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02594 NEUTRALISING CAPACITY OF TMC120 (DAPIVIRINE) ON A RANGE OF CIRCULATING HIV-1 PRIMARY ISOLATES Njai, Harr F* The most ideal microbicidal must be able to neutralise a wide range of circulating HIV-1 subtypes to prevent new infections, especially in the third world. A pre-treatment system previously developed was used to study the neutralising capacity of TMC120 (R147681, dapivirine) and UC781, on Ba-L (NSI/R5) virus and six primary isolates (subtypes A, A/G, B, C and CRF02_AG) mostly from seropositive African individuals. Monocyte derived dendritic cells (MO-DC) and autologous CD4 T cells co-cultures were used as target cells, because they mimic early in vivo targets of the HIV sexual transmission (including interstitial DC and mucosal T cells). Cell-free virus was first immobilised on a poly-l-lysine (PLL) treated 96-well plate and pre-treated with drug for 1 hour. Afterwards, the drug was thoroughly washed away (6X); target cells were added and cultured for 2 weeks. Viral production was measured on supernatant with HIV antigen ELISA. Negative results were confirmed by showing absence of proviral DNA in the cells. TMC120 inhibited replication of Ba-L with an EC50 value of 49nM, it had a more potent inhibition capacity on the primary isolates with an EC50 value ranging from 22nM - <10nM. UC781 inhibited replication of the reference strain Ba-L with an EC50 value of 500nM. EC50 values on the primary isolates ranged from 34nM 588nM. Both drugs were able to completely prevent HIV infection at 10nM-100nM (TMC120) or 1,000nM-10,000nM (UC781), hence TMC120 is a promising potentially sterilizing microbicide. Drs Harr F Njai |
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