From: Garden of therapeutic delights: new targets in rheumatic diseases
 | Target | Representative molecules | Representative clinical trials |
---|---|---|---|
Cytokines and growth factors | IL-6 receptor | Tocilizumab | Completed phase III in RA. Phase III for sJIA. |
 | IL-15 | AMG714 mAb | Insufficient efficacy in phase II (RA). |
 | IL-17 | AIN457 mAb | Phase I in RA, psoriasis, and others. |
 | IL-23/IL-12 | Ustekinumab | Phase II for psoriatic arthritis. |
 | BLyS/BAFF | Belimumab | Lack of efficacy in RA. Phase III in SLE. |
 | BLyS/BAFF and APRIL | Atacicept | Phase I in RA. |
 | LTα/LTβ/LIGHT | Baminercept | Lack of efficacy in RA for LTβ (phase II). |
B-cell targeting | CD20 | Ocrelizumab | Phase II in RA, SLE. |
 |  | Ofatumumab | Phase II in RA. |
 |  | TRU-015 (SMIP) | Phase II in RA. |
 | CD22 | Epratuzumab | Phase II in SLE. |
Costimulation | CD80/CD86 | Abatacept | Phase II/III in SLE. |
Osteoclasts | RANKL | Denosumab | Decreased erosions in RA (phase II). |
Intracellular pathways | JAK1/JAK2/Tyk2 | INCB018424 | Phase I/II in RA and transplant. |
 | JAK3 | CP-690,550 |  |
 | Syk | Fostamatinib | Phase II in RA. |
 | p38 | Multiple compounds | Phase II in RA, ankylosing spondylitis, Crohn disease, and other inflammatory diseases. |
 | PDGF-R, c-kit, c-abl | Imatinib | Phase II in RA and scleroderma. |
 | ERK/MEK | ARRY-162 | Phase II in RA. |
 | PI3Kγ | AS-605240 | Preclinical. |
Chemokines and other GPCRs | CCR5 | Maraviroc | Phase II in RA. |
 | Adenosine A3 receptor agonist | IB-MECA (CF101) | Phase II in RA. |
Ion channels | P2X7 antagonist | CE-224,535 | Phase II in RA. |