LUPKYNIS

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.

AbsorptionThe median T max of voclosporin is 1.5 hours (1 to 4 hours) when administered on an empty stomach. Effect of Food Co-administration of voclosporin with food decreased both the rate and extent of absorption: with either low- or high-fat ...

The safety and efficacy of LUPKYNIS were investigated in

Study 1(NCT03021499), a 52-week, randomized, double-blind, placebo-controlled trial in patients with a diagnosis of systemic lupus erythematosus and with International Society of Nephrology / Renal Pathology Society (ISN/RPS) biopsy-proven active Class III or IV LN (alone or in combination with Class V LN) or Class V LN. Patients with Class III or IV LN (alone or in combination with Class V LN) were required to have a urine protein to creatinine (UPCR) ratio of ≥1.5 mg/mg; patients with Class V LN were required to have a UPCR of ≥2 mg/m...

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 Warn...

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...

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 hyper...

7 DRUG INTERACTIONS Moderate CYP3A4 inhibitors: Reduce LUPKYNIS daily dosage to 15.8 mg in the morning and 7.9 mg in the evening. ( 2.5 , 7.1 , 12.3 ) Strong and moderate CYP3A4 inducers: Avoid co-administration. ( 7.1 , 12.3 ) Certain P-gp substrates: Reduce dosage of certain P-gp substrates with a narrow therapeutic window when co-administered with LUPKYNIS. ( 7.2 , 12.3 ) 7.1 Effect of Other Dr...