One Hundred and Eleventh Series – May 9-10, 2019 Portland, Oregon

Why Do Patients Develop ANCA Disease?

Ronald J. Falk, MD Nan and Hugh Cullman Eminent Professor of Medicine Chair, Department of Medicine University of North Carolina, Chapel Hill NC USA

1 Common Clinical Questions

1. “What is the name of my disease?” “How did I get it?”

What is the cause of disease?

2. “What will make it go away?”

What factors are involved in disease pathogenesis?

3. “What will prevent it from coming back?” What causes a relapse, and what sustains a remission?

2 Our First Case

JP is a 15-year-old female with the sudden onset of coughing up blood in a previously healthy child. There was a 2-week history of flu-like illness.

Physical examination was marked by and pulmonary findings of diffuse crackles in both lung fields.

The serum creatinine was 10 mg/dL.

Treatment was with pulses of methylprednisolone.

3 Antigen Specificity

Cytoplasmic ANCA Perinuclear ANCA

Proteinase 3 Myeloperoxidase (PR3-ANCA), BPI, (MPO-ANCA), 4 others elastase, others The Early ANCA Story

• Autoantibodies against neutrophils and monocytes: tool for diagnosis and marker of disease activity in Wegener’s granulomatosis o van der Woude FJ, Rasmussen N, Lobatto S et al. Lancet 1985; 325(8426):425-9 • Anti-neutrophil cytoplasmic autoantibodies with specificity for myeloperoxidase in patients with and idiopathic necrotizing and crescentic glomerulonephritis o Falk RJ, Jennette JC. N Engl J Med 1988; 318(25):1651-7 • Wegener’s granulomatosis autoantibodies identify a novel diisopropylfluorophosphate-binding protein in the lysosomes of normal human neutrophils o Goldschmeding R et al. J Clin Invest 1989; 84(5):1577-87 • Specificity of anti-neutrophil cytoplasmic autoantibodies for proteinase 3 o Jennette JC, Hoidal JR, Falk RJ. Blood 1990 74(11):2263-4

5 ANCA testing led to:

• A new classification system and a unified, overall name: ANCA vasculitis or ANCA-associated vasculitis

• Recognition that disparate clinical symptoms are part of the same disease process

• Simplification of induction therapy strategies

• Organization of several randomized clinical trials

6 Immune Complex Small Vessel Vasculitis 2012 Chapel Hill Cryoglobulinemic Vasculitis Consensus Conference IgA Vasculitis (Henoch-Schönlein) Vasculitis Nomenclature Hypocomplementemic Urticarial Vasculitis (Anti-C1q Vasculitis) Medium Vessel Vasculitis Polyarteritis Nodosa Anti-GBM Disease

ANCA-Associated Small Vessel Vasculitis Granulomatosis with Polyangiitis (Wegener’s) Eosinophilic Granulomatosis with Polyangiitis Large Vessel Vasculitis (Churg-Strauss) Takayasu Jennette JC, Falk RJ et al. Arthritis Rheum 2013;65:1-11 ANCA-associated vasculitis can affect virtually any tissue and organ in the body:

Pulmonary Glomerular alveolar capillaries capillaries (glomerulonephritis) (capillaritis) Necrosis Crescent

Venules in Small arteries in many organs multiple organs (venulitis) (arteritis)

Capillaries: Venules: Arteries: • Glomerulonephritis • Purpura • Mononeuritis multiplex • Pulmonary capillaritis • Medullary angiitis • Skin nodules and ulcers Concept of Pauci-Immune Glomerulonephritis

Crescentic Glomerulonephritis Immune Pauci- Anti-GBMComplex Immune

>90% ANCA+ 9 Signs and Symptoms of Necrotizing Small Vessel Vasculitis

• Cutaneous purpura, nodules and ulcerations • (mononeuritis multiplex) • and blood in stool • , and renal insufficiency • Hemoptysis and pulmonary infiltrates or nodules • Necrotizing (hemorrhagic) sinusitis • and • Muscle and pancreatic enzymes in blood • Propensity for venous thrombosis 10 Light Microscopic Morphology

FOCAL SCLEROSING GN CHRONIC GN

FOCAL NECROSIS AND CRESCENTIC END STAGE NECROSIS FEW CRESCENTS GN KIDNEY

HEMATURIA and/or ACUTE RAPIDLY SLOWLY PROTEINURIA NEPHRITIS PROGRESSIVE PROGRESSIVE NEPHRITIS NEPHRITIS

11 12

Antigen Specificity

Cytoplasmic ANCA Perinuclear ANCA

Proteinase 3 Myeloperoxidase (PR3-ANCA), BPI, (MPO-ANCA), 14 others elastase, others ANCA Disease

