Voclosporin

LUPKYNIS is a calcineurin-inhibitor immunosuppressant. The mechanism of voclosporin suppression of calcineurin has not been fully established.

• LUPKYNIS is indicated in combination with a background immunosuppressive therapy regimen [see Clinical Studies ( 14 )] for the treatment of adult patients with active lupus nephritis (LN). Limitations of Use: Safety and efficacy of LUPKYNIS have not been established in combination with cyclophosphamide.

• LUPKYNIS is contraindicated in: Patients concomitantly using strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) because these medications can significantly increase exposure to LUPKYNIS which may increase the risk of acute and/or chronic nephrotoxicity [see Warnings and Precautions ( 5.3 ), Drug Interactions ( 7.1 ), and Pharmacokinetics ( 12.3 )] . Patients with a history of serious or severe hypersensitivity reaction, including anaphylaxis, to LUPKYNIS or any of its excipients [see Warnings and Precautions ( 5.8 )] .contraindicated

Administration : LUPKYNIS must be swallowed whole on an empty stomach. ( 2.1 ) Administer consistently as close to a 12-hour schedule as possible, and with at least 8 hours between doses. ( 2.1 ) If a dose is missed, instruct the patient to take it as soon as possible within 4 hours after missing the dose. Beyond the 4-hour time frame, instruct the patient to wait until the usual scheduled time to take the next regular dose. Instruct the patient not to double the next dose. ( 2.1 ) Instruct patients to avoid eating grapefruit or drinking grapefruit juice while taking LUPKYNIS. ( 2.1 , 7.1 ) Dosage Recommendations : Before initiating LUPKYNIS, establish an accurate baseline estimated glomerular filtration rate (eGFR) and check blood pressure (BP). Use of LUPKYNIS is not recommended in patients with a baseline eGFR ≤45 mL/min/1.73 m 2 unless the benefit exceeds the risk; these patients may be at increased risk for acute and/or chronic nephrotoxicity. ( 2.2 , 5.3 ) Do not initiate LUPKYNIS in patients with baseline BP >165/105 mmHg or with hypertensive emergency. ( 2.2 , 5.4 ) Recommended starting dose: 23.7 mg orally, twice a day. ( 2.3 ) Use LUPKYNIS in combination with mycophenolate mofetil (MMF) and corticosteroids. ( 2.3 ) Modify the LUPKYNIS dose based on eGFR ( 2.3 , 5.3 ): Assess eGFR every two weeks for the first month, every four weeks through the first year, and quarterly thereafter. If eGFR <60 mL/min/1.73 m 2 and reduced from baseline by >20% and <30%, reduce the dose by 7.9 mg twice a day.

Nephrotoxicity (acute and/or chronic): May occur due to LUPKYNIS or concomitant nephrotoxic drugs. Monitor renal function; consider dosage reduction. ( 5.3 ) Hypertension: May require antihypertensive therapy; monitor relevant drug interactions. ( 5.4 ) Neurotoxicity: Including risk of posterior reversible encephalopathy syndrome (PRES); monitor for neurologic abnormalities; reduce dosage or discontinue LUPKYNIS. ( 5.5 ) Hyperkalemia: Risk may be increased with other agents associated with hyperkalemia; monitor serum potassium levels. ( 5.6 ) QT Prolongation: Consider obtaining electrocardiograms and monitoring electrolytes in patients at high risk. ( 5.7 ) Hypersensitivity Reactions: Discontinue LUPKYNIS; treat and monitor until signs and symptoms resolve. ( 5.8 ) Immunizations: Avoid live vaccines. ( 5.9 ) Pure Red Cell Aplasia: Consider discontinuation. ( 5.10 ) 5.1 Lymphoma and Other Malignancies Immunosuppressants, including LUPKYNIS, increase the risk of developing lymphomas and other malignancies, particularly of the skin. The risk appears to be related to the intensity and duration of immunosuppression rather than to the use of any specific agent. Examine patients for skin changes and advise to avoid or limit sun exposure and to avoid artificial UV light (tanning beds, sun lamps) by wearing protective clothing and using a broad spectrum sunscreen with a high protection factor (SPF 30 or higher).

The following clinically significant adverse reactions are described elsewhere in the labeling: Lymphoma and Other Malignancies [see Warnings and Precautions ( 5.1 )] Serious Infections [see Warnings and Precautions ( 5.2 )] Nephrotoxicity due to LUPKYNIS and Drug Interactions [see Warnings and Precautions ( 5.3 )] Hypertension [see Warnings and Precautions ( 5.4 )] Neurotoxicity [see Warnings and Precautions ( 5.5 )] Hyperkalemia [see Warnings and Precautions ( 5.6 )] QTc Prolongation [see Warnings and Precautions ( 5.7 )] Hypersensitivity Reactions [see Warnings and Precautions ( 5.8 )] Immunizations [see Warnings and Precautions ( 5.9 ) ] Pure Red Cell Aplasia [see Warnings and Precautions ( 5.10 )] The most commonly reported adverse reactions (≥3%) were: glomerular filtration rate decreased, hypertension, diarrhea, headache, anemia, cough, urinary tract infection, abdominal pain upper, dyspepsia, alopecia, renal impairment, abdominal pain, mouth ulceration, fatigue, tremor, acute kidney injury, and decreased appetite. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Aurinia Pharmaceuticals at 1-833-672-0028 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Pregnancy: May cause fetal harm. ( 8.1 ) Renal Impairment: Use of LUPKYNIS is not recommended in patients with a baseline eGFR ≤45 mL/min/1.73 m 2 unless the benefit exceeds the risk. If used in patients with severe renal impairment at baseline, LUPKYNIS should be used at a reduced dose. ( 2.4 , 8.6 ) Hepatic Impairment: Mild and moderate hepatic impairment: Dose reduction is required. Severe hepatic impairment: Avoid LUPKYNIS use. ( 2.4 , 8.7 ) 8.1 Pregnancy Risk Summary Avoid use of LUPKYNIS in pregnant women due to the alcohol content of the drug formulation. The available data on the use of LUPKYNIS in pregnant patients are insufficient to determine whether there is a drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with systemic lupus erythematosus (SLE) (see Clinical Considerations ) . LUPKYNIS may be used in combination with a background immunosuppressive therapy regimen that includes MMF. MMF used in pregnant women and men whose female partners are pregnant can cause fetal harm (major birth defects and miscarriage). Refer to the MMF prescribing information for more information on its use during pregnancy.

Metabolism

The whole blood voclosporin pharmacokinetics increase in a greater than dose-proportional manner over the therapeutic range. With a twice daily dosing regimen, voclosporin achieves steady-state after 6 days and the accumulation is approximately 2-fold.

Cases of accidental overdose have been reported with LUPKYNIS; symptoms may include tremor, headache, nausea and vomiting, infections, tachycardia, urticaria, lethargy, and increases in blood urea nitrogen, serum creatinine, and alanine aminotransferase levels. No specific antidote to LUPKYNIS therapy is available. If overdose occurs, general supportive measures and symptomatic treatment should be conducted, including stopping treatment with LUPKYNIS and assessing blood urea nitrogen, serum creatinine, eGFR and alanine aminotransferase levels. Consider contacting a poison center (1-800-222-1222) or medical toxicologist for advice and review of overdosage management recommendations.

• Jan 22, 2021NDANDA213716Aurinia

1. 1Therapy Interrupted95811%
2. 2Product Dose Omission Issue7869.3%
3. 3Hypertension6928.2%
4. 4Headache6677.9%
5. 5Nausea6077.2%
6. 6Diarrhoea5206.2%
7. 7Fatigue4985.9%
8. 8Proteinuria4575.4%
9. 9Blood Pressure Increased3494.1%
10. 10Vomiting3193.8%
11. 11Abdominal Discomfort3133.7%
12. 12Product Use Issue3093.7%
13. 13Glomerular Filtration Rate Decreased2993.5%
14. 14Arthralgia2703.2%
15. 15Dizziness2643.1%

The 10 most recently updated of 27 ClinicalTrials.gov registrations naming Voclosporin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• PRESERVE: LUPKYNIS in Combination With Belimumab, Obinutuzumab or Anifrolumab in Patients With Lupus Nephritis
  Recruiting · Phase 4 · Interventional · 150 enrolled · Aurinia Pharmaceuticals Inc.
  NCT07611214updated 2026-06-12
• Long-Term Voclosporin Treatment in Adolescent and Pediatric Subjects With Lupus Nephritis
  Terminated · Phase 3 · Interventional · 4 enrolled · Aurinia Pharmaceuticals Inc.
  NCT05962788updated 2026-02-10
• Voclosporin in Adolescent and Pediatric Subjects With Lupus Nephritis
  Terminated · Phase 3 · Interventional · 9 enrolled · Aurinia Pharmaceuticals Inc.
  NCT05288855updated 2026-02-10
• Safety and Efficacy of Combination Belimumab and Voclosporin in the Treatment of Proliferative Forms of Lupus Glomerulopathy: Synergy Trial
  Recruiting · Phase 4 · Interventional · 30 enrolled · NephroNet, Inc.
  NCT07225387updated 2025-11-06
• LUPKYNIS Drug-use Results Survey
  Recruiting · Observational · 400 enrolled · Otsuka Pharmaceutical Co., Ltd.
  NCT07053891updated 2025-09-19
• Examining Distinct Immunophenotypes to Validate and Enhance Rational Treatment in Systemic Lupus
  Terminated · Phase 2 · Interventional · 12 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT05306873updated 2025-09-09
• A Prospective Observational Registry of Patients Treated With LUPKYNIS® (Voclosporin) in the US
  Completed · Observational · 229 enrolled · Aurinia Pharmaceuticals Inc.
  NCT05337124updated 2025-06-24
• Special Access for the Use of Voclosporin for Kidney Transplantation
  No longer available · Expanded access · Weill Medical College of Cornell University
  NCT01236287updated 2025-01-29
• Anti-Viral Effects of Voclosporin in COVID-19 Positive Kidney Transplant Recipients
  Completed · Phase 2 · Interventional · 20 enrolled · Leiden University Medical Center
  NCT04701528updated 2024-10-17
• A Study of QLG1074 Combined With Background Therapy in Subjects With Active Lupus Nephritis
  Recruiting · Phase 3 · Interventional · 270 enrolled · Qilu Pharmaceutical Co., Ltd.
  NCT06406205updated 2024-05-09

Frequently asked questions

How does Voclosporin work?

LUPKYNIS is a calcineurin-inhibitor immunosuppressant. The mechanism of voclosporin suppression of calcineurin has not been fully established.

What is Voclosporin used for?

According to FDA labeling, Voclosporin carries indications including: LUPKYNIS is indicated in combination with a background immunosuppressive therapy regimen [see Clinical Studies ( 14 )] for the treatment of adult patients with active lupus nephritis (LN). Limitations of Use: Safety and efficacy of LUPKYNIS have not been established in combination with cyclophosphamide.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Voclosporin?

Voclosporin is classified as Calcineurin inhibitors, Calcineurin Inhibitor Immunosuppressant, Calcineurin Inhibitors, Organic Anion Transporting Polypeptide 1B1 Inhibitors, Organic Anion Transporting Polypeptide 1B3 Inhibitors, P-Glycoprotein Inhibitors.

What are the brand names for Voclosporin?

Voclosporin is marketed under brand names including Lupkynis.

What are the contraindications for Voclosporin?

Voclosporin labeling lists contraindications including: LUPKYNIS is contraindicated in: Patients concomitantly using strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) because these medications can significantly increase exposure to LUPKYNIS which may increase the risk of acute and/or chronic nephrotoxicity [see Warnings and Precautions ( 5.3 ), Drug Interactions ( 7.1 ), and Pharmacokinetics ( 12.3 )] . Patients with a history of serious or severe hypersensitivity reaction, including anaphylaxis, to LUPKYNIS or any of its excipients [see Warnings and Precautions ( 5.8 )] .. Always consult the full prescribing information and a clinician.