Discovery of inhibitors of BK polyomavirus

Period of Performance: 07/02/2016 - 06/30/2017

$342K

Phase 1 SBIR

Recipient Firm

Venatorx Pharmaceuticals, Inc.
Malvern, PA 19355
Principal Investigator

Abstract

PROJECT SUMMARYNovel inhibitors of BK polyomavirus (BKPyV) are urgently needed to prevent the occurrence of virus-inducednephropathy, allograft failure and hemorrhagic cystitis following transplantation. The objective of this Phase I SBIRfeasibility study is to identify drug-like compounds that specifically inhibit BKPyV replication. During the course of thisPhase I funding period, we will execute a hit finding campaign with a library of 100,000 compounds with optimal drug-likeproperties. Quality hits that emerge from the assay will be subjected to follow-on testing that will investigate the potency,selectivity, and mechanism of action. The most interesting of these compounds will be subjected to medicinal chemistrydriven hit-to-lead efforts to explore structure-activity relationships (SAR). The overall goal of this project is to discover oneor more novel lead series, which is defined as a chemotype inhibitor that demonstrates tractable SAR, potent antiviralactivity against the available BKPyV strains and minimal cytotoxicity. Success in these endeavors will trigger thesubmission of a Phase II application that will advance the program from Early Lead Optimization through to CandidateSelection.