Table 3.
The Registered Phase 2/3 Clinical Trials on Compounds with Potential Disease-Modifying Effects on Inflammation
| Drug Class/ Compound | Drug in Development | ClinialTrials.gov Identifier | Company | Structure | Targeted Tissue | Mechanism of Action | Route | OA Site | Stage of Development |
|---|---|---|---|---|---|---|---|---|---|
| Anti-IL-1 | |||||||||
| Gevokizumab (XOMA-052) | NCT01683396 | XOMA (USA) | Immunoglobulin G2, anti-(human interleukin 1beta) (human-Mus musculus XOMA 052 heavy chain), disulfide with human-Mus musculus XOMA 052 kappa-chain, dimer | Inflammation | Neutralizing IL-1β | S/C | Hand | Phase 2 (completed in Feb 2014) (n=91) |
|
| NCT01882491 | XOMA (USA) | Phase 2 (completed in Feb 2014) (n=87) |
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| AMG108 | NCT00110942 | Amgen (USA) | A fully human, immunoglobulin subclass G2 (IgG2) monoclonal antibody to IL-1R1 | Inflammation | Inhibiting IL-1 | S/C | Knee | Phase 2 (completed in Nov 2005) (n=160) |
|
|
Lutikizumab (ABT-981) |
NCT02087904 | AbbVie (USA) | A dual variable domain immunoglobulin (DVD-Ig) of the IgG1/k | Inflammation | Neutralizing IL-1α and IL-1β | S/C | Knee | Phase 2 (completed in Dec 2016) (n=350) |
|
| NCT02384538 | AbbVie (USA) | S/C | Hand | Phase 2 (completed in July 2016 (n=132) |
|||||
| Anakinra | NCT00110916 | Amgen Inc | 7-[[2-(2-amino-1,3-thiazol-4-yl)-2-(2,2-dimethylpropanoyloxymethoxyimino)acetyl]amino]-3-ethenyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid | Inflammation | Interleukin-1 receptor antagonist | IA | Knee | Phase 2 (completed in Feb 2005 (n=165) |
|
| Canakinumab | NCT01160822 | Novartis (Switzerland) | Immunoglobulin G1, anti-(human interleukin-1beta (IL-12)) human monoclonal ACZ885; (1Glu>Glp)-gamma heavy chain (221–214ʹ)-disulfide with kappa light chain, dimer (227–227ʹ’:230–230ʹ’)-bisdisulfide | Inflammation | Neutralizing IL-1β | IA | Knee | Phase 2 (completed in July 2011) (n=169) |
|
| Diacerein | NCT02688400 | TRB Chemedica International SA (Switzerland) | 2-Anthracenecarboxylic acid, 4.5-bis(acetyloxy)-9,10-dihydro-9,10-dioxo- (9CI) | Inflammation | Inhibiting the production and activity of IL-1 | Oral | Knee | Phase 3 (completed in Dec 2019) (n=380) |
|
| Anti-IL-6 | |||||||||
| Tocilizumab | NCT02477059 | Assistance Publique - Hôpitaux de Paris | Interleukin-6-Receptor Inhibitor | IV | Hand | Phase 3 (completed in Feb 2019) (n=104) |
|||
| DNA plasmid with IL10 transgene | |||||||||
| XT-150 | NCT04124042 | Xalud Therapeutics, Inc. | - | Inflammation | Suppresses proinflammatory cytokine activity | IA | Knee | Phase 2 Recruiting and estimated completed in Feb 2022 (n=270) |
|
| Anti-TNF | |||||||||
| Adalimumab | NCT00296894 | University Hospital, Ghent | Immunoglobulin G1, anti-(human tumor necrosis factor) (human monoclonal D2E7 heavy chain), disulfide with human monoclonal D2E7 light chain, dimer | Inflammation | Binds specifically to TNF-α and blocks its interaction with endogenous TNF | S/C | Hand | Phase 2 (completed in 2009) | |
| ACTRN12612000791831 | Abbott Australasia Pty Ltd and University of Tasmania | Phase 3 (Completed in Nov 2015) (n=42) |
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| LY3016859 | NCT04456686 | Eli Lilly and Company | High-affinity humanized IgG4 monoclonal antibody | Antibody that binds to key residues in the C-terminal regions of TGF-α and epiregulin, preventing their binding to the EGFR | IV | Knee | Phase 2 (recruiting and estimated to be completed in Sept 2022) (n=125) |
||
| Etanercept | NTR1192 | S/C | Hand | Phase 2 (completed in 2017) (n=90) |
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| Infliximab | NCT01144143 | IA | Knee | Phase 4 (Completed in Jan 2011) (n=16) |
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Abbreviations: EGFR, epidermal growth factor receptor; TGF, transforming growth factor.