On February 13th 2017, Gilead Sciences, Inc. (NASDAQ:GILD) announced the preclinical study results on HIV capsid inhibitors (CAI) evaluation as an antiretroviral treatment (ARV). These inhibitors are said to be active over a long period of time. According to the study, novel HIV -1 capsid inhibitors had high potent antiviral activity and were resistant to vitro ARVs.
Nobert Bischofberger, Chief Scientific Officer, Research and Development Vice President at Gilead, as well as PhD holder, says that capsid inhibition was is an unexplored target for antiviral therapy. The results released show potential role of the particular class as a new, long-acting HIV treatment and prevention method for the future. He also adds that the research is an illustration of Gilead Science’s commitment to advance in the field of HIV and its work to develop and progress treatments for people affected by and living with the disease.
GS-CA1 was found to be an embodied member of a new group of CAIs and is a potent inhibitor of HIV-1 replication in human blood cells. The same displays similarities in potency with many HIV-1 clinical cut-offs. The study, in relation, also found that the CAIs connect to a site at the border of two neighboring monomers within a capsid that accelerate the latter’s assembly in vitro.
Some HIV-1 mutants are resistant to ARVs and some particular variants of HIV capsids, which are M661, Q67H, L56I or N74D. The CAIs identified in the study ensured continued activity in vitro against these mutants. Preclinical studies reveal a double action mode that targets late stages of virion maturity and post-entry functions of capsids. A high amount of in vitro stability is experienced in GS-CA1. It also features a ten-week and over concentration of subcutaneous administrations of a preclinical pharmacokinetic profile that targets plasma concentrations.
Gilead Sciences Inc. has plans underway to select a candidate that will be in charge of development, in Investigational New Drug (IND). This will facilitate toxicology revisions that will also enable Phase 1 clinical trials set to be done in 2018. GS-CA1 has not yet been cleared to be safe.
The findings will be presented at the 2017 Conference on Retroviruses and Opportunistic Infections in an oral session in Seattle.