Table 1.
Oral agents currently in Phase III trials for multiple sclerosis
| Agent | Molecule type | Therapeutic target | Current/previous use | Expected dosing regimen |
|---|---|---|---|---|
| Fingolimod | Partial sphingosine-1-phosphate receptor agonist | Lymphocyte trafficking | Renal transplantation (failed Phase III trials) | 5.0 or 1.25 mg daily |
| Laquinimod | Derivative of linomide (roquinimex) | Prevention of T-cell activation | Oncology (antiangiogenic agent) | 0.6 mg daily |
| BG-12 | Fumaric acid derivative | Prevention of T-cell activation | Psoriasis (approved in Germany) | 720 mg daily |
| Teriflunomide | Active metabolite of leflunomide | Lymphocyte antiproliferation agent | Rheumatoid arthritis | 7.0 or 14.0 mg daily |
| Cladribine | Purine nucleoside analog pro-drug | Preferential reduction of T and B lymphocyte subtypes | Hairy cell leukemia and lymphoma | Short-course annual dosing regimen (3.5 mg/kg or 5.25 mg/kg over 96 weeks) |