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Abstract

Grant Number: 1R41DA016033-01
PI Name: DIX, THOMAS A.
PI Email: tad@argolyn.com
PI Title:
Project Title: NON-NATURAL AMINO ACIDS IN PEPTIDE DRUG DEVELOPMENT

Abstract: DESCRIPTION (provided by applicant): Argolyn Bioscience Inc. is an early stage biotechnology company that creates novel peptide drugs and diagnostics with greatly improved intrinsic pharmaceutical properties through substitution of non-natural amino acid analogues for arginine (Arg) or lysine (Lys). In proof-of concept studies thus far, application of the Argolyn technology to peptides of therapeutic interest has resulted in dramatic increases in receptor binding, induction of receptor selectivity, blood and plasma stabilization, and delivery through the blood brain barrier (BBB). A key question for our technology is its breadth: can any peptide of biological interest be improved? The Company currently has late-discovery-stage lead candidates in psychosis, pain, and thrombosis; the psychosis and thrombosis leads are being pursued through other STTRs (submitted) and currently active grants. In this proposal, we will use ABS17, our lead candidate in pain, as another vehicle with which to evaluate the robustness of the technology. We propose to evaluate the systemic pharmacokinetics, blood brain barrier access, oral bioavailability, microsomal stability, and preliminary toxicity of ABS17. Completion of the Specific Aims of this proposal, in combination with data already accumulated on this peptide, will "round out" the preclinical work and provide a third peptide candidate on which the Argolyn platform was successfully applied. It will also lead directly into the Phase 2 STTR that will address the technology more generically (immunogenicity, toxicity of the individual non-natural amino acid residues, and model peptides containing them, etc.).

Thesaurus Terms:
aminoacid, biotherapeutic agent, drug design /synthesis /production, peptide, pharmacokinetics
blood brain barrier, drug metabolism, pain, peptide chemical synthesis
laboratory rat

Institution: ARGOLYN BIOSCIENCE, INC.
710 JOHNNIE DODDS BLVD, STE 202
MOUNT PLEASANT, SC 29464
Fiscal Year: 2002
Department:
Project Start: 30-SEP-2002
Project End: 30-NOV-2003
ICD: NATIONAL INSTITUTE ON DRUG ABUSE
IRG: ZRG1


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