Toxicity FTC (Emtriva) A comprehensive package of toxicology studies was submitted in support of FTC registration, documenting toxicity in rodents, chronic toxicity in rodents and monkeys (up to 312 months), carcinogenicity studies in rodents (up to 2 years), genotoxicity in vitro and in vivo, reproductive toxicity in rodents and rabbits, and immunotoxicity in rats. Emtricitabine was generally well-tolerated in the toxicity studies. Relative exposure in repeat-dose toxicity studies Relative exposures (animal: human) in the repeat-dose studies are shown below in Table 3. 3: Emtricitabine (table sourced from Emtriva Submission) Species Dose AUC0-24 h Exposure ratio g.h/mL day ♂ ♀ ♂ ♀ Mouse 1 120 103 73.9 11 8 month 600 499 304 52 32 (Day 32) 3000 1936 1516 201 157 6 167 82.3 93.1 9 10 month 500 248 284 29 (Week 26) 1500 732 899 76 93 6 120 170 115 18 12 month 600 586 491 61 51 (Day 175) 3000 2026 1549 210 161 2 year 80 27.5 23.7 3 2 (Week 250 90.9 91.7 9 10 26) 750 287 323 30 33 Rat 3 120 65.6 69.3 7 7 month 600 329 362 34 38 (Day 90) 3000 1276 1646 132 171 60 2 year 42.9 52.5 4 5
Toxicity FTC (Emtriva) A comprehensive package of toxicology studies was submitted in support of FTC registration, documenting toxicity in rodents, chronic toxicity in rodents and monkeys (up to 312 months), carcinogenicity studies in rodents (up to 2 years), genotoxicity in vitro and in vivo, reproductive toxicity in rodents and rabbits, and immunotoxicity in rats. Emtricitabine was generally well-tolerated in the toxicity studies. Relative exposure in repeat-dose toxicity studies Relative exposures (animal: human) in the repeat-dose studies are shown below in Table 3. 3: Emtricitabine (table sourced from Emtriva Submission) Species Dose day AUC0-24 h g.h/mL Exposure ratio ♂ ♀ ♂ ♀ Mouse 1 month (Day 32) 120 103 73.9 11 8 600 499 304 52 32 3000 1936 1516 201 157 6 month (Week 26) 167 82.3 93.1 9 10 500 248 284 29 1500 732 899 76 93 6 month (Day 175) 120 170 115 18 12 600 586 491 61 51 3000 2026 1549 210 161 2 year (Week 26) 80 27.5 23.7 3 2 250 90.9 91.7 9 10 750 287 323 30 33 Rat 3 month (Day 90) 120 65.6 69.3 7 7 600 329 362 34 38 3000 1276 1646 132 171 2 year 60 42.9 52.5 4 5