PR3-ANCA Disease

ANCA- MPO-ANCA Negative Disease Disease

FOR EXAMPLE: MPO-ANCA glomerulonephritis MPO-ANCA microscopic polyangiitis PR3-ANCA granulomatosis disease MPO-ANCA Churg-Strauss Syndrome

15 Falk RJ and Jennette JC. J Am Soc Nephrol 2010; 21(5):745-52 CCX168 (Avacopan) azathioprine plasmapheresis

mycophenolate

glucocorticoids

©cjb Current Therapy Plasmapheresis or IV methylprednisolone then IV cyclophosphamide and/or rituximab then azathioprine or rituximab and/or Stop In general, remission rates are on the order of 70% to 93%.

Relapse rates vary from 0% to 50%. Worrying about Over-Immunosuppression

19 Take Home Message #1

ANCA, which was an early biomarker of disease, is now the name of the disease, resulting in earlier diagnosis and more prompt therapy.

20 Common Clinical Questions

1. “What is the name of my disease?” “How did I get it?” What is the cause of disease?

2. “What will make it go away?” What factors are involved in disease pathogenesis?

3. “What will prevent it from coming back?” What causes a relapse, and what sustains a remission?

21 Pathogenesis of ANCA Necrotizing Vasculitis

To cause vasculitis, ANCA must induce this event sequence:

. Leukocyte margination, adherence, and diapedesis

. Leukocyte activation with degranulation and generation of toxic oxygen metabolites

. Vascular necrosis with karyorrhexis and fibrinous insudation

22 JCJ Hypothetical Pathogenesis of ANCA Vasculitis by ANCA

Primed neutrophils are activated by ANCA with involvement of FcR and complement activation amplification.

Modified from: Falk RJ, Jennette JC. J Am Soc Nephrol 2010; 21:745-52 23 MPO-ANCA Mediated Necrotizing and Crescentic Glomerulonephritis and Vasculitis in Mice

Immunize with MPO

MPO-KO 1. Immunize MPO-knockout mice with murine MPO. Anti-MPO antibodies 2. Transfer anti-MPO IgG into Rag2-/- or WT B6 mice.

3. Causes MPO-ANCA-induced pauci-immune necrotizing and crescentic glomerulonephritis and small vessel vasculitis.

Xiao H, Heeringa P, Hu P, Liu Z, Zhao M, Aratani Y, Maeda N, Falk RJ, Jennette JC. J Clin Invest 2002; 110:955-963. Comparative Pathology of Human AAV and Anti-MPO Mouse Model of AAV Mouse Human

Glomerulonephritis Fibrinoid necrosis Crescent

Vasculitis Fibrinoid necrosis Inflammation

25 In this anti-MPO IgG induced mouse model of ANCA glomerulonephritis: • Anti-MPO IgG alone can cause disease

o Jennette JC et al. J Am Soc Nephrol 2006; 17:1235-1242 • Neutrophils are required

o Xiao H et al. Am J Pathol 2005; 167:39-45 • Neutrophil priming exacerbates disease

o Jennette JC et al. J Am Soc Nephrol 2006; 17:1235-1242 • T cells do not cause acute disease

o Xiao H et al. J Clin Invest 2002; 110:955-963 • Abrogation of the alternative complement pathway prevents disease

o Xiao H et al. Am J Pathol 2007; 170:52-64 • C5a receptor antagonists abrogate disease

o Schreiber A et al. J Am Soc Nephrol 2009; 20:289-298 26 An orally active antagonist of human C5a receptor given to mice with knocked in human C5a receptor and knocked out mouse C5a receptor suppresses induction of glomerulonephritis by anti-MPO IgG

Xiao H, et al. J Am Soc Nephrol 2014; 25(2):225-231

Glomerulonephritis Clinical Study Group (UK) CLEAR trial (NCT01363388): Phase 2 trial of CCX168 (complement inhibitor) in ANCA vasculitis

27 Take Home Message #2

ANCA are pathogenic and target circulating cells rather than directly attacking the target organ (vessels).

