Version May 2024
Increased risk for developing malignancies and serious infections with voclosporin or other immunosuppressants that may lead to hospitalization or death.
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: 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.
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).
Mild to moderate impairment (Child-Pugh class A or B): 15.8 mg twice daily.
Severe impairment (Child-Pugh class C): Use not recommended.
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.
Refer to adult dosing; use caution.
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
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.
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).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Lupkynis: 7.9 mg
No
Capsules (Lupkynis Oral)
7.9 mg (per each): $97.96
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.
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.
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
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.
Voclosporin may be confused with cyclosporine.
This medication is in a class the Institute for Safe Medication Practices (ISMP) includes among its list of drug classes that have a heightened risk of causing significant patient harm when used in error.
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits P-glycoprotein/ABCB1
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 Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Abrocitinib: May enhance the immunosuppressive effect of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid combination
Afatinib: P-glycoprotein/ABCB1 Inhibitors may increase the 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 the serum concentration of Aliskiren. Risk C: Monitor therapy
Androgens: Hypertension-Associated Agents may enhance the hypertensive effect of Androgens. Risk C: Monitor therapy
Antithymocyte Globulin (Equine): Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of Antithymocyte Globulin (Equine). Specifically, these effects may be unmasked if the dose of immunosuppressive therapy is reduced. Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Antithymocyte Globulin (Equine). Specifically, infections may occur with greater severity and/or atypical presentations. Risk C: Monitor therapy
Baricitinib: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Baricitinib. Risk X: Avoid combination
BCG Products: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of BCG Products. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of BCG Products. Risk X: Avoid combination
Berotralstat: Voclosporin may increase the serum concentration of Berotralstat. Berotralstat may increase the 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 berotralstat. Additionally, decrease the berotralstat dose to 110 mg daily when combined with voclosporin. Risk D: Consider therapy modification
Bilastine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Bilastine. Risk X: Avoid combination
Brincidofovir: Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Brincidofovir. Risk C: Monitor therapy
Brivudine: May enhance the adverse/toxic effect of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid combination
Celiprolol: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Celiprolol. Risk C: Monitor therapy
Chikungunya Vaccine (Live): Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of Chikungunya Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Chikungunya Vaccine (Live). Risk X: Avoid combination
Cladribine: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Cladribine. Risk X: Avoid combination
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Coccidioides immitis Skin Test: Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the diagnostic effect of Coccidioides immitis Skin Test. 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 the 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 diminish the therapeutic effect 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 enhance the adverse/toxic effect of Voclosporin. Risk X: Avoid combination
CycloSPORINE (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of CycloSPORINE (Systemic). Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Voclosporin. Risk X: Avoid combination
CYP3A4 Inducers (Strong): May decrease the serum concentration of Voclosporin. Risk X: Avoid combination
CYP3A4 Inhibitors (Moderate): May increase the 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 the serum concentration of Voclosporin. Risk X: Avoid combination
Dabigatran Etexilate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentrations of the active metabolite(s) of Dabigatran Etexilate. Risk C: Monitor therapy
Dengue Tetravalent Vaccine (Live): Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of Dengue Tetravalent Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Dengue Tetravalent Vaccine (Live). Risk X: Avoid combination
Denosumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect 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 enhance the immunosuppressive effect of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid combination
Digoxin: P-glycoprotein/ABCB1 Inhibitors may increase the 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 the serum concentration of DOXOrubicin (Conventional). Risk X: Avoid combination
DOXOrubicin (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of DOXOrubicin (Liposomal). Risk C: Monitor therapy
Edoxaban: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Edoxaban. Risk C: Monitor therapy
Etoposide: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Etoposide. Risk C: Monitor therapy
Etoposide Phosphate: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Etoposide Phosphate. Risk C: Monitor therapy
Etrasimod: May enhance the immunosuppressive effect of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid combination
Everolimus: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Everolimus. Risk C: Monitor therapy
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Filgotinib: May enhance the immunosuppressive effect of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk X: Avoid combination
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Glecaprevir and Pibrentasvir: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Glecaprevir and Pibrentasvir. Risk C: Monitor therapy
Grapefruit Juice: May increase the serum concentration of Voclosporin. Risk X: Avoid combination
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy
Inebilizumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Inebilizumab. Risk C: Monitor therapy
Influenza Virus Vaccines: Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect 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
Lapatinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Lapatinib. Risk C: Monitor therapy
Larotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Larotrectinib. Risk C: Monitor therapy
Lefamulin: P-glycoprotein/ABCB1 Inhibitors may increase the 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 enhance the immunosuppressive effect 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
Morphine (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Morphine (Systemic). Risk C: Monitor therapy
Mumps- Rubella- or Varicella-Containing Live Vaccines: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of Mumps- Rubella- or Varicella-Containing Live Vaccines. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Mumps- Rubella- or Varicella-Containing Live Vaccines. Risk X: Avoid combination
