Oral enzyme combination therapy reduces systemic inflammation, urinary CTXII and pain in knee osteoarthritis: a proof-of-mechanism, randomised, crossover, double-blind, placebo-controlled trial

Objectives Oral enzyme combination (OEC) therapy with bromelain, trypsin and rutoside reduces pain and improves function in patients with knee osteoarthritis (OA). Here, we investigated several potential biological mechanisms underlying the clinical effects of OEC therapy in patients with establishe...

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Main Authors: Thomas Pap, Odd Erik Johansen, Yves Henrotin, Valérie Badot, Stefanie Rau, Maximilian von Eynatten, Jean-Emile Dubuc, Siddhartha Lieten, Didier Urbin-Choffray, Karl Brabants
Format: Article
Language:English
Published: BMJ Publishing Group 2025-08-01
Series:RMD Open
Online Access:https://rmdopen.bmj.com/content/11/3/e005433.full
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author Thomas Pap
Odd Erik Johansen
Yves Henrotin
Valérie Badot
Stefanie Rau
Maximilian von Eynatten
Jean-Emile Dubuc
Siddhartha Lieten
Didier Urbin-Choffray
Karl Brabants
author_facet Thomas Pap
Odd Erik Johansen
Yves Henrotin
Valérie Badot
Stefanie Rau
Maximilian von Eynatten
Jean-Emile Dubuc
Siddhartha Lieten
Didier Urbin-Choffray
Karl Brabants
author_sort Thomas Pap
collection DOAJ
description Objectives Oral enzyme combination (OEC) therapy with bromelain, trypsin and rutoside reduces pain and improves function in patients with knee osteoarthritis (OA). Here, we investigated several potential biological mechanisms underlying the clinical effects of OEC therapy in patients with established knee OA with respect to innate immunity, systemic inflammation and cartilage turnover (EudraCT 2020-003154-80, NCT05038410).Methods Patients (age ≥40 years, body mass index (BMI) ≤35 kg/m2) with symptomatic knee OA were randomised to either placebo or OEC, administered 2×3 tablets/day, for 8 weeks before crossing over after a 4-week washout period. Different markers exploring innate immunity, inflammation and cartilage matrix degradation have been measured in the blood using immunoassays or cytometric methods. Data from the modified intention-to-treat population (mITT) were analysed using a generalised linear mixed model. No correction for multiple comparisons was made due to the exploratory nature of the study.Results Altogether, 45 patients were randomised; 43 completed both treatment sequences (mITT; mean age: 63.3 years; mean BMI: 27.4 kg/m2; mean global Knee injury and Osteoarthritis Outcome Score (KOOS): 48.7). OEC significantly increased levels of α2-macroglobulin (p=0.038) and interleukin-10 (p<0.0001) while decreasing urinary carboxyl-terminal cross-linked telopeptide of type II collagen (p=0.038). Patients administered OEC exhibited significant improvements in KOOS Pain (p=0.0464) and Symptoms (p=0.026) subdomains but not globally. OEC was well tolerated, with no serious related adverse events reported in either group.Conclusions One of the key findings of this proof-of-mechanism study is that OEC modulates IL-10 production, suggesting an anti-inflammatory effect in patients with knee OA. This main finding contributes to explaining the effects of OEC on pain and function in these patients.Trial registration number NCT05038410.
