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Histopathologic Review of Selected Tissues Covance Laboratories Study No. 6329-231: 26-Week Capsule Toxicity Study with Ammonium Perfluorooctanoate (APFO) in Cynomolgus Monkeys and Riker Laboratories Study No. 0281CR0012: Study of Rats Receiving Fluorochemical FC-143 in Diet for Two Years WIL Research Study No. WIL-180049 Report Date: 14-Jan-2016 SUBMITTED BY: George A. Parker, DVM, PhD, DACVP, DABT Page 1 of 10 INTRODUCTION: This report is based on a Sponsor-directed review of histologic sections of large intestine from Covance Laboratories Study No. 6329-231, a 26-Week Capsule Toxicity Study with Ammonium Perfluorooctanoate (APFO) in Cynomolgus Monkeys and Riker Laboratories Study No. 0281CR0012, a two-year dietary study of fluorochemical FC-143 (ammonium perfluorooctanoate, APFO) in Sprague Dawley rats. The goal of the review was to confirm or refute the histopathologic findings of the original study pathologists with regards to any evidence of test article-related inflammation in the large intestine specimens. METHODOLOGY: For Covance Study No. 6329-231, histopathologic examination was performed on sections of cecum, colon, and rectum. For Riker Study No. 0281CR0012, histopathologic examination was performed on sections of colon. All tissues had been stained with hematoxylin and eosin (H&E). The histologic sections were examined without knowledge of the study pathologist(s)' original findings in individual animals. REVIEW OBSERVATIONS: Histopathologic findings in large intestinal specimens from individual animals are included in the appended Excel spreadsheet. The colon of rats from Riker Study No. 0281CR0012 typically had a mild lymphocytic infiltration, as expected as part of the mucosal immune system. The mucosal inflammatory cell population typically included a minimal number of neutrophils. The neutrophil population was slightly increased in 2 females from the 0 ppm group, 8 males from the 300 ppm group, and 4 females from the 300 ppm group. Overt evidence of subacute inflammation, which included an inflammatory cell infiltration with associated evidence of slight tissue disruption, was observed in the colon of 2 females from the 0 ppm group and 1 male from the 300 ppm group. A number of rats from Riker Study No. 0281CR0012 had nematode parasites in the lumen of the colon. There were no definitive histologic changes associated with presence of the parasites, which were histologically consistent with Syphacia spp. Syphacia spp. were long considered to be non-pathogenic in rats, given the absence of histopathologic changes associated with the parasites, but it is now known that Syphacia spp. infestation can alter cytokine profiles in mice (Michels et al., 2006) and intestinal 1 Page 2 of 10 electrolyte transport in rats (Lubcke eta/., 1992). Occasional monkeys in Covance Study No. 6329-231 had overt lesions that were consistent with Oesophagstomum spp. infestation of the large intestine. This nematode parasite was very common in the intestinal tract of nonhuman primates prior to the advent of highly effective parasiticides such as ivermectin. The large intestinal mucosa of monkeys from Covance Study No. 6329-231 commonly had a mild infiltration of lymphocytes and plasma cells with a few eosinophils and neutrophils. This inflammatory cell population was considered to be normal background histomorphology, though it is possible intestinal parasitism contributed to the inflammatory cell population. The large intestine specimens had no overt histologic evidence of inflammation other than that associated with the parasitic granulomas. CONCLUSIONS: Review of colon sections of Sprague Dawley rats from Riker Study No. 0281 CROO 12 and cecum, colon, and rectum sections of