Voclosporin

LUPKYNIS

What it isCalcineurin inhibitor; lupus nephritis with mycophenolate and steroids.

Why this oneIt achieves renal response faster than standard therapy, and unlike cyclosporine it needs no level monitoring.

What limits itNephrotoxicity and hypertension as for the class. CYP3A4-dependent; QT prolongation.

FDA-approved for

BOXED WARNING Increased risk of malignancies and serious infections with immunosuppressants (may lead to hospitalization or death)

FDA dosing	Population	Start	Target	Max
Lupus nephritis (with MMF + corticosteroids)	adult	23.7 mg BID	23.7 mg BID	23.7 mg BID

Renal Not recommended if baseline eGFR ≤45 unless benefit exceeds risk; reduced dose in severe renal impairment; modify dose per eGFR changes

Hepatic Mild-moderate: dose reduction required; severe: avoid

If dose missed by >4 h, skip it; maintain at least 8 h between doses

Concomitant strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) — nephrotoxicity risk

Pregnancy Avoid (alcohol content; used with MMF, which can cause fetal harm)

Lactation Small amounts in human milk; data insufficient

⚠ BOXED WARNING

Cost, est. cash$1,000–$15,000+/month

Generic entry2037 est.

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades2 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.

CYP3A4 substrate