic peptides can benefit from
our resin-bound oxidant. Future derivatives can impact the diagnostics market which
represents a far larger opportunity for this class of products.
Principal Investigator:
Deanna W. Long
Small Business Information at Submission:
PEPTIDES INTERNATIONAL, INC.
11621 ELECTRON DR LOUISVILLE, KY 40223
EIN/Tax ID:
611029008
DUNS:
N/A
Number of Employees:
N/A
Woman-Owned:
No
Minority-Owned:
No
HUBZone-Owned:
No