cynomolgus monkeys from Covance Study No. 6329-231 did not reveal evidence of test article-related inflammatory lesions in either study. In both studies the animals had spontaneous parasitic diseases that involved the large intestines. SUBMITTED BY: d t i d George A. Parker, DVM, PhD, DACVP,DABT Reviewing Pathologist 17'eH?l~lf Date 2 Page 3 of 10 REFERENCES: Lubcke, R.; Hutcheson, F. A.; Barbezat, G. O. Impaired intestinal electrolyte transport in rats infested with the common parasite Syphacia muris. Dig Dis Sci 1992, 37(1), 60-64. Michels, C.; Goyal, P.; Nieuwenhuizen, N.; Brombacher, F. Infection with Syphacia obvelata (Pinworm) Induces Protective Th2 Immune Responses and Influences Ovalbumin-Induced Allergic Reactions. Infect Immun 2006, 74(10), 5926-5932. 3 Page 4 of 10 0281CR-0012: 2-year rat study Rat ID 3581 3582 3583 3585 3586 3587 3590 3591 3593 3594 3595 3596 3597 3599 3600 3601 3602 3603 3605 3606 3607 3608 3609 3610 3611 3612 3614 3615 3616 3618 3619 3621 3623 3624 3625 3628 3629 3630 3631 3632 3633 3634 3635 3636 3637 Sex Dose Group Sac Week M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 19 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 99 M 300 ppm 106 M 300 ppm 106 M 300 ppm 72 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 90 M 300 ppm 27 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 Cecum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP Colon EN = essentially normal NP = not present EN EN EN EN EN Neutrophilic infiltration, minimal EN EN EN EN EN EN Neutrophilic infiltration, minimal EN Neutrophilic infiltration, minimal EN EN Neutrophilic infiltration, minimal EN EN EN EN EN Neutrophilic infiltration, minimal EN Autolysis, severe EN EN Autolysis, severe EN EN EN EN Neutrophilic infiltration, minimal EN Neutrophilic infiltration, minimal EN NP EN Neutrophilic infiltration, minimal EN NP EN Inflammation, subacute, mild EN Page 5 of 10 Rectum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP 0281CR-0012: 2-year rat study Rat ID 3639 3640 3641 3644 3645 4641 4643 4644 4645 4646 4647 4648 4649 4650 4651 4653 4654 4657 4658 4659 4660 4661 4662 4663 4665 4667 4668 4670 4672 4673 4675 4677 4678 4679 4680 4681 4682 4683 4684 4685 4686 4688 4690 4691 4693 Sex Dose Group Sac Week M 300 ppm 106 M 300 ppm 72 M 300 ppm 106 M 300 ppm 106 M 300 ppm 106 F 300 ppm 73 F 300 ppm 78 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 88 F 300 ppm 105 F 300 ppm 104 F 300 ppm 96 F 300 ppm 87 F 300 ppm 57 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 94 F 300 ppm 105 F 300 ppm 81 F 300 ppm 92 F 300 ppm 105 F 300 ppm 79 F 300 ppm 105 F 300 ppm 105 F 300 ppm 49 F 300 ppm 105 F 300 ppm 104 F 300 ppm 97 F 300 ppm 94 F 300 ppm 105 F 300 ppm 103 F 300 ppm 75 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 100 F 300 ppm 105 Cecum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP Colon EN = essentially normal NP = not present EN EN EN EN EN EN EN EN EN EN EN NP EN NP NP Neutrophilic infiltration, minimal Autolysis, severe EN EN EN slide glued in box. Immovable EN EN NP EN EN EN EN EN EN EN EN EN EN NP EN NP EN Autolysis, severe EN NP Nematodiasis, minimal EN EN Neutrophilic infiltration, minimal Page 6 of 10 Rectum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP 0281CR-0012: 2-year rat study Rat ID 4694 4695 4696 4697 4698 4700 4701 4702 4703 4705 3518 3519 3521 3523 3524 3525 3526 3528 3529 3530 3531 3532 3533 3534 3536 3537 3538 3539 3540 3541 3542 3544 3545 3547 3548 3549 3552 3553 3554 3555 3556 3557 3558 3560 3561 Sex Dose Group Sac Week F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 105 F 300 ppm 96 F 300 ppm 105 F 300 ppm 87 F 300 ppm 105 F 300 ppm 62 M 0 ppm 106 M 0 ppm 106 M 0 ppm 92 M 0 ppm 95 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 96 