28 Major Phases of Autoimmune Disease

Genetic Predisposition

ANCA Production + T Cell and Macrophage Defective T and B Cell Mediation of Acute Injury (by neutrophils and monocytes) Response to Injury Regulation

Environmental Resolution Scarring Factors

Relapse/Recurrence

29

Patient Y ANCA Titer ANCA Patient X

Active Disease Disease Remission Active Disease

30 Cryptic Epitopes in MPO

6/4/2019 31 PR3 Transcripts are Detected in Mature Neutrophils and Monocytes But Not in Lymphocytes of ANCA

32 Yang JJ et al. J Am Soc Nephrol 2004; 15:2103-14 PRTN3 and MPO mRNA levels in leukocytes from ANCA patients are significantly increased compared to levels from healthy controls

PRTN3mRNA p<0.0001 MPOmRNA p<0.0001

8000 12000

7000 10000

6000

8000 5000

4000 6000

mRNA Expression mRNA 3000 4000

2000 (Relative to a standard curve)

2000 1000

0 0

HC (n=169) ANCA (n=969) HC (n-169) ANCA (n=969)

33 PRTN3 and MPO mRNA Levels are Closely Correlated with Disease Activity During Disease Course

MPOmRNA 1000 4000

750 3000

500 2000

mRNA Expression mRNA 250 1000

(Relative (Relative to a standard curve) 0 0

A R A A R A A A R A A R A A

34 PR3 and MPO Gene Transcription are Closely Correlated 1600 R² = 0.70 1400 P<0.0001

1200

1000

800

600

400 MPOmRNA (Spearman Rank) MPOmRNA

200

0 0 200 400 600 800 1000 1200 1400 1600 PR3mRNA (Spearman Rank) 35 MPO and PR3 expression results in new protein production in neutrophils isolated from patients with ANCA vasculitis.

McInnis E et al. J Am Soc Nephrol 2015; 26(2): 390-9 36 Transcriptional Dysregulation Linked to Alternative Transcripts

PRTN3 PRTN3-002

About 25% of patients are positive for the alternative transcript, mostly during active disease 37 McInnis E et al. J Am Soc Nephrol 2015; 26(2): 390-9 Epigenetic Silencing of Neutrophil Granule Genes

Ciavatta DJ et al. J Clin Invest 2010 ; 120(9):3209-19 38 DNA Methylation at CpG Islands Leads to Transcriptional Silencing of Gene Promoters

M Methylated Unmethylated

Gene Expression

CpG Island Gene

M M M Gene Expression Repressed

CpG Island Gene PRTN3 Promoter

CTGAGGGCTGTGGCCATGTTGCCCACCTGGCCAGGGACCCCCGAC CG element TTGGGTGGGTGACAGCCAGCCTCCCCGCCCCCACAAAGGTTGG

GACCTTGAGCCCAAAGCCCCCACCTCCTCCCCGGAGTCCGTTCTG PU.1 ACTCCCAGGCTCCCAAGGCAAAAGGAGGAAGTGGGGACCCAGCC

TGGGCATTGGGCAACTCAACGGCCTCTGGCATTGGGCTATAAGA

Met GGAGCTTGACCGTGGGTGCACCCTGGACCCCACCATG PRTN3 Promoter

CTGAGGGCTGTGGCCATGTTGCCCACCTGGCCAGGGACCCCCGAC CG element TTGGGTGGGTGACAGCCAGCCTCCCCGCCCCCACAAAGGTTGG

GACCTTGAGCCCAAAGCCCCCACCTCCTCCCCGGAGTCCGTTCTG PU.1 ACTCCCAGGCTCCCAAGGCAAAAGGAGGAAGTGGGGACCCAGCC

TGGGCATTGGGCAACTCAACGGCCTCTGGCATTGGGCTATAAGA

Met GGAGCTTGACCGTGGGTGCACCCTGGACCCCACCATG Change in DNA Methylation at PRTN3 Promoter Predicts Relapse

42 Jones BE et al. J Am Soc Nephrol 2017; 28(4):1175-87 Take Home Message #4

It is not just the presence of ANCA, but also an epigenetic dysregulation of ANCA antigen genes that may be responsible for causing the disease.

43 Common Clinical Questions

1. “What is the name of my disease?” “How did I get it?” What is the cause of disease?

2. “What will make it go away?” What factors are involved in disease pathogenesis?

3. “What will prevent it from coming back?” What causes a relapse, and what sustains a remission?

44 Acute Injury Response to Injury

Jennette JC et al. Annu Rev Pathol Mech Dis 2013; 8:139–60 Biology of Relapse and Remission

Need for biomarkers of

Remission and Relapse

46 Patient Global Assessment Scored During Times of Remission and Disease Relapse

The Vasculitis Clinical Research Consortium reports an increase in the patient global assessment tool, which captures how patients judge their own disease activity, often precedes detection of disease activity by the physician by at least 3 months.

47 Tomasson G et al. Arthritis Rheum 2014; 66:428-32. Active Urine Sediment

48 What will cause a relapse, and

what sustains a remission?

49 Common Clinical Questions

1. “What is the name of my disease?” “How did I get it?” What is the cause of disease?

2. “What will make it go away?” What factors are involved in disease pathogenesis?

3. “What will prevent it from coming back?” What causes a relapse, and what sustains a remission?

50  UNC Kidney Center