Nadofaragene Firadenovec: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of Nadofaragene Firadenovec. Specifically, the risk of disseminated adenovirus infection may be increased. Risk X: Avoid combination
Nadolol: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Nadolol. Risk C: Monitor therapy
Naldemedine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Naldemedine. Risk C: Monitor therapy
Naloxegol: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Naloxegol. Risk C: Monitor therapy
Natalizumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Natalizumab. Risk X: Avoid combination
OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors): Voclosporin may increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Ocrelizumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Ocrelizumab. Risk C: Monitor therapy
Ofatumumab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Ofatumumab. Risk C: Monitor therapy
PAZOPanib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of PAZOPanib. Risk X: Avoid combination
Pidotimod: Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Pidotimod. Risk C: Monitor therapy
Pimecrolimus: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Pimecrolimus. Risk X: Avoid combination
Pneumococcal Vaccines: Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Pneumococcal Vaccines. Risk C: Monitor therapy
Poliovirus Vaccine (Live/Trivalent/Oral): Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of Poliovirus Vaccine (Live/Trivalent/Oral). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Poliovirus Vaccine (Live/Trivalent/Oral). Risk X: Avoid combination
Polymethylmethacrylate: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the potential for allergic or hypersensitivity reactions to 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 the 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 enhance the QTc-prolonging effect 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 therapy
Rabies Vaccine: Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect 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 the serum concentration of Ranolazine. Risk C: Monitor therapy
Relugolix: P-glycoprotein/ABCB1 Inhibitors may increase the 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
Relugolix, Estradiol, and Norethindrone: P-glycoprotein/ABCB1 Inhibitors may increase the 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
Repotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Repotrectinib. Risk X: Avoid combination
RifAXIMin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RifAXIMin. Risk C: Monitor therapy
Rimegepant: P-glycoprotein/ABCB1 Inhibitors may increase the 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 the serum concentration of RisperiDONE. Risk C: Monitor therapy
Ritlecitinib: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Ritlecitinib. Risk X: Avoid combination
RomiDEPsin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RomiDEPsin. Risk C: Monitor therapy
Ruxolitinib (Topical): Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Ruxolitinib (Topical). Risk X: Avoid combination
Silodosin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Silodosin. Risk C: Monitor therapy
Sipuleucel-T: Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect 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 the 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 the serum concentration of Sirolimus (Protein Bound). Risk X: Avoid combination
Solriamfetol: May enhance the hypertensive effect of Hypertension-Associated Agents. Risk C: Monitor therapy
Sphingosine 1-Phosphate (S1P) Receptor Modulator: May enhance the immunosuppressive effect of Immunosuppressants (Therapeutic Immunosuppressant Agents). Risk C: Monitor therapy
Tacrolimus (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Tacrolimus (Topical): Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Tacrolimus (Topical). Risk X: Avoid combination
Talazoparib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Talazoparib. Risk C: Monitor therapy
Talimogene Laherparepvec: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect 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 combination
Tegaserod (Withdrawn from US Market): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Tegaserod (Withdrawn from US Market). Risk C: Monitor therapy
Teniposide: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Teniposide. Risk C: Monitor therapy
Tenofovir Disoproxil Fumarate: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor therapy
Tertomotide: Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Tertomotide. Risk X: Avoid combination
Tofacitinib: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect 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 combination
Topotecan: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
Typhoid Vaccine: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of Typhoid Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Typhoid Vaccine. Risk X: Avoid combination
Ublituximab: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the immunosuppressive effect of Ublituximab. Risk C: Monitor therapy
Ubrogepant: P-glycoprotein/ABCB1 Inhibitors may increase the 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 enhance the immunosuppressive effect of Upadacitinib. Risk X: Avoid combination
Vaccines (Inactivated/Non-Replicating): Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Vaccines (Inactivated/Non-Replicating). Management: Give inactivated vaccines at least 2 weeks prior to initiation of immunosuppressants when possible. Patients vaccinated less than 14 days before initiating or during therapy should be revaccinated at least 2 to 3 months after therapy is complete. Risk D: Consider therapy modification
Vaccines (Live): Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of Vaccines (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Vaccines (Live). Risk X: Avoid combination
Venetoclax: P-glycoprotein/ABCB1 Inhibitors may increase the 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 (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of VinCRIStine (Liposomal). Risk X: Avoid combination
Yellow Fever Vaccine: Immunosuppressants (Therapeutic Immunosuppressant Agents) may enhance the adverse/toxic effect of Yellow Fever Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Therapeutic Immunosuppressant Agents) may diminish the therapeutic effect of Yellow Fever Vaccine. Risk X: Avoid combination
Grapefruit or grapefruit juice may increase voclosporin plasma concentrations. Management: Avoid grapefruit and grapefruit juice during therapy.
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.
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.
It is not known if voclosporin is present in breast milk.
Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during therapy and for 7 days after the last voclosporin dose. 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.
Avoid grapefruit and grapefruit juice.
eGFR at baseline, then every 2 weeks for the first month then, every 4 weeks 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).
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.
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).
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).
آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟
