| Lymphocyte-targeted therapy | Mechanism of action | Route/Dose | Results | Status | AEDs | |
| Alemtuzumab | Anti-CD52 | IV 12 mg dose/y | 75% ↓ SAD (12 mg dose), 74% ↓ RR | Phase III | ITP (3 pts), Graves disease (20%) | |
| Rituximab | Anti-CD20 | IV (1 gram dose, Q2w, × 2) | 91% ↓ CEL in RRMS | Phase II | Infusion reaction, allergies | |
| Cladribine | Purine nucleoside analog | Oral (3.5 and 5.25 mg/kg total dose) | 58% ↓ RR, 43% disease free | Phase III | HZV, lymphopenia, HA, nasopharyngitis, lymphopenia | |
| Daclizumab | Anti-CD25/anti-IL2 | SQ 2 mg/kg (Q2w) | 72% ↓ CEL in RRMS patients | Phase II | Skin rash, chest discomfort, headaches, lymphopenia | |
| CTLA4Ig | Prevents T cell activation | IV (2, 10.0, 20.0, or 35.0 mg/kg) | No significant changes | Phase I | Lymphadenopathy, urinary tract infections, headaches, blurred vision, and upper respiratory tract infections | |
| Immune sequestration | ||||||
| Fingolimod | Sphingosine-1- phosphate (S1P) analog | Oral (1.25 and 5 mg) | 80% ↓ CEL, 50% ↓ RR | Phase III | Bradycardia, nasopharyngitis, dyspnea, headaches, diarrhea, nausea, encephalitis, skin cancer | |
| SB-683699 | Alpha-4 integrin antagonist | Oral (150 - 1200 mg Twice Daily) | No data available | Phase II | No data available | |
| Unspecific immune suppression | ||||||
| Laquinimod | Antiinflammatory | Oral 0.6 mg/d | 40% ↓ CEL | Phase III | LFT elevation, Budd Chiari | |
| Fumaric acid (BG12) | Antiinflammatory/ Neuroprotective | Oral (120 - 240 mg TID) | 69% ↓ CEL | Phase III | Diarrhea, cramps, nausea and flushing | |
| Teriflunomide | Inhibition of immune cell proliferation | Oral (7 and 14 mg dose) | 61% ↓ CEL | Phase II | Nasopharyngitis, alopecia, nausea, limb pain, diarrhea, and arthralgia | |