II. Indications
-
Lupus Nephritis (active)
- Used in combination with other immunosupressants
- FDA approved in 2021
III. Mechanism
- See Calcineurin Inhibitor
- Voclosporin is a Cyclosporine A analog with a single Amino Acid altered
- Modification increases Calcineurin Inhibitor activity
- Like Cyclosporine, Voclosporin acts as a Calcineurin Inhibitor via cyclophilin binding
- Voclosporin also inhibits P-Glycoprotein and OAT 1B1 and 1B3
IV. Medications
- Voclosporin Capsules: 7.9 mg
V. Dosing
- See other references for specific dosing regimens per indication
- Prescribers are typically specialists knowledgeable about the risks and monitoring of Voclosporin
- Decrease dose in renal dysfunction, and adjust doses based on serum levels
- Must be swallowed whole on an empty Stomach for consistent absorption
- Dose as close to every 12 hours as possible (doses should be at least >8 hours apart)
VI. Adverse Effects
- Nephrotoxicity
- Hepatotoxicity
- Cardiovascular adverse effects
- Neurologic adverse effects
- Gastrointestinal
- Secondary Malignancy (class effect)
- Squamous cell cancer
- Lymphoproliferative disorders
- Hematologic
- Pure red cell aplasia
- Miscellaneous adverse effects
- Hyperkalemia
- Serious infections (Bacterial, viral, fungal)
- Alopecia
VII. Safety
- Unknown safety in Lactation
- Avoid in pregnancy (unknown safety)
- Other Calcineurin Inhibitor have previously been labeled as Pregnancy Category C
VIII. Pharmacokinetics
- Hepatic Metabolism (CYP3A4)
- Excreted in the feces
IX. Drug Interactions
- See Calcineurin Inhibitor
-
Nephrotoxic Drugs (e.g. Aminoglycosides, Amphotericin B)
- Avoid in combination with Voclosporin (combination increases nephrotoxicity)
- Numerous Drug Interactions (see other references)
- Tacrolimus is CYP3A4 metabolized
- Many medications alter Tacrolimus absorption and serum levels
- Live Virus Vaccines
- Avoid with Voclosporin
X. Resources
- Voclosporin (StatPearls)
- Voclosporin (DailyMed)