Table 1.
Drugs currently approved by the FDA or undergoing/completed Phase III trials, arranged according to the mechanism of action. Phase I–II trials are not listed.
| Name | Brand name | Mechanism of action | Target disease: FDA status |
|---|---|---|---|
| T cell depleting agents: | |||
| Lymphocyte Immune Globulin (horse), Anti-thymocyte Globulin (rabbit) | Atgam® (horse) Thymoglobulin® (rabbit) | Depleting horse/rabbit polyclonal anti-thymocyte antibody |
renal transplant: approved aplastic anemia: approved (Atgam) |
| Muronomab (OKT3) | Orthoclone OKT® 3 | Mouse anti-human CD3ε mAb | acute transplant rejection, GVHD: approved |
| Teplizumab (hOKT3γ1(Ala-Ala), MGA031)) | humanized OKT3 | T1DM: phase III | |
| Visilizumab | Nuvion® | humanized non-FcR-binding anti-CD3ε mAb | UC: phase III |
| Otelixizumab(TRX 4) | Tolerx® | humanized anti-CD3ε mAb | T1DM: phase III |
| Alemtuzumab | Campath® | humanized anti-CD52 mAb |
B cell CLL: approved MS: phase III |
| Targeting trafficking/adhesion: | |||
| Fingolimod (FTY720) | S1P receptor agonist | relapsing-remitting MS, renal transplant: phase III | |
| CCX282-B | Traficet-EN® | CCR9 inhibitor | CD: phase II/III |
| Natalizumab | Tysabri® | humanized anti-α4 integrin mAb |
relapsing-remitting MS: approved (TOUCH™ program) CD: phase III |
| Efalizumab | Raptiva® | humanized anti-CD11a mAb, blocks LFA-1 | chronic mod-severe plaque psoriasis: approved (pulled from market) |
| Alefacept | Amevive® | Fc fusion protein with extracellular portion of LFA-3, blocks CD2 |
chronic mod-severe plaque psoriasis: approved GVHD: phase III |
| Alicaforsen(ISIS 2302) | anti-sense ICAM-1 inhibitor | CD: phase III | |
| Targeting T cell receptor signaling: | |||
| Cyclosporine A | Gengraf®,Neoral®,Sandimmune® | calcineurin inhibitor | transplant, severe active RA, severe plaque psoriasis: approved |
| Tacrolimus (FK506) | Prograf® (systemic) Protopic® (topical) | calcineurin inhibitor |
transplant: approved mod-severe atopic dermatitis: approved (topical) UC, RA, myasthenia gravis, GVHD: phase III |
| Targeting costimulatory and accessory molecules: | |||
| Abatacept (BMS-188667) | Orencia® | Fc fusion protein with extracellular domain of CTLA-4, blocks CD28–CD80/86 interaction |
mod-severe RA: approved (2nd line agent) early RA, lupus nephritis, IBD, JIA: phase III |
| Belatacept (BMS-224818, LEA29Y) | same as Abatacept, higher affinity | transplant: phase II/III | |
| Zanolimumab (HuMax-CD4) | human anti-CD4 mAb, partially depleting | RA: phase II/III | |
| Targeting cytokines/cytokine signaling: | |||
| Daclizumab (HAT) | Zenapax® | humanized anti-Tac mAb: binds to the α-chain (CD25)of IL-2R |
renal transplant: approved GVHD, lung transplant: phase III |
| Basiliximab | Simulect® | chimeric mAb which blocks the α-chain of the IL-2R |
renal transplant: approved lung/liver transplant: phase III |
| CP690,550 | Jak3 inhibitor | RA: phase III | |
| Sirolimus | Rapamune® | mTOR inhibitor |
renal transplant: approved GVHD: phase III |
| Everolimus (RAD001) | Certican® | mTOR inhibitor | renal/heart transplant: approved in Europe and Canada, filed in the US |
| Ustekinumab (CNTO1275) | Stelara® | human anti-p40 mAb, blocks IL-12/IL-23 | psoriasis: approved in Europe and Canada, filed in the US |
| Tocilizumab (MRA) | Actemra® | humanized anti-IL-6 receptor mAb |
RA: approved in Europe and Japan, filed in US JIA: approved Japan, Phase III US |
Select abbreviations: CLL(chronic lymphocytic leukemia); CD (Crohn's disease); FcR(Fc receptor); GVHD(graft versus host disease); IBD(inflammatory bowel disease); JIA(juvenile idiopathic arthritis); mAb(monoclonal antibody); MS(multiple sclerosis); RA(rheumatoid arthritis); T1DM(type 1 diabetes mellitus); UC(ulcerative colitis)