Table 1 A comprehensive summary of the most promising OA pharmacological agents
From: Osteoarthritis: a narrative review of molecular approaches to disease management
Agents | Molecular target(s) | Effect |
|---|---|---|
Anikanra | IL-Ra | Anti-inflammatory |
IA dexamethasone | IL-1b, IL-6, and IL-8, MMPs | Anti-inflammatory Chondroprotection |
Sivelestat sodium hydrate | TNF-α and IL-6 through NF-kB and HMGB1. | Anti-inflammatory Chondroprotection |
JQ1 and flavopiridol | -Brd4 and CDK9 -IL-1, IL-6 | Chondroprotection Reduce Synovitis |
Antioxidants: NAC, Mn 3 porphyrin, vitamin E and C | ROS | Chondroprotection Prevent apoptosis |
Caspase inhibitors | Caspases | Chondroprotection Prevent apoptosis |
SS-31 (mitoprotective peptide) | Mitochondrial membrane, cardiolipin. | Maintain MT function and structure Chondroprotection |
Doxycycline | MMP-13 | Chondroprotection Reduce synovitis |
EMBC injection | MMPs | Chondroprotection Osteophyte formation inhibition |
Ipriflavone | IHH pathway MMP-13 Collagen X | Chondroprotection |
SOST/sclerostin | WNT signaling NB-kB MMP-2 and MMP-3 | Chondroprotection Osteophyte formation inhibition |
AMD3100 | PI3K/AKT pathways MMP-1, MMP-3, MMP-13 | Chondroprotection |
Remifentanil | PI3K/AKT pathways | Chondroprotection |
Bisphosphonates: ALN, zoledronic acid | Bone turnover Osteoclastic activity | Regenerative Remodeling Chondroprotective |
GF: BMB7 Sprifermin (FGF18) | Chondrocyte repair | Regenerative Chondroprotection |
MSCs | Chondrocyte repair Inhibits: IL-6, IL-8, CCs, CXCs, cell adhesions (ICAMS-1, VCAMS-1). Stimulates: IL-4, IL-10 Phagocytic PMNs M2 macrophages | Regenerative Immunomodulator Anti-inflammatory |
NBQX | AMPA/KAINATE glutamate receptor | Anti-inflammatory Chondroprotection Reduce pain |
IA liposomal adenosine | A2A receptor | Chondroprotection |
IA bortezomib | Proteasome inhibitor | Ameliorate synovial lymphatic drainage Chondroprotection |
Erlotinib | Integrin a1b1 protection via reduction of EGFR signaling | Chondroprotection Bone volume preservation |
KUS121 (VCP modulator) | TNF-α and IL-6 MMP-1, MMP-13, and ADAMTS5 | Chondroprotection Anti-inflammatory Prevent apoptosis |
Rebamipide | NF-kB, increased COL2A, TIMP3, TGFb, and FGF2 Decreased IL-1b, TNF-α, NF-kB, MMP-3, MMP-13, and ADAMTS5 | Chondroprotection Anti-inflammatory Improved Histology |
Amino sugars: N-acetylglucosamine | Chondrocytes Cytokines | Anti-inflammatory |
Lubricants: HA, lubricin | Synovial lubricant deficiency | Lubrication Chondroprotection |