Table 1.
Agents available or under study for reducing IL-1 activity
| Agent | Availability | Mechanism of action | Company | Refs |
|---|---|---|---|---|
| Anakinra | Approved | Receptor antagonist for IL-1RI | Swedish Orphan BioVitrum (see Supplementary information S1 (table)) | – |
| Rilonacept* | Approved | Soluble IL-1 receptor that binds IL-1β>IL-1α>IL-1Ra | Regeneron | 91,102 |
| Canakinumab | Approved | Neutralizing anti-IL-1β IgG1 mAb | Novartis | 60,76,93, 112,142 |
| Gevokizumab | Phase II | Neutralizing anti-IL-1β IgG2 mAb | Xoma | 59, 119 |
| LY2189102 | Phase II | Neutralizing anti-IL-1β IgG1 mAb | Lilly | 77 |
| MABp1 | Phase I/II | Neutralizing anti-IL-1α IgG1 mAb | XBiotech | 78 |
| MEDI-8968 | Phase II/III | Blocking antibody to IL-1RI | MedImmune | 18 |
| CYT013 | Phase I | Therapeutic vaccine targeting IL-1β | Cytos Biotechnology | – |
| sIL-1RI‡ | Halted | Binds IL-1Ra>IL-1α>IL-1β | Amgen | 63,64,65 |
| sIL-1RII§ | Halted | Binds IL-1β complex with soluble IL-1RAcP | Amgen | – |
| EBI-005 | Phase I/II | Chimeric IL-1Ra–IL-1β | Eleven Biotherapeutics | – |
| CMPX-1023 | Preclinical | Alphabody | Complix | – |
| VX-765 | Phase II | Oral caspase 1 inhibitor Vertex | Vertex | – |
IgG1, immunoglobulin G1; IL-1, interleukin 1; IL-1Ra, IL-1 receptor antagonist; IL-1RAcP, IL-1 receptor accessory protein; IL-1RI, IL-1 receptor type I; mAb, monoclonal antibody.
*
A soluble decoy receptor; composed of extracellular domains of IL-1RI fused to the extracellular domains of IL-1RAcP.
‡
Soluble IL-1RI; composed of extracellular domains of IL-1RI; binds to IL-1Ra, IL-1α and IL-1β in decreasing order of affinity: IL-1Ra>IL-1α>IL-1β.
§
Efficacy depends on the binding of IL-1β with soluble IL-1RAcP; binds to IL-1β, IL-1α and IL-1Ra in decreasing order of affinity: IL-1β>IL-1α>IL-1Ra.