Table 1.
Immunosuppressive agent | Dose | Main indications in SLE | Adverse events | Special issue | |
---|---|---|---|---|---|
Non-steroidal immunosuppressants | CYC |
Low dose 500 mg, iv, biweekly, 4 times High dose 0.75–1.0 mg/m2, iv, monthly, 6 times |
Severe organ involvement: LN NPSLE Vasculitis |
Cystitis (especially high doses) Gastrointestinal Hematological |
Teratogenic effect Premature ovarian failure Malignancies To prevent bladder toxicity—Mesna administration For overall less toxicity—regimen according to Euro-Lupus [51] |
MMF | 2.0–3.0 g/day, orally |
Hematologic Skin LN in induction and maintenance therapy |
Gastrointestinal Hematological |
Teratogenic effect | |
Calcineurin inhibitors | |||||
CsA | 3.0—5.0 mg/kg/day, orally |
LN Skin Hematologic |
Nephrotoxicity Metabolic (hypertension, hyperglycemia, hyperlipidemia) Hirsutism |
Safe during pregnancy and lactation Continuing with folic acid during pregnancy |
|
Voclosporin | 23.7 mg, twice daily, orally | LN |
Hypertension Nephrotoxicity Serious infections Malignancies |
Combination therapy with MMF in LN Dose adjustment based on eGFR Advantages compared with CsA and tacrolimus with respect to dosing and tolerability |
|
Tacrolimus | 0.2–0.3 mg/kg/day, orally | LN |
Nephrotoxicity Cardiomyopathy |
Combination therapy with MMF in LN with nephrotic proteinuria | |
AZA |
1.0–5.0 mg/kg/day, orally Pregnancy and lactation: ≤ 2.0 mg/kg/day, orally |
Hematologic Skin LN in maintenance therapy |
Gastrointestinal Hepatotoxicity Hematological |
Drug interactions with allopurinol Safe during pregnancy and lactation Mild GCs-sparring effect |
|
MTX | 7.5–25 mg/week, orally/sc |
Joints Skin Serositis |
Gastrointestinal Hepatotoxicity Hematological |
Teratogenic effect Mild GCs-sparring effect Use with caution in elderly patients and in patients with reduced GFR (< 30 ml/min) |
|
Biologics | Belimumab |
Iv: 10.0 mg/kg on days 0, 14 and 28, then every 28 days sc: 200 mg/week In LN: 400 mg/week, 4 times; then 200 mg/week |
Skin Joints LN |
Infections Depression Progressive multifocal encephalopathy |
Complementary treatment in seropositive moderate to severe SLE Not recommended in severe NPSLE FDA-approved to treat seropositive, moderate SLE in children 5–17 years of age |
Anifrolumab | 300 mg, iv, every 4 weeks |
Skin Joints |
Infections, especially herpes zoster |
Complementary treatment in seropositive moderate-to-severe SLE GCs-sparing effect |
|
Rituximab | 500–1000 mg, iv, on days 0 and 14, the next course to be administered after 6 months |
Refractory LN NPSLE |
Progressive multifocal encephalopathy Infections |
Drug off label Different administration schedules |
AZA azathioprine, CsA cyclosporine, CYC cyclophosphamide, eGFR estimated glomerular filtration rate, GCs glucocorticosteroids, FDA Food and Drug Administration, GFR glomerular filtration rate, iv intravenous, LN lupus nephritis, MMF mycophenolate mofetil, NPSLE neuropsychiatric systemic lupus erythematosus, sc subcutaneous