Short Course
Antiviral Drug Discovery

Small Molecule Candidates to Combat Human Viral Infections

April 15, 2013 | 3:30pm - 6:30pm

This one-day symposium will bring together medicinal chemists who discover and develop new antiviral therapies. With the world becoming a smaller place, viral infections once contained to specific areas are now more wide-spread, increasing the need for novel therapies to combat once-rare viral infections. Thus, in addition to following the promising progress of new all-oral combination therapies to combat HCV, the meeting will also focus on treatments for human-targeted viruses that represent emerging unmet medical needs.

Discovery of GS-9620, an Oral TLR-7 Agonist for the Treatment of Hepatitis B Infection

Randall HalcombRandall Halcomb, Ph.D., Director, Medicinal Chemistry, Gilead Sciences

An unmet need for the treatment of chronic hepatitis B virus infection is a finite therapy
that results in immunologic control of the virus, with potential for viral clearance.
Current best options require a course of interferon treatment, with its associated side
effects, or lifelong treatment with antiviral drugs. This presentation will describe our
work toward the discovery of an orally administered TLR-7 agonist to treat chronic HBV
infection. This resulted in the identification of GS-9620, which is currently under clinical

Developing Antivirals for Emerging Disease

Dennis HrubyDennis E. Hruby, Ph.D., CSO, Siga Technologies

The talk will provide an overview of the dangers of the next viral pandemic emerging from nature, the challenges of developing antivirals against emerging viral diseases and then focus on two examples from the SIGA pipeline, Dengue antivirals and Lassa antivirals.

Development of Smallpox Antiviral Drugs in the Post-Eradication Era

Robert JordanRobert Jordan, Ph.D., Director, Biology, Gilead Sciences

Antiviral drug development for treatment of smallpox has been hampered by the absence of human disease, requiring the use of animal models to establish pharmacokinetic-pharacodynamic relationships to guide effective human dosing strategies. Cidofovir, CMX001, and ST-246 are clinical stage compounds currently being evaluated for treatment of pathogenic orthopoxvirus infections. While all three compounds are effective at treating orthopoxvirus infections in animal models, and are safe and well tolerated in human clinical trials, establishing effective human dosing strategies using animal efficacy data remains a major challenge for the development of these therapeutics.

Developing Pan-Inhibitors of Enveloped Viruses

Benhur LeeBenhur Lee, M.D., Professor, Department of Microbiology, Immunology and Molecular Genetics, School of Medicine at UCLA

Advances in antiviral therapeutics have allowed for effective management of specific viral infections such as HIV, and more recently, HCV infections. Yet, the one-bug-one-drug paradigm of drug discovery is insufficient to meet the looming threat of emerging and re-emerging viral pathogens. We will present our recent work (and those of our close collaborators) on distinct classes of broad-spectrum antiviral compounds that act on the virus-cell membrane fusion process itself, and thus have the property of inhibiting the entry of many enveloped viruses from taxonomically divergent families. Their mechanisms of action suggest new paradigms for antiviral drug development.

Panel Discussion: Future Directions in Antiviral Research

Moderator: Christy Hebner, Ph.D., Research Scientist II, HCV Clinical Virology, Gilead Sciences, Inc.

  • With effective antivirals on the market for management of HIV and HBV and additional promising treatments to cure HCV likely to hit the market soon, what do you foresee as the next major target(s) for antiviral research?
  • Does pursuing viruses affecting smaller populations or the third-world change the way we perform antiviral drug discovery research? If so, how?
  • What do you foresee as the role of small molecules, biologics, and vaccines in the future of antiviral therapies?
  • Predictions—the next big antiviral breakthrough?