Attenuation of inflammatory polyarthritis in TNF transgenic mice by diacerein: comparative analysis with dexamethasone, methotrexate and anti-TNF protocols

Douni, Eleni; Sfikakis, Petros P.; Haralambous, Sylva; Fernandes, Peter; Kollias, George

doi:10.1186/ar1028

Cited by 57 publications

(31 citation statements)

References 35 publications

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“…The main degradation reaction, detectable by the above-considered techniques in the most stressed conditions, was an hydrolytic pathway leading to the formation of rhein (2).…”

Section: Forced Degradation Studiesmentioning

confidence: 99%

“…1) are anthraquinone compounds that ameliorate the course of osteoarthritis [2][3][4][5][6][7][8]. Diacerhein is a slow acting symptomatic treatment of osteoarthritis, which has demonstrated efficacy on functional manifestations of osteoarthritis and on the structural component.…”

Section: Introductionmentioning

confidence: 99%

“…Diacerhein (1) and its active metabolite rhein (2) [1] ( Fig. 1) are anthraquinone compounds that ameliorate the course of osteoarthritis [2][3][4][5][6][7][8].…”

Section: Introductionmentioning

confidence: 99%

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A validated HPLC stability-indicating method for the determination of diacerhein in bulk drug substance

Giannellini

Salvatore

Bartolucci

et al. 2005

Journal of Pharmaceutical and Biomedical Analysis

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“…The main degradation reaction, detectable by the above-considered techniques in the most stressed conditions, was an hydrolytic pathway leading to the formation of rhein (2).…”

Section: Forced Degradation Studiesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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A validated HPLC stability-indicating method for the determination of diacerhein in bulk drug substance

Giannellini

Salvatore

Bartolucci

et al. 2005

Journal of Pharmaceutical and Biomedical Analysis

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“…The effects of the two products were monitored by weekly assessments of body weight and clinical symptoms. Arthritis symptoms were evaluated macroscopically using a scoring system that has been described previously [26]. Scores ranged from 0.0 [no signs of arthritis] to 3.0 [heavy arthritis with ankylosis detected on flexion, severely impaired movement, and the mouse moribund].…”

Section: In Vivo Efficacy In a Human Tg197 Tnf Transgenic Mouse Modelmentioning

confidence: 99%

Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel^®)

Hofmann

Kronthaler

Fritsch

et al. 2016

Expert Opinion on Biological Therapy

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Background and objective: Biosimilars are approved biologics that are comparable to an originator product with respect to quality, safety and efficacy. Herein, the authors describe the functional and nonclinical studies designed to determine the biosimilarity of GP2015 and originator etanercept (Enbrel ® ). Methods:The development of an Enbrel biosimilar (GP2015) involved extensive characterization of the originator. A step-wise target-directed and iterative technical development program involving state-ofthe-art functional characterization studies and non-clinical evaluations (pharmacokinetics, pharmacodynamics and safety/toxicology) was applied with the aim of confirming that GP2015 is comparable to originator (Enbrel) at the non-clinical level. Results: In in vitro tests, GP2015 and Enbrel had comparable binding affinities to TNF-α, C1q complement and a complete panel of Fc-Receptors. Comprehensive functional characterization testing confirmed the comparability of GP2015 with Enbrel in terms of its ability to bind to and neutralize TNF-α, which reflects the primary mechanism of action of etanercept. Non-clinical data confirmed that the proposed biosimilar to Enbrel, GP2015, is comparable with regards to its pharmacokinetic properties and pharmacodynamic activity, and efficacy as well as safety/toxicity.

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“…Previous studies revealed the beneficial effect of this drug not only for cartilage protection, but also for synovitis and reduction in bone erosion in a mice model of inflammatory arthritis [41]. The mechanisms of the anti-inflammatory effect of diacerein have not yet been completely clarified but Tamura et al (2002) [42] demonstrated, using inflammatory animal models, a different spectrum of anti-inflammatory activity of diacerein than those of NSAIDs, which may be due to the inhibition of IL-1 and the production of reactive oxygen species [42, 43].…”

Section: Discussionmentioning

confidence: 99%

Effects of diacerein on cartilage and subchondral bone in early stages of osteoarthritis in a rabbit model

Permuy

Guede²,

López-Peña

et al. 2015

BMC Vet Res

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BackgroundOsteoarthritis is thought to be the most prevalent chronic and disabling joint disease in animals and humans. At present, there is no ideal treatment option. The aim of this study was to assess the effects of the treatment with oral diacerein on articular cartilage, synovial membrane and subchondral bone in an experimental rabbit model of osteoarthritis by micro-CT evaluation and histological analysis. To this purpose, osteoarthritis was surgically induced on one knee of 16 rabbits using the contralateral knee as healthy controls. Treatment was started three weeks later and lasted eight weeks. Animals were divided into two groups for treatment: Placebo (treated daily with oral saline) and diacerein (treated orally with 1.5 mg/kg/day of diacerein).ResultsSample analysis revealed that this model induced osteoarthritis in the operated knee joint. Osteoarthritis placebo group showed a significant increase in non-calcified cartilage thickness and volume with respect to the control placebo group and important changes in the synovial membrane; whereas the parameters measured in subchondral bone remained unchanged. In the osteoarthritis diacerein-treated group the results showed an improvement with respect to the OA placebo group in all parameters, although the results were not statistically significant.ConclusionThe results of this animal study suggested that the diacerein treatment for OA may be able to ameliorate the swelling and surface alterations of the cartilage and exert an anti-inflammatory effect on the synovial membrane, which might contribute to OA improvement, as well as an anabolic effect on subchondral trabecular bone.

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Attenuation of inflammatory polyarthritis in TNF transgenic mice by diacerein: comparative analysis with dexamethasone, methotrexate and anti-TNF protocols

Cited by 57 publications

References 35 publications

A validated HPLC stability-indicating method for the determination of diacerhein in bulk drug substance

A validated HPLC stability-indicating method for the determination of diacerhein in bulk drug substance

Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel^®)

Effects of diacerein on cartilage and subchondral bone in early stages of osteoarthritis in a rabbit model

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Attenuation of inflammatory polyarthritis in TNF transgenic mice by diacerein: comparative analysis with dexamethasone, methotrexate and anti-TNF protocols

Cited by 57 publications

References 35 publications

A validated HPLC stability-indicating method for the determination of diacerhein in bulk drug substance

A validated HPLC stability-indicating method for the determination of diacerhein in bulk drug substance

Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel®)

Effects of diacerein on cartilage and subchondral bone in early stages of osteoarthritis in a rabbit model

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Product

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Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel^®)