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Title

Stability of 5P12-RANTES, A Candidate Rectal Microbicide, in Human Rectal Lavage

Authors
McGowan, Ian
Published in AIDS Research and Human Retroviruses. 2017, vol. 33, no. 8, p. 768-777
Abstract In the absence of an effective vaccine, strategies to prevent HIV transmission are urgently needed. Condomless receptive anal intercourse represents a major route of transmission, and efforts are being made to develop strategies, in which potent anti-HIV drugs are formulated for topical application to the rectum before sex. 5P12-RANTES is a promising candidate for such a purpose. It is an analog of the human chemokine RANTES/CCL5, which potently blocks CCR5, the principal coreceptor used by HIV to enter and infect target cells. As a protein, 5P12-RANTES is potentially vulnerable to attack by proteases in the rectal environment. In this study, we tested the stability of 5P12-RANTES on exposure to rectal lavage samples obtained from healthy volunteers, using a sensitive HIV entry inhibition assay as an indicator of stability. Varying levels of inactivating activity toward 5P12-RANTES were detected across the different lavage samples. Analysis of even the most aggressive samples indicated that protease activity in the rectal environment is unlikely to impact on the anti-HIV activity of 5P12-RANTES when applied pericoitally at the envisaged clinical dose (1 mM). This study indicates that 5P12-RANTES has adequate stability for further development as an HIV prevention drug for rectal use.
Keywords Anti-Infective Agents/metabolismChemokinesCC/metabolismDrug StabilityHealthy VolunteersHumansHydrolysisRectum/enzymology
Identifiers
PMID: 28177261
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Research group Hiv (835)
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(ISO format)
CERINI, Fabrice et al. Stability of 5P12-RANTES, A Candidate Rectal Microbicide, in Human Rectal Lavage. In: AIDS Research and Human Retroviruses, 2017, vol. 33, n° 8, p. 768-777. https://archive-ouverte.unige.ch/unige:112662

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Deposited on : 2019-01-09

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