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Antiretrovirals for Prevention: Maraviroc Exposure in the Semen and Rectal Tissue of Healthy Male Volunteers after Single and Multiple Dosing
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Reported by Jules Levin
CROI 2010 Feb SF
Kevin C Brown*, Kristine B Patterson, Stephanie A Malone, Nicholas J Shaheen, Heather MA Prince, Julie B Dumond, Melissa Spacek, Paris E Heidt, Myron S Cohen, Angela DM Kashuba
University of North Carolina, Chapel Hill, NC, USA
Conclusions
Maraviroc Semen Exposure Lower than BP
- AUC were 57% (SD) and 62% (MD) of BP
- C12h were 106% (SD) and 71% (MD) of BP
- Discordant with female genital tract
- Protein binding in semen plasma is lower than blood plasma (9% vs 75%)
Maraviroc Rectal Tissue Exposure Higher than BP
- AUC were 9 (SD) and 28 (MD) fold higher than BP
- C12h were 60 (SD) and 91 (MD) fold higher than BP
IMPLICATIONS
Drug Concentrations in Male and Female Genital Tracts may Differ
- Predictions can't always be made with data from one sex
Maraviroc Concentrates in Rectal Tissue
- This is promising for primary prevention
- Can lower or infrequent dosing protect the rectum?
Protein‐free Maraviroc is High in Semen
- Protein‐free concentrations ≥ 28 x IC90
- Will these concentrations minimize local replication and protect recipient tissues?
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