Pharm

Voclosporin

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Voclosporin, Lupkynis

  • See Also
  1. Calcineurin Inhibitor
  • Indications
  1. Lupus Nephritis (active)
    1. Used in combination with other immunosupressants
    2. FDA approved in 2021
  • Mechanism
  1. See Calcineurin Inhibitor
  2. Voclosporin is a Cyclosporine A analog with a single Amino Acid altered
    1. Modification increases Calcineurin Inhibitor activity
    2. Like Cyclosporine, Voclosporin acts as a Calcineurin Inhibitor via cyclophilin binding
    3. Voclosporin also inhibits P-Glycoprotein and OAT 1B1 and 1B3
  • Medications
  1. Voclosporin Capsules: 7.9 mg
  • Dosing
  1. See other references for specific dosing regimens per indication
  2. Prescribers are typically specialists knowledgeable about the risks and monitoring of Voclosporin
  3. Decrease dose in renal dysfunction, and adjust doses based on serum levels
  4. Must be swallowed whole on an empty Stomach for consistent absorption
  5. Dose as close to every 12 hours as possible (doses should be at least >8 hours apart)
  • Adverse Effects
  1. Nephrotoxicity
  2. Hepatotoxicity
  3. Cardiovascular adverse effects
    1. Hypertension
    2. QTc Prolongation
  4. Neurologic adverse effects
    1. Posterior Reversible Encephalopathy Syndrome (PRES)
    2. Headaches
    3. Tremor
  5. Gastrointestinal
    1. Nausea or Vomiting
    2. Diarrhea
    3. Abdominal Pain
    4. Anorexia
  6. Secondary Malignancy (class effect)
    1. Squamous cell cancer
    2. Lymphoproliferative disorders
  7. Hematologic
    1. Pure red cell aplasia
  8. Miscellaneous adverse effects
    1. Hyperkalemia
    2. Serious infections (Bacterial, viral, fungal)
    3. Alopecia
  • Safety
  1. Unknown safety in Lactation
  2. Avoid in pregnancy (unknown safety)
    1. Other Calcineurin Inhibitor have previously been labeled as Pregnancy Category C
  • Pharmacokinetics
  1. Hepatic Metabolism (CYP3A4)
  2. Excreted in the feces
  • Drug Interactions
  1. See Calcineurin Inhibitor
  2. Nephrotoxic Drugs (e.g. Aminoglycosides, Amphotericin B)
    1. Avoid in combination with Voclosporin (combination increases nephrotoxicity)
  3. Numerous Drug Interactions (see other references)
    1. Tacrolimus is CYP3A4 metabolized
    2. Many medications alter Tacrolimus absorption and serum levels
  4. Live Virus Vaccines
    1. Avoid with Voclosporin
  • Resources
  1. Voclosporin (StatPearls)
    1. https://www.ncbi.nlm.nih.gov/books/NBK592419/
  2. Voclosporin (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9f489295-1156-52c7-5fd0-5c4c52f9b813