Voclosporin

Voclosporin is a prescription medication used for the treatment of active lupus nephritis.

• Voclosporin is available under the following different brand names: Lupkynis

Common side effects of Voclosporin include:

• Decreased glomerular filtration rate,
• High blood pressure (hypertension),
• Diarrhea,
• Headache,
• Anemia,
• Cough,
• Urinary tract infection (UTI),
• Abdominal pain,
• Indigestion/heartburn,
• Hair loss,
• Renal impairment,
• Mouth ulceration,
• Fatigue,
• Tremor,
• Acute kidney injury, and
• Decreased appetite

Serious side effects of Voclosporin include:

• Confusion
• Numbness and tingling
• Seizures
• Changes in alertness
• Headache
• Vision changes
• Muscle tremors

Rare side effects of Voclosporin include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Capsule

• 7.9 mg

Lupus Nephritis

Adult dosage

• 23.7 mg orally two times a day initially; modify dose based on eGFR

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Voclosporin has severe interactions with at least 29 other drugs.
• Voclosporin has serious interactions with at least 72 other drugs.
• Voclosporin has moderate interactions with at least 353 other drugs.
• Voclosporin has minor interactions with at least 30 other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Coadministration of strong CYP3A4 inhibitors (. g, ketoconazole, itraconazole, clarithromycin)
• Serious or severe hypersensitivity reactions to voclosporin or any of its excipients

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Voclosporin?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Voclosporin?”

Cautions

• Hypertension is a common adverse reaction and may require antihypertensive therapy; monitor relevant drug interactions
• May cause a spectrum of neurotoxicity, which may include posterior reversible encephalopathy syndrome, delirium, seizure, coma, tremors, paresthesia, headache, mental status changes, and changes in motor and sensory functions; monitor for neurologic abnormalities; reduce dosage or discontinue therapy
• Hyperkalemia reported with calcineurin inhibitors; the risk may be increased if coadministered with other agents associated with hyperkalemia (. g, potassium-sparing diuretics, ACE inhibitors, angiotensin receptor blockers); monitor serum potassium levels
• Cases of pure red cell aplasia (PRCA) were reported in patients treated with another calcineurin-inhibitor immunosuppressant; reported risk factors were parvovirus B19 infection, underlying disease, or concomitant medications associated with PRCA; if diagnosed, consider discontinuation
• Lymphoma and other malignancies
  • Immunosuppressants, including voclosporin, increase the risk of developing lymphomas and other malignancies, particularly of the skin
  • Risk may be related to the intensity and duration of immunosuppression
  • Examine for skin changes
  • Avoid or limit sun exposure and avoid artificial UV light (tanning beds, sun lamps) by wearing protective clothing and using a broad-spectrum sunscreen with a high protection factor (SPF above30)
• Serious infections
  • Immunosuppressants, including voclosporin, increase the risk of developing bacterial, viral, fungal, and protozoal infections, including opportunistic infections
  • Infections may lead to serious, including fatal, outcomes
  • Viral infections reported include cytomegalovirus and herpes zoster infections
  • Monitor for any developing infection
  • Consider benefits and risks; use the lowest effective dose needed to maintain response
• Nephrotoxicity
  • Nephrotoxicity reported; may cause acute and/or chronic nephrotoxicity
  • Monitor renal function; consider dosage reduction or discontinuation at baseline
  • Safety and efficacy not established above1 year; consider risks and benefits of longer durations of treatment considering treatment response and risk of nephrotoxicity
  • Concomitant nephrotoxic drugs may increase the risk of nephrotoxicity
• Drug interaction overview
• Sensitive CYP3A4 substrate; P-gp inhibitor; OATP1B1 inhibitor
• CYP3A4 inhibitors
  • Coadministration with strong or moderate CYP3A4 inhibitors increases voclosporin effects and the risk of adverse reactions
  • Use contraindicated for strong CYP3A4 inhibitors; reduce voclosporin dose for moderate CYP3A4 inhibitors; avoid food or drink containing grapefruit during treatment
• CYP3A4 inducers
  • Coadministration with strong or moderate CYP3A4 inducers decreases voclosporin effects and efficacy
  • Avoid coadministration of strong and moderate CYP3A4 inducers
• P-GP substrates
  • Coadministration of voclosporin increases effects and risk of adverse reactions of P-gp substrates; reduce the dose of P-gp substrates with a narrow therapeutic window, if needed
• OATP1B substrates
  • Effects on OATP1B1 substrates (.g, statins) have not been studied clinically; information suggests voclosporin may increