| Compound | Mode of action | Clinical phase | In vivo validation | Reference |
| Rituximab | Anti-CD20 | Approved | B cell depletion in non-human primates | Looney10 |
| Infliximab | Anti-TNF | Approved | Effects on Inflammatory processes | Maini and Feldman11 |
| Adulimimab (D2E7) | Anti-TNF | Approved | None found on this particular compound | |
| Hydrochloroquine | Antimalarial | Approved | None found on this particular compound | |
| Belimumab | Anti-Blys | III | B cell depletion in non-human primates | Halpern et al12 |
| TRU-015 | Anti-CD20 | II | B cell depletion in non-human primates | Trubion Pharmaceuticals13 |
| HuMax-CD20 | Anti-CD20 | II | B cell depletion in laboratory tests and animal studies | Genmab14 |
| Cimzia | F(ab′)PEGylated anti-TNF | III | None found on this particular compound | |
| AVE9897 (MLN 3897) | CCR1 antagonist | II | None found on this particular compound, however, CCR1 antagonism works therapeutically in mouse CIA | Amat et al15 |
| Rhu-Dex | Anti-CD80 | II | None found on this particular compound | |
| CRx-102 | Dipyridimole and prednisolone | II | None found on this particular compound | |
| 681323 (GSK) | p38 inhibitor | II | None found on this particular compound | GlaxoSmithKline16 |
| 856553 (GSK) | p38 inhibitor | II | None found on this particular compound | GlaxoSmithKline16 |
| 247150 | iNOS inhibition | II | None found on this particular compound | |
| Rosiglitazone XR (GSK) | PPAR agonist | II | None found on this particular compound, however, PPAR agonism works prophylactically in mouse CIA | Tomita et al17 |
| RJW 445380 | Cathepsin S inhibitor | II | Decreased CIA in cathepsin S deficient mice | Nakagawa et al18 |
| UK 427857 | CCR5 inhibitor | II | None found on this particular compound, however, CCR5 antagonism works prophylactically in mouse CIA | Yang et al19 |
CCR, Chemokine (C-C motif) receptor; iNOS, inducible nitric oxide synthase; PEG, polyethylene glycol; PPAR, peroxisome proliferator-activated receptor; TNF, tumour necrosis factor.