Lupus Nephritis Medication

Updated: Feb 25, 2021
  • Author: Lawrence H Brent, MD; Chief Editor: Vecihi Batuman, MD, FASN  more...
  • Print
Medication

Medication Summary

Corticosteroids are used in all patients with clinically significant renal disease. Immunosuppressive agents, particularly cyclophosphamide, azathioprine, and mycophenolate mofetil, are used in patients with aggressive renal lesions because they improve the renal outcome. They may also be used in patients with inadequate response or excessive toxicity to corticosteroids. Cyclosporine and tacrolimus have been used in some cases.

Next:

Corticosteroids

Class Summary

Corticosteroids are very useful in controlling acute inflammatory manifestations of systemic lupus erythematosus (SLE). Alone, they may be adequate in treating milder forms of lupus nephritis with a lower risk of progressive renal dysfunction, such as minimal mesangial lupus nephritis, mesangial proliferative lupus nephritis, early focal lupus nephritis, or membranous lupus nephritis. Oral corticosteroids can be used in most patients. If adequate absorption is a concern (eg, bowel edema in a patient with nephrosis), intravenous (IV) methylprednisolone can be used.

Prednisone

Prednisone is commonly used to treat inflammatory manifestations of SLE. Treatment of clinically significant lupus nephritis should include moderate-to-high doses initially.

Methylprednisolone (Medrol, Solu-Medrol, A-Methapred)

Methylprednisolone is used in much the same manner as prednisone. It is more potent: 4 mg of methylprednisolone is equivalent to 5 mg of prednisone. Intravenous dosing is used in the inpatient setting.

Previous
Next:

Immunosuppressives

Class Summary

In particular, cyclophosphamide, mycophenolate, and azathioprine are used in patients with aggressive renal lesions (eg, focal or diffuse lupus nephritis) because they improve renal outcome. These agents can also be used in patients with inadequate response or excessive toxicity to corticosteroids. Mycophenolate mofetil has been shown to be effective for treatment of lupus nephritis. Mycophenolate mofetil was found to be superior to azathioprine in maintaining control and preventing relapses of lupus nephritis in patients who have responded to induction therapy. [62]

Cyclophosphamide

Cyclophosphamide is indicated for treatment of most patients with focal lupus nephritis or diffuse lupus nephritis. Although it has significant toxicity, it has been shown to prevent the progression of nephritis and improve renal outcome.

Azathioprine (Imuran, Azasan)

Azathioprine is useful in moderate-to-severe lupus nephritis. It improves renal outcome, but it does not appear to be as effective as cyclophosphamide, although it is less toxic.

Mycophenolate mofetil (CellCept) or mycophenolic acid (Myfortic)

Mycophenolate mofetil is an option for induction therapy with class III/IV lupus nephritis. It has generally been well tolerated and, in several studies, has been as effective as (and possibly more effective than) more traditional therapies, including cyclophosphamide and azathioprine, with less toxicity. The American College of Rheumatology guidelines recommend mycophenolate mofetil as the preferred agent for African Americans and Hispanics.

Hydroxychloroquine (Plaquenil)

The exact anti-inflammatory mechanism of action of hydroxychloroquine is not well understood. Its effect is thought be related to increasing the pH within intracellular vacuoles, which alters protein degradation by acidic hydrolases in the lysosomes and assembly of macromolecules in the endosomes and the Golgi apparatus. Acidic pH is required for protein antigen processing for presentation on antigen-presenting cells with MCH class II receptors. The ultimate effect of hydroxychloroquine is to reduce antigen presentation by antigen-presenting cells to CD4- positive T lymphocytes, resulting in downregulation of the immune response. The American College of Rheumatology guidelines recommend that all patients with SLE and nephritis be treated with a background of hydroxychloroquine, unless contraindicated.

Previous
Next:

Monoclonal Antibodies

Belimumab (Benlysta)

Monoclonal antibody blocks the binding of BLyS (a B-cell survival factor) to B-cells. It inhibits the survival of B-cells and reduces B-cell differentiation into immunoglobulin-producing plasma cells. It is indicated for the treatment of active lupus nephritis in adults who are receiving standard therapy.

Rituximab (Rituxan, Riabni, Rituximab-abbs)

Monoclonal chimeric antibody directed against CD20 and induces a long-lasting B-cell depletion. Rituximab has been used as off-label treatment for lupus nephritis. It is recommended by EULAR/ERA-EDTA as an alternative option for nonresponsive class III to V lupus nephritis.

Previous
Next:

Calcineurin Inhibitors

Class Summary

Through the inhibition of calcineurin, these therapies reduce cytokine activation, block interleukin IL-2 expression and T-cell mediated immune responses.

Cyclosporine (Gengraf, Neoral, Sandimmune)

Cyclosporine inhibits production and release of interleukin II and interleukin II-induced activation of resting T-lymphocytes. Use is not approved by the FDA but recommended by EULAR/ERA-EDTA as an alternative option for pure class V lupus nephritis.

Tacrolimus (Astagraf XL, Envarsus XR, Hecoria)

Tacrolimus is an immunosuppressive agent that inhibits of calcineurin-induced dephosphorylation of synaptopodin, a critical protein that regulates actin filaments of the podocyte cytoskeleton. Use is not approved by the FDA but recommended by EULAR/ERA-EDTA as an alternative option for pure class V lupus nephritis. 

Voclosporin (Lupkynis)

Novel high potency calcineurin-inhibitor reduces T-cell activation and stabilizes podocytes, which protect against proteinuria. First oral therapy approved in combination with immunosuppressive therapy for lupus nephritis

Previous