Small molecules block viral integration of genetic material into host cells.
Pfizer negotiated an exclusive license to a family of potential anti-HIV compounds known as ledgins, developed by researchers at K.U. Leuven in Belgium. The agreement also gives Pfizer rights to sublicense the IP, in return for an up-front fee and future payments to the university, dependent on development, regulatory, and sales milestones.
Ledgins are a family of compounds demonstrating a new mechanism of action that inhibits interaction between HIV’s viral integrase and the cellular protein LEDGF/p75, the university claims. It is hoped that this activity will form the basis of a class of anti-HIV drugs that circumvent the problems of resistance associated with existing treatments.
In 2002 researchers at K.U. Leuven discovered that HIV uses LEDGF/p75 to integrate its genetic material into the host. A drug discovery program supported by the Centre for Drug Design and Discovery (CD3) at K.U. Leuven Research and Development subsequently identified the first small molecule capable of inhibiting HIV integrase interacting with LEDGF/p75. The family of inhibitors now includes several compound classes that have been developed up to the lead stage, K.U. Leuven claims. “This license agreement constitutes a milestone for CD3 and demonstrates that CD3, as an investment fund and technology transfer platform for innovative academic drug discovery, can deliver new potential drugs by collaborating with university expert research groups,” remarks Patrick Chaltin, CD3 managing director.
Established in 2006, CD3 is the investment fund and technology transfer arm for K.U. Leuven’s small molecule drug discovery IP.