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. 2023 Nov 27;9(12):e22912. doi: 10.1016/j.heliyon.2023.e22912

Table 1.

Evaluation of clinical and pre-clinical studies on BTK inhibitors in pemphigus diseases.

Study ID Study Design Sample Size Age (Mean) Gender Ratio (M: male) Type of Disease Previous Treatment BTK Inhibitor Treatment Treatment Duration (weeks) Outcome Measurement Efficacy Adverse events Comorbidities Follow-up Evaluation
Goodale, 2020 [11] Experimental 9 8.2 M: 56% Canine pemphigus foliaceus None Atuzabrutinib 15 mg/kg daily in combination with PRN prednisolone 1 mg/kg twice a day 16–20 Physical examination, anti-Dsc-1 titer, and Wilcoxon rank sum test 33% near-complete remission
44% poor or fair response despite initial improvement
Recurrence of a previously excised mast cell tumor (11%), lymphadenopathy, and Immune-mediated polyarthritis (22%) 33% severe allergic dermatitis, 11% mast cell tumor, 11% chronic pancreatitis Relapse following treatment break from BTKi
Goodale, 2020 [12] Experimental 4 9.25 M: 25% Canine pemphigus foliaceus None Rilzabrutinib, 17–33 mg/kg 20 cPDAI, Serum anti-Dsc-1, and Dsg-1 IgG titers 75% near-complete remission
25% fair response
Pyometra (25%) Not mentioned Not mentioned
Lee, 2017 [9] Case report 1 51 M Paraneoplastic pemphigus Oral Corticosteroid, intravenous Corticosteroid, and Rituximab Ibrutinib 420 mg daily in combination with rituximab 16 Physical examination and clinical evaluation Decrease signs and symptoms, especially cutaneous manifestations Florid ecchymosis and purpura CLL Clinical remission after total taper after 3 months
Murrell, 2021 [13] Clinical trial Phase II 27 51 M: 44% Moderate to severe pemphigus Vulgaris High-dose corticosteroids and rituximab Rilzabrutinib 400–600 mg twice daily with or without low-dose corticosteroid 12 Primary endpoint: CDA within 4 weeks.
Secondary endpoint: time to receive CDA, complete remission, relapse post rilzabrutinib, and corticosteroid usage.
PDAI score, anti-dsg3 antibody level
Primary endpoint CDA; 52%, decrease mean corticosteroid dose,
22% complete remission by week 24,
Improve PDAI score Decrease anti-Dsg3 antibody level
Nausea (15%), upper abdominal pain (11%), headache (15%), cellulitis grade 3 (n = 1), Diabetes mellitus type 2 (n = 1), congenital pulmonary sequestration (n = 1) 12 weeks, successful treatment with Rilzabrutinib alone without moderate to high dose corticosteroids after 12 weeks
Ito, 2018 [10] Case report 1 62 M Paraneoplastic pemphigus Bendamustine combined with rituximab Ibrutinib 420 mg daily Not mentioned Physical examination and clinical evaluation Decrease in signs and symptoms Not mentioned B-CLL/SLL Not mentioned
Yamgami, 2021 [4] Clinical trial Phase II 16 52.5 ± 8.8 M: 50% Pemphigus vulgaris (50%),
Pemphigus foliaceus (37.5%), and pemphigus vegetans (12.5%)
Oral corticosteroid and adjuvant therapy Postprandial oral tirabrutinib 80 mg once daily 52 Primary endpoint: complete remission after 24 weeks.
Secondary endpoint: absolute remission rate over time, remission rate over time, and change in PDAI score, anti-Dsg1 and Dsg3 antibody, and oral corticosteroid exposure over time
Complete remission rate:18.8% after 24 weeks and 50% after 52 weeks
Decrease mean prednisolone dose over time
Decrease anti-Dsg1 and Dsg3 titers baseline.
Decrease PDAI score
Nasopharyngitis (n = 5), influenza (n = 3), pemphigus (n = 3), hypertension (n = 3), folliculitis (n = 2),
oral candidiasis (n = 2,
hepatic enzyme increase (n = 2),
adverse drug reaction: nasopharyngitis (n = 3)
Not mentioned Not mentioned

B-CLL/SLL: B-cell chronic lymphocytic leukemia/small lymphocytic lymphoma; CDA: control of disease activity; CLL: Chronic lymphocytic leukemia; Dsc: desmocollin; Dsg: desmoglein; Ig: immunoglobulin; PDAI: Pemphigus disease area index; mg: milligram; PRN: pro re nata.