30 1,507 NC 5.14/NC 100 7,397 NC 25.24/NC 2 years (TDF) 600 44,300 NA 151.19/NA (carcinogenicity) Females 50,900 NA 173.72/NA Rat (SD) 6 months (TAF) Males 5 740 NA 2.52 25 3,530 NA 12.05 100 15,930 NA 54.37 Females 5 600 NA 2.05 25 4,000 NA 13.65 100 15,140 NA 51.67 2 (TDF) Males 10/300 16,690 NA 56.96/NA (carcinogenicity) 30 2,700 NA 9.22/NA 100 6,600 NA 22.53/NA Females 10/300 15,720 NA 53.65/NA 30 3,060 NA 10.44/NA 100 7,460 NA 25.46/NA Dog (Beagle) 9 months (TAF) Males 2 1,300 90 4.44/0.44 6 3,890 1290 6.25/6.26 18/12 14,900 2160 13.28/10.48 Females 2 1,070 60 3.65/0.29 6 5010 780 17.10/3.79 18/12 12,570 1750 42.90/8.50 Monkey 4 (TAF) Combined 3 350 NC 1.19/NA (Rhesus) 30 5,870 1030 20.03/5.0 Human steady state (10 mg) 293* 206* – – (healthy (TAF) volunteers) * Mean steady AUCSS in pivotal studies for TFV (GS-US-292-0104 and GS-US-292-0111); ** = animal: human plasma AUCss 0–24h NC = not calculated, NA = not applicable
30 1,507 NC 5.14/NC 100 7,397 NC 25.24/NC 2 years (TDF) (carcinogenicity) 600 44,300 NA 151.19/NA Females 50,900 NA 173.72/NA Rat (SD) 6 months (TAF) Males 5 740 NA 2.52 25 3,530 NA 12.05 100 15,930 NA 54.37 Females 5 600 NA 2.05 25 4,000 NA 13.65 100 15,140 NA 51.67 2 (TDF) (carcinogenicity) Males 10/300 16,690 NA 56.96/NA 30 2,700 NA 9.22/NA 100 6,600 NA 22.53/NA Females 10/300 15,720 NA 53.65/NA 30 3,060 NA 10.44/NA 100 7,460 NA 25.46/NA Dog (Beagle) 9 months (TAF) Males 2 1,300 90 4.44/0.44 6 3,890 1290 6.25/6.26 18/12 14,900 2160 13.28/10.48 Females 2 1,070 60 3.65/0.29 6 5010 780 17.10/3.79 18/12 12,570 1750 42.90/8.50 Monkey (Rhesus) 4 (TAF) Combined 3 350 NC 1.19/NA 30 5,870 1030 20.03/5.0 Human (healthy volunteers) steady state (TAF) – (10 mg) 293* 206* – * Mean steady AUCSS in pivotal studies for TFV (GS-US-292-0104 and GS-US-292-0111); ** = animal: human plasma AUCss 0–24h NC = not calculated, NA = not applicable
auspar-elvitegravir-160628.docx