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 105 M 0 ppm 106 M 0 ppm 73 M 0 ppm 106 M 0 ppm 106 M 0 ppm 64 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 104 M 0 ppm 85 M 0 ppm 106 M 0 ppm 86 M 0 ppm 106 M 0 ppm 88 M 0 ppm 106 M 0 ppm 102 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 35 M 0 ppm 106 Cecum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP Colon EN = essentially normal NP = not present EN EN Neutrophilic infiltration, minimal Neutrophilic infiltration, minimal EN EN EN EN EN Autolysis, severe EN EN EN EN Nematodiasis, mild EN EN EN EN EN EN EN NP EN Nematodiasis, mild EN EN Nematodiasis, minimal NP EN EN EN Autolysis, severe EN EN EN EN NP EN EN EN EN EN EN Nematodiasis, mild Page 7 of 10 Rectum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP 0281CR-0012: 2-year rat study Rat ID 3562 3563 3564 3565 3566 3567 3569 3571 3572 3573 3574 3576 3577 3578 3579 4576 4577 4579 4580 4581 4583 4584 4586 4587 4591 4592 4593 4594 4595 4596 4597 4598 4599 4600 4602 4603 4604 4605 4606 4607 4609 4611 4612 4613 4614 Sex Dose Group Sac Week M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 84 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 106 M 0 ppm 99 M 0 ppm 55 M 0 ppm 106 M 0 ppm 106 M 0 ppm 86 F 0 ppm 25 F 0 ppm 99 F 0 ppm 84 F 0 ppm 52 F 0 ppm 85 F 0 ppm 105 F 0 ppm 105 F 0 ppm 105 F 0 ppm 105 F 0 ppm 105 F 0 ppm 88 F 0 ppm 105 F 0 ppm 79 F 0 ppm 105 F 0 ppm 78 F 0 ppm 105 F 0 ppm 105 F 0 ppm 102 F 0 ppm 99 F 0 ppm 105 F 0 ppm 105 F 0 ppm 105 F 0 ppm 77 F 0 ppm 105 F 0 ppm 40 F 0 ppm 105 F 0 ppm 105 F 0 ppm 105 F 0 ppm 89 F 0 ppm 105 Cecum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP Colon EN = essentially normal NP = not present Nematodiasis, minimal EN EN NP EN EN NP EN EN Nematodiasis, minimal EN EN EN EN EN EN NP EN EN EN EN NP EN EN EN NP EN EN EN EN EN EN Inflammation, subacute, mild EN EN EN NP Neutrophilic infiltration, minimal EN EN NP NP EN NP EN Page 8 of 10 Rectum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP 0281CR-0012: 2-year rat study Rat ID 4615 4616 4617 4618 4619 4621 4622 4623 4624 4625 4626 4627 4628 4633 4634 4635 4636 4637 4638 4639 Sex Dose Group Sac Week F 0 ppm 105 F 0 ppm 105 F 0 ppm 73 F 0 ppm 93 F 0 ppm 64 F 0 ppm 99 F 0 ppm 62 F 0 ppm 96 F 0 ppm 100 F 0 ppm 100 F 0 ppm 105 F 0 ppm 105 F 0 ppm 105 F 0 ppm 63 F 0 ppm 105 F 0 ppm 94 F 0 ppm 105 F 0 ppm 82 F 0 ppm 105 F 0 ppm 56 Cecum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP Colon EN = essentially normal NP = not present EN EN EN Neutrophilic infiltration, minimal EN Nematodiasis, mild EN EN EN EN EN EN EN Inflammation, subacute, mild EN EN Nematodiasis, minimal EN EN EN Rectum NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP NP Page 9 of 10 Page 10 of 10 6329-231 6-month PFOA monkey study Dose Group Animal ID Last day of dosing Time of necropsy Control 5709 5714 5715 5718 5720 5725 Week 27 Week 27 Week 27 Week 27 Week 27 Week 27 week 27 week 27 week 27 week 40 Week 40 week 27 EN = essentially normal Cecum Colon EN EN EN EN EN Pigment, brown, minimal EN Granuloma, parasitic EN EN EN Infiltrate, eosinophil, minimal 3 mg/kg 5702 Week 27 week 27 EN EN 5706 Week 27 week 27 EN EN 5717 Week 27 week 27 EN EN 5721 Week 27 Day 137 (unscheduled necropsy) EN EN 10 mg/kg 5707 5708 5710 5712 5716 5719 Week 27 Week 27 Week 27 Week 27 Week 27 Week 27 week 27 week 27 week 27 week 40 week 40 week 27 EN Granuloma, moderate (consistent with parasitic granulomas) EN Granuloma, moderate (consistent with parasitic granulomas) 30/20 mg/kg 5724 Day 29 Day 29 (unscheduled necropsy) 5716 Day 43 Week 27 EN 5722 Day 66 Week 27 EN 5703 Day 81 Week 27 EN 5704 Week 27 Week 27 EN 5713 Week 27 Week 27 EN EN EN EN Pigment, brown, mild EN Rectum EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN