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Voclosporin: Drug information

Voclosporin: Drug information
2025© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Voclosporin: Patient drug information"

For abbreviations, symbols, and age group definitions show table
ALERT: US Boxed Warning
Malignancies and serious infections

Increased risk for developing malignancies and serious infections with voclosporin or other immunosuppressants that may lead to hospitalization or death.

Brand Names: US
  • Lupkynis
Pharmacologic Category
  • Calcineurin Inhibitor;
  • Immunosuppressant Agent
Dosing: Adult

Note: Initiation of therapy is not recommended in patients with an eGFR ≤45 mL/minute/1.73 m2 unless benefits outweigh risks or in patients with BP >165/105 mmHg or with hypertensive emergency. For patients not experiencing a therapeutic benefit by 24 weeks, consider discontinuation of therapy.

Lupus nephritis

Lupus nephritis: Oral:

Initial: 23.7 mg twice daily in combination with corticosteroids and mycophenolate. Refer to the dosing in renal impairment section for further guidance on initiating therapy in patients with severe impairment or for dose adjustments as determined by eGFR following initiation of therapy.

Missed doses: If a dose is missed by >4 hours, omit that dose and take the next dose at the regularly scheduled time; do not administer extra doses to make up for a missed dose.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Dosage adjustment for renal impairment prior to treatment initiation: Note: Patients with eGFR ≤45 mL/minute/1.73 m2 (determined using CKD-EPI) were excluded from clinical trials (Ref); do not initiate therapy unless benefits outweigh the risks. Also, the manufacturer recommendations for baseline dose adjustments are expressed in terms of CrCl and based on pharmacokinetic data utilizing the Cockroft-Gault formula.

CrCl >30 mL/minute: Initial: No dosage adjustment necessary.

CrCl <30 mL/minute: Initial:15.8 mg twice daily.

Dosage adjustment for eGFR reductions during treatment : Note: Patients with a persistent decrease of eGFR should be evaluated for chronic calcineurin-inhibitor nephrotoxicity.

eGFR <60 mL/minute/1 .73 m2 and reduced from baseline by >20% and <30%: Decrease dose by 7.9 mg twice daily; reassess eGFR within 2 weeks and if eGFR is still reduced by >20% further reduce dose to 7.9 mg twice daily.

eGFR <60 mL/minute/1 .73 m2 and reduced from baseline by ≥30%: Discontinue therapy; reassess eGFR within 2 weeks and consider reinitiating at a lower dose (eg, 7.9 mg twice daily) only if eGFR has returned to ≥80% of baseline.

Note: In patients that required a decrease in dose due to eGFR, consider increasing the dose by 7.9 mg twice daily for each eGFR measurement that is ≥80% of baseline; do not exceed starting dose (23.7 mg twice daily).

Dosing: Liver Impairment: Adult

Mild to moderate impairment (Child-Pugh class A or B): 15.8 mg twice daily.

Severe impairment (Child-Pugh class C): Use not recommended.

Dosing: Adjustment for Toxicity: Adult

Hypertension: BP >165/105 mmHg or hypertensive emergency: Discontinue therapy and initiate antihypertensives.

Neurotoxicity: Consider dosage reduction or discontinuation of therapy.

Pure red cell aplasia: Discontinuation of therapy should be considered with diagnosis of pure red cell aplasia.

Dosing: Older Adult

Refer to adult dosing; use caution.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Cardiovascular: Hypertension (19%; including severe hypertension)

Gastrointestinal: Diarrhea (19%)

Genitourinary: Urinary tract infection (10%)

Hematologic & oncologic: Anemia (12%)

Nervous system: Headache (15%)

Renal: Mean glomerular filtration rate decreased (26%)

Respiratory: Cough (11%)

1% to 10%:

Dermatologic: Alopecia (6%), hypertrichosis (≤3%)

Gastrointestinal: Abdominal pain (5%), decreased appetite (3%), dyspepsia (6%), gingivitis (≤3%), oral mucosa ulcer (4%), upper abdominal pain (7%)

Nervous system: Fatigue (4%)

Neuromuscular & skeletal: Tremor (3%)

Renal: Acute kidney injury (3%), renal insufficiency (6%)

Frequency not defined:

Cardiovascular: Prolonged QT interval on ECG (dose-dependent)

Dermatologic: Pyoderma gangrenosum

Endocrine & metabolic: Hyperkalemia

Gastrointestinal: Gastroenteritis

Genitourinary: Azotemia, cervical carcinoma, oliguria, proteinuria

Hematologic & oncologic: Breast neoplasm (excision), malignant lymphoma, malignant neoplasm, skin neoplasm

Infection: Herpes zoster infection (including herpes zoster cutaneous disseminated), infection (including serious infection), opportunistic infection (including cytomegalovirus disease)

Nervous system: Central nervous system disease (including disturbance in attention, dizziness, hypoesthesia, migraine, paresthesia, reversible posterior leukoencephalopathy syndrome, postherpetic neuralgia, seizure, severe nervous system disease, tension headache)

Ophthalmic: Chorioretinitis (cytomegalovirus)

Renal: Increased serum creatinine, nephrotoxicity, renal failure syndrome

Respiratory: Pneumonia, upper respiratory tract infection, viral upper respiratory tract infection

Contraindications

Serious or severe hypersensitivity to voclosporin or any component of the formulation; concomitant use of CYP3A4 inhibitors (eg, ketoconazole, itraconazole, clarithromycin).

Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Warnings/Precautions

Concerns related to adverse effects:

• Cardiovascular: Voclosporin has been shown to prolong the QTc interval in a dose-dependent manner after single dose administration at a dose higher than the recommended lupus nephritis therapeutic dose. Concomitant use with other QTc prolonging medications may result in clinically significant QT prolongation. The risk of occurrence of torsade de pointes and/or sudden death in association with the use QTc prolonging medications may be increased in certain circumstances (eg, patients with bradycardia, congenital QT prolongation electrolyte disturbances).

• Hyperkalemia: Mild-to-severe hyperkalemia may occur; risk may be increased with concomitant use of medicines associated with hyperkalemia (eg, angiotensin-converting enzyme inhibitors, angiotensin receptor blockers, potassium sparing diuretics).

• Hypertension: May occur; use of antihypertensives or dose reduction of voclosporin may be required. Discontinue therapy for significant increase in BP (>165/105 mmHg) or for hypertensive emergency.

• Infections: Serious, including fatal, infections (bacterial, viral, fungal, protozoal) may occur. Assess risk versus benefits of continued therapy in patients that develop an infection.

• Malignancies: Malignancies, including lymphoma and other malignancies (predominantly skin malignancies), may occur with immunosuppressants. The risk for malignancies is related to intensity/duration of therapy. Limit or avoid sun and UV light exposure; use appropriate sun protection.

• Nephrotoxicity: Nephrotoxicity (acute or chronic) may occur; risk may be increased with use of other nephrotoxic drugs (eg, sirolimus, cyclosporine).

• Neurotoxicity: Neurotoxicity, including tremors, paresthesias, headache, mental status changes, and motor/sensory function changes, may occur; severe toxicity, including posterior reversible encephalopathy syndrome, delirium, seizure, and coma have also been reported.

• Pure red cell aplasia: Pure red cell aplasia (PRCA) has been reported in patients receiving calcineurin-inhibitor immunosuppressants. Use with caution in patients with risk factors for PRCA, including parvovirus B19 infection, underlying disease, or use of concomitant medications associated with PRCA (eg, mycophenolate). Discontinuation of therapy should be considered with diagnosis of PRCA.

Disease-related concerns:

• Hepatic impairment: Dose reductions are recommended when initiating in patients with mild and moderate impairment (Child-Pugh class A and Child Pugh class B). Use is not recommended in patients with severe impairment (Child-Pugh class C).

• Renal impairment: Use is not recommended unless benefits outweigh the risks in patients with baseline eGFR ≤45 mL/minute/1.73 m2. Dose reductions are recommended if initiated in patients with severe renal impairment at baseline, and dose reduction or discontinuation is recommended in patients with eGFR <60 mL/minute/1.73 m2 who experience a deterioration of eGFR >20% from baseline.

Other warnings/precautions:

• Immunizations: Patients should be brought up to date with all immunizations before initiating therapy. Patients should not be immunized with live vaccines during or shortly after treatment and should avoid close contact with recently vaccinated (live vaccine) individuals. Inactivated vaccines may be administered (response may be diminished).

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Lupkynis: 7.9 mg

Generic Equivalent Available: US

No

Pricing: US

Capsules (Lupkynis Oral)

7.9 mg (per each): $105.70

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Oral: Administer on an empty stomach as close to every 12 hours as possible, but with a minimum of 8 hours between doses. Swallow capsules whole; do not crush, divide, or open.

Medication Guide and/or Vaccine Information Statement (VIS)

An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:

Lupkynis: https://d1io3yog0oux5.cloudfront.net/auriniapharma/files/pages/lupkynis-medication-guide/FPI-0010+Approved+LUPKYNIS+Med+Guide+22Jan2021.pdf

Use: Labeled Indications

Lupus nephritis: Treatment of adult patients with active lupus nephritis, in combination with a background immunosuppressive therapy regimen.

Limitations of use: Safety and efficacy have not been established in combination with cyclophosphamide; use not recommended.

Medication Safety Issues
Sound-alike/look-alike issues:

Voclosporin may be confused with cyclosporine.

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (immunosuppressant agent, parenteral and oral) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Community/Ambulatory Care and Long-Term Care Settings).

Metabolism/Transport Effects

Substrate of CYP3A4 (Major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits P-glycoprotein;

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Abrocitinib: May increase immunosuppressive effects of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid

Afatinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Afatinib. Management: If combined, administer the P-gp inhibitor simultaneously with, or after, the dose of afatinib. Monitor closely for signs and symptoms of afatinib toxicity and if the combination is not tolerated, reduce the afatinib dose by 10 mg. Risk D: Consider Therapy Modification

Aliskiren: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Aliskiren. Risk C: Monitor

Androgens: Hypertension-Associated Agents may increase hypertensive effects of Androgens. Risk C: Monitor

Antithymocyte Globulin (Equine): Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Antithymocyte Globulin (Equine). Specifically, these effects may be unmasked if the dose of immunosuppressive therapy is reduced. Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Antithymocyte Globulin (Equine). Specifically, infections may occur with greater severity and/or atypical presentations. Risk C: Monitor

Baricitinib: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Baricitinib. Risk X: Avoid

BCG Products: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of BCG Products. Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of BCG Products. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Beta-Acetyldigoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Beta-Acetyldigoxin. Risk C: Monitor

Bilastine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Bilastine. Risk X: Avoid

Brincidofovir: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Brincidofovir. Risk C: Monitor

Brivudine: May increase adverse/toxic effects of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid

Celiprolol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Celiprolol. Risk C: Monitor

Chikungunya Vaccine (Live): Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Chikungunya Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Chikungunya Vaccine (Live). Risk X: Avoid

Cladribine: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Cladribine. Risk X: Avoid

Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor

Coccidioides immitis Skin Test: Coadministration of Immunosuppressants (Therapeutic Immunosuppressant Agents) and Coccidioides immitis Skin Test may alter diagnostic results. Management: Consider discontinuing therapeutic immunosuppressants several weeks prior to coccidioides immitis skin antigen testing to increase the likelihood of accurate diagnostic results. Risk D: Consider Therapy Modification

Colchicine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Colchicine. Colchicine distribution into certain tissues (e.g., brain) may also be increased. Management: This combination is often contraindicated, but combined use may be permitted with dose adjustment and monitoring. Recommendations vary based on brand, indication, use of CYP3A4 inhibitors, and hepatic/renal function. See interaction monograph for details. Risk D: Consider Therapy Modification

COVID-19 Vaccines: Calcineurin Inhibitors (Systemic) may decrease therapeutic effects of COVID-19 Vaccines. Management: Rheumatology guidelines recommend holding calcineurin inhibitors for 1 to 2 weeks after each vaccine dose as permitted by the underlying disease. This is specific to the use of calcineurin inhibitors for rheumatologic or musculoskeletal disease. Risk D: Consider Therapy Modification

CycloPHOSphamide: May increase adverse/toxic effects of Voclosporin. Risk X: Avoid

CycloSPORINE (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of CycloSPORINE (Systemic). Risk C: Monitor

CYP3A4 Inducers (Moderate): May decrease serum concentration of Voclosporin. Risk X: Avoid

CYP3A4 Inducers (Strong): May decrease serum concentration of Voclosporin. Risk X: Avoid

CYP3A4 Inhibitors (Moderate): May increase serum concentration of Voclosporin. Management: Decrease the voclosporin dose to 15.8 mg in the morning and 7.9 mg in the evening when combined with moderate CYP3A4 inhibitors. Risk D: Consider Therapy Modification

CYP3A4 Inhibitors (Strong): May increase serum concentration of Voclosporin. Risk X: Avoid

Dabigatran Etexilate: P-glycoprotein/ABCB1 Inhibitors may increase active metabolite exposure of Dabigatran Etexilate. Risk C: Monitor

Dengue Tetravalent Vaccine (Live): Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Dengue Tetravalent Vaccine (Live). Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Dengue Tetravalent Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Denosumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Denosumab. Management: Consider the risk of serious infections versus the potential benefits of coadministration of denosumab and immunosuppressants. If combined, monitor for signs/symptoms of serious infections. Risk D: Consider Therapy Modification

Deucravacitinib: May increase immunosuppressive effects of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid

Digitoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Digitoxin. Risk C: Monitor

Digoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Digoxin. Management: Measure digoxin serum concentrations before initiating treatment with these P-glycoprotein (P-gp) inhibitors. Reduce digoxin concentrations by either reducing the digoxin dose by 15% to 30% or by modifying the dosing frequency. Risk D: Consider Therapy Modification

DOXOrubicin (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of DOXOrubicin (Conventional). Risk X: Avoid

DOXOrubicin (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of DOXOrubicin (Liposomal). Risk C: Monitor

Edoxaban: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Edoxaban. Risk C: Monitor

Ensartinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ensartinib. Risk X: Avoid

Etoposide Phosphate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Etoposide Phosphate. Risk C: Monitor

Etoposide: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Etoposide. Risk C: Monitor

Etrasimod: May increase immunosuppressive effects of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid

Everolimus: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Everolimus. Risk C: Monitor

Filgotinib: May increase immunosuppressive effects of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid

Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification

Glecaprevir and Pibrentasvir: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Glecaprevir and Pibrentasvir. Risk C: Monitor

Grapefruit Juice: May increase serum concentration of Voclosporin. Risk X: Avoid

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may increase QTc-prolonging effects of Haloperidol. Risk C: Monitor

Inebilizumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Inebilizumab. Risk C: Monitor

Influenza Virus Vaccines: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Influenza Virus Vaccines. Management: Administer influenza vaccines at least 2 weeks prior to initiating immunosuppressants if possible. If vaccination occurs less than 2 weeks prior to or during therapy, revaccinate 2 to 3 months after therapy discontinued if immune competence restored. Risk D: Consider Therapy Modification

Itraconazole: May increase serum concentration of Voclosporin. Risk X: Avoid

Lapatinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Lapatinib. Risk C: Monitor

Larotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Larotrectinib. Risk C: Monitor

Lefamulin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin tablets with P-glycoprotein/ABCB1 inhibitors. If concomitant use is required, monitor for lefamulin adverse effects. Risk D: Consider Therapy Modification

Leflunomide: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Leflunomide. Management: Increase the frequency of chronic monitoring of platelet, white blood cell count, and hemoglobin or hematocrit to monthly, instead of every 6 to 8 weeks, if leflunomide is coadministered with immunosuppressive agents. Risk D: Consider Therapy Modification

Mavorixafor: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Mavorixafor. Risk C: Monitor

Morphine (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Morphine (Systemic). Risk C: Monitor

Mumps- Rubella- or Varicella-Containing Live Vaccines: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Mumps- Rubella- or Varicella-Containing Live Vaccines. Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Mumps- Rubella- or Varicella-Containing Live Vaccines. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Nadofaragene Firadenovec: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Nadofaragene Firadenovec. Specifically, the risk of disseminated adenovirus infection may be increased. Risk X: Avoid

Nadolol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Nadolol. Risk C: Monitor

Naldemedine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Naldemedine. Risk C: Monitor

Naloxegol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Naloxegol. Risk C: Monitor

Natalizumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Natalizumab. Risk X: Avoid

OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors): Voclosporin may increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor

Ocrelizumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Ocrelizumab. Risk C: Monitor

Ofatumumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Ofatumumab. Risk C: Monitor

PAZOPanib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of PAZOPanib. Risk X: Avoid

Pidotimod: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Pidotimod. Risk C: Monitor

Pimecrolimus: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Pimecrolimus. Risk X: Avoid

Pneumococcal Vaccines: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Pneumococcal Vaccines. Risk C: Monitor

Poliovirus Vaccine (Live/Trivalent/Oral): Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Poliovirus Vaccine (Live/Trivalent/Oral). Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Poliovirus Vaccine (Live/Trivalent/Oral). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Polymethylmethacrylate: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase hypersensitivity effects of Polymethylmethacrylate. Management: Use caution when considering use of bovine collagen-containing implants such as the polymethylmethacrylate-based Bellafill brand implant in patients who are receiving immunosuppressants. Consider use of additional skin tests prior to administration. Risk D: Consider Therapy Modification

Pralsetinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Pralsetinib. Management: If this combo cannot be avoided, decrease pralsetinib dose from 400 mg daily to 300 mg daily; from 300 mg daily to 200 mg daily; and from 200 mg daily to 100 mg daily. Risk D: Consider Therapy Modification

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor

Rabies Vaccine: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Rabies Vaccine. Management: Complete rabies vaccination at least 2 weeks before initiation of immunosuppressant therapy if possible. If combined, check for rabies antibody titers, and if vaccination is for post exposure prophylaxis, administer a 5th dose of the vaccine. Risk D: Consider Therapy Modification

Ranolazine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ranolazine. Risk C: Monitor

Relugolix, Estradiol, and Norethindrone: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Relugolix, Estradiol, and Norethindrone. Management: Avoid use of relugolix/estradiol/norethindrone with P-glycoprotein (P-gp) inhibitors. If concomitant use is unavoidable, relugolix/estradiol/norethindrone should be administered at least 6 hours before the P-gp inhibitor. Risk D: Consider Therapy Modification

Relugolix: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Relugolix. Management: Avoid coadministration of relugolix with oral P-gp inhibitors whenever possible. If combined, take relugolix at least 6 hours prior to the P-gp inhibitor and monitor patients more frequently for adverse reactions. Risk D: Consider Therapy Modification

Repotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Repotrectinib. Risk X: Avoid

RifAXIMin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RifAXIMin. Risk C: Monitor

Rimegepant: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Rimegepant. Management: Avoid administration of another dose of rimegepant within 48 hours if given concomitantly with a P-glycoprotein (P-gp) inhibitor. Risk D: Consider Therapy Modification

RisperiDONE: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RisperiDONE. Risk C: Monitor

Ritlecitinib: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Ritlecitinib. Risk X: Avoid

RomiDEPsin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RomiDEPsin. Risk C: Monitor

Ruxolitinib (Topical): Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Ruxolitinib (Topical). Risk X: Avoid

Silodosin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Silodosin. Risk C: Monitor

Sipuleucel-T: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Sipuleucel-T. Management: Consider reducing the dose or discontinuing the use of immunosuppressants prior to initiating sipuleucel-T therapy. Risk D: Consider Therapy Modification

Sirolimus (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Sirolimus (Conventional). Management: Avoid concurrent use of sirolimus with P-glycoprotein (P-gp) inhibitors when possible and alternative agents with lesser interaction potential with sirolimus should be considered. Monitor for increased sirolimus concentrations/toxicity if combined. Risk D: Consider Therapy Modification

Sirolimus (Protein Bound): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Sirolimus (Protein Bound). Risk X: Avoid

Solriamfetol: May increase hypertensive effects of Hypertension-Associated Agents. Risk C: Monitor

Sphingosine 1-Phosphate (S1P) Receptor Modulators: May increase immunosuppressive effects of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk C: Monitor

Tacrolimus (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Tacrolimus (Systemic). Risk C: Monitor

Tacrolimus (Topical): Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Tacrolimus (Topical). Risk X: Avoid

Talazoparib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Talazoparib. Risk C: Monitor

Talimogene Laherparepvec: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Talimogene Laherparepvec. Specifically, the risk of infection from the live, attenuated herpes simplex virus contained in talimogene laherparepvec may be increased. Risk X: Avoid

Teniposide: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Teniposide. Risk C: Monitor

Tenofovir Disoproxil Fumarate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor

Tertomotide: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Tertomotide. Risk X: Avoid

Tofacitinib: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Tofacitinib. Management: Coadministration of tofacitinib with potent immunosuppressants is not recommended. Use with non-biologic disease-modifying antirheumatic drugs (DMARDs) was permitted in psoriatic arthritis clinical trials. Risk X: Avoid

Topotecan: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Topotecan. Risk X: Avoid

Typhoid Vaccine: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Typhoid Vaccine. Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Typhoid Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Ublituximab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Ublituximab. Risk C: Monitor

Ubrogepant: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a P-gp inhibitor. Risk D: Consider Therapy Modification

Upadacitinib: Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase immunosuppressive effects of Upadacitinib. Risk X: Avoid

Vaccines (Live): Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Vaccines (Live). Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Vaccines (Live). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Vaccines (Non-Live/Inactivated/Non-Replicating): Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Vaccines (Non-Live/Inactivated/Non-Replicating). Management: Give non-live/inactivated/non-replicating vaccines at least 2 weeks prior to starting immunosuppressants when possible. Patients vaccinated less than 14 days before or during therapy should be revaccinated at least 2 to 3 months after therapy is complete. Risk D: Consider Therapy Modification

Venetoclax: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Venetoclax. Management: Reduce the venetoclax dose by at least 50% in patients requiring concomitant treatment with P-glycoprotein (P-gp) inhibitors. Resume the previous venetoclax dose 2 to 3 days after discontinuation of a P-gp inhibitor. Risk D: Consider Therapy Modification

VinCRIStine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of VinCRIStine. Risk X: Avoid

Yellow Fever Vaccine: Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Yellow Fever Vaccine. Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Yellow Fever Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid

Zoster Vaccine (Live/Attenuated): Immunosuppressants (Therapeutic Immunosuppressant Agents) may increase adverse/toxic effects of Zoster Vaccine (Live/Attenuated). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may decrease therapeutic effects of Zoster Vaccine (Live/Attenuated). Risk X: Avoid

Food Interactions

Grapefruit or grapefruit juice may increase voclosporin plasma concentrations. Management: Avoid grapefruit and grapefruit juice during therapy.

Reproductive Considerations

If a calcineurin-inhibitor is needed in a patient who may become pregnant, agents other than voclosporin are preferred (ACR [Sammaritano 2020]).

Voclosporin may be used in combination with other immunosuppressants, such as mycophenolate mofetil. If used in combination with mycophenolate or other agents, also refer to the individual monographs for additional information related to use in patients who may become pregnant, or patients with partners who could become pregnant.

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies. Due to the alcohol content of voclosporin, use should be avoided in pregnant patients.

If a calcineurin-inhibitor is needed during pregnancy, agents other than voclosporin are preferred (ACR [Sammaritano 2020]).

Voclosporin may be used in combination with other immunosuppressants, such as mycophenolate mofetil. If used in combination with mycophenolate or other agents, also refer to the individual monographs for additional information related to use in pregnancy.

Breastfeeding Considerations

Voclosporin is present in breast milk.

Limited data related to the presence of voclosporin in breast milk are available from the manufacturer. Lactating patients were given a single dose of voclosporin 23.7 mg. The breast milk to maternal blood ratio was 0.42 to 0.95. The estimated daily infant dose of voclosporin via breast milk was 0.00675 mg/kg/day based on an infant milk intake of 200 mL/kg/day.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. If a calcineurin inhibitor is needed in lactating patients, agents other than voclosporin are preferred (ACR [Sammaritano 2020]).

Voclosporin may be used in combination with other immunosuppressants, such as mycophenolate mofetil. If used in combination with mycophenolate or other agents, also refer to the individual monographs for additional information related to use in patients who are breastfeeding.

Dietary Considerations

Avoid grapefruit and grapefruit juice.

Monitoring Parameters

eGFR at baseline, then every 2 weeks for the first month, then every 4 weeks through the first year, and then quarterly thereafter; urinary protein excretion (as clinically indicated); BP at baseline then every 2 weeks for the first month; serum potassium (periodically during treatment). Monitor for signs and symptoms of infection, malignancy (eg, lymphoma, skin cancer), neurotoxicity, pure red cell aplasia, and QT prolongation (consider obtaining ECG and monitoring electrolytes in patients at high risk).

Mechanism of Action

Suppresses cellular immunity (inhibits lymphocyte proliferation, T-cell cytokine production, and expression of T-cell activation surface antigens) by inhibiting the activation of the calmodulin binding catalytic subunit, thus preventing the dephosphorylation of the transcription factor, nuclear factor of activated T-cell cytoplasmic.

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Following a low- or high-fat meal, Cmax and AUC were decreased by 29% to 53% and 15% to 25%, respectively.

Distribution: Vss/F: 2,154 L.

Protein binding: 97%.

Metabolism: Primarily hepatic via CYP3A4.

Half-life elimination: Terminal: ~30 hours (range: 24.9 to 36.5 hours).

Time to peak: Median (fasting): 1.5 hours (range: 1 to 4 hours).

Excretion: Feces (~93%; 5% as unchanged drug); urine (~2%; <1% as unchanged drug).

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Renal function: Cmax and AUC increased by 1.5-fold and 1.7-fold, respectively, in subjects with CrCl <30 mL/minute compared to those with normal kidney function (CrCl >90 mL/minute).

Hepatic function: Cmax and AUC were increased by ~1.5-fold to 2-fold in subjects with mild and moderate hepatic impairment (Child-Pugh class A and B).

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AT) Austria: Lupkynis;
  • (CH) Switzerland: Lupkynis;
  • (DE) Germany: Lupkynis;
  • (ES) Spain: Lupkynis;
  • (FI) Finland: Lupkynis;
  • (GB) United Kingdom: Lupkynis;
  • (HU) Hungary: Lupkynis;
  • (IT) Italy: Lupkynis;
  • (LU) Luxembourg: Lupkynis;
  • (LV) Latvia: Lupkynis;
  • (NL) Netherlands: Lupkynis;
  • (NO) Norway: Lupkynis;
  • (PL) Poland: Lupkynis;
  • (PR) Puerto Rico: Lupkynis;
  • (SE) Sweden: Lupkynis
  1. Lupkynis (voclosporin) [prescribing information]. Rockville, MD: Aurinia Pharma US Inc; May 2024.
  2. Rovin BH, Solomons N, Pendergraft WF 3rd, et al; AURA-LV Study Group. A randomized, controlled double-blind study comparing the efficacy and safety of dose-ranging voclosporin with placebo in achieving remission in patients with active lupus nephritis. Kidney Int. 2019;95(1):219-231. doi:10.1016/j.kint.2018.08.025 [PubMed 30420324]
  3. Sammaritano LR, Bermas BL, Chakravarty EE, et al. 2020 American College of Rheumatology guideline for the management of reproductive health in rheumatic and musculoskeletal diseases. Arthritis Rheumatol. 2020;72(4):529-556. doi:10.1002/art.41191 [PubMed 32090480]
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