molecules of the month


oral Toll-like receptor TLR7 agonist

3 mg Q2W, Ph. II for HIV/AIDS

from opt. of 8-oxopurine agonist

Science Translational Medicine

Gilead Sciences, Foster City, CA

1 min read

8. The Gilead Toll-like receptor 7 (TLR7) agonist, vesatolimod (GS-9620), is a tolerated, low-dose oral TLR7 agonist. It is intended to induce immune cell activation to help eliminate reservoirs of HIV during antiviral therapy. It was first developed to treat chronic hepatitis B and C infection to induce a liver-targeted antiviral effect without inducing the adverse effects associated with current systemic interferon-alpha (IFN-alpha) therapies. Unfortunately, early clinical data showed it was ineffective against hepatitis B virus (HBV). Preclinical studies with TLR7 agonists in rhesus macaques infected with SIV or SHIV showed virus control after antiretroviral therapy interruption, and combination regimens resulted in complete elimination of the viral reservoir in some animals. In Gilead's Ph. II study with vesatolimod, the TLR7…

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