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spelling doaj-art-fd1e0eb78b224ca3a2173b6cb25f890a2025-08-20T03:03:03ZengBMJ Publishing GroupRMD Open2056-59332025-08-0111310.1136/rmdopen-2025-005433Oral enzyme combination therapy reduces systemic inflammation, urinary CTXII and pain in knee osteoarthritis: a proof-of-mechanism, randomised, crossover, double-blind, placebo-controlled trialThomas Pap0Odd Erik Johansen1Yves Henrotin2Valérie Badot3Stefanie Rau4Maximilian von Eynatten5Jean-Emile Dubuc6Siddhartha Lieten7Didier Urbin-Choffray8Karl Brabants9Institute of Musculoskeletal Medicine, University Hospital Münster, Münster, GermanyNestle Health Science SA, Vevey, SwitzerlandmusculoSKeletal Innovative Research Lab (mSKIL), Université de Liège, Liège, BelgiumDepartment of Rheumatology, CHU Brugmann, Brussels, BelgiumNestle Health Science SA, Vevey, SwitzerlandNestle Health Science SA, Vevey, SwitzerlandCliniques universitaires Saint-Luc, Brussels, BelgiumDepartment of Geriatrics, Universitair Ziekenhuis Brussel, Brussels, BelgiumCentre Hospitalier Régional de la Citadelle, Liège, BelgiumZiekenhuisnetwerk Antwerpen vzw, Antwerp, BelgiumObjectives Oral enzyme combination (OEC) therapy with bromelain, trypsin and rutoside reduces pain and improves function in patients with knee osteoarthritis (OA). Here, we investigated several potential biological mechanisms underlying the clinical effects of OEC therapy in patients with established knee OA with respect to innate immunity, systemic inflammation and cartilage turnover (EudraCT 2020-003154-80, NCT05038410).Methods Patients (age ≥40 years, body mass index (BMI) ≤35 kg/m2) with symptomatic knee OA were randomised to either placebo or OEC, administered 2×3 tablets/day, for 8 weeks before crossing over after a 4-week washout period. Different markers exploring innate immunity, inflammation and cartilage matrix degradation have been measured in the blood using immunoassays or cytometric methods. Data from the modified intention-to-treat population (mITT) were analysed using a generalised linear mixed model. No correction for multiple comparisons was made due to the exploratory nature of the study.Results Altogether, 45 patients were randomised; 43 completed both treatment sequences (mITT; mean age: 63.3 years; mean BMI: 27.4 kg/m2; mean global Knee injury and Osteoarthritis Outcome Score (KOOS): 48.7). OEC significantly increased levels of α2-macroglobulin (p=0.038) and interleukin-10 (p<0.0001) while decreasing urinary carboxyl-terminal cross-linked telopeptide of type II collagen (p=0.038). Patients administered OEC exhibited significant improvements in KOOS Pain (p=0.0464) and Symptoms (p=0.026) subdomains but not globally. OEC was well tolerated, with no serious related adverse events reported in either group.Conclusions One of the key findings of this proof-of-mechanism study is that OEC modulates IL-10 production, suggesting an anti-inflammatory effect in patients with knee OA. This main finding contributes to explaining the effects of OEC on pain and function in these patients.Trial registration number NCT05038410.https://rmdopen.bmj.com/content/11/3/e005433.full
spellingShingle Thomas Pap
Odd Erik Johansen
Yves Henrotin
Valérie Badot
Stefanie Rau
Maximilian von Eynatten
Jean-Emile Dubuc
Siddhartha Lieten
Didier Urbin-Choffray
Karl Brabants
Oral enzyme combination therapy reduces systemic inflammation, urinary CTXII and pain in knee osteoarthritis: a proof-of-mechanism, randomised, crossover, double-blind, placebo-controlled trial
RMD Open
title Oral enzyme combination therapy reduces systemic inflammation, urinary CTXII and pain in knee osteoarthritis: a proof-of-mechanism, randomised, crossover, double-blind, placebo-controlled trial
title_full Oral enzyme combination therapy reduces systemic inflammation, urinary CTXII and pain in knee osteoarthritis: a proof-of-mechanism, randomised, crossover, double-blind, placebo-controlled trial
title_fullStr Oral enzyme combination therapy reduces systemic inflammation, urinary CTXII and pain in knee osteoarthritis: a proof-of-mechanism, randomised, crossover, double-blind, placebo-controlled trial
title_full_unstemmed Oral enzyme combination therapy reduces systemic inflammation, urinary CTXII and pain in knee osteoarthritis: a proof-of-mechanism, randomised, crossover, double-blind, placebo-controlled trial
title_short Oral enzyme combination therapy reduces systemic inflammation, urinary CTXII and pain in knee osteoarthritis: a proof-of-mechanism, randomised, crossover, double-blind, placebo-controlled trial
title_sort oral enzyme combination therapy reduces systemic inflammation urinary ctxii and pain in knee osteoarthritis a proof of mechanism randomised crossover double blind placebo controlled trial
url https://rmdopen.bmj.com/content/11/3/e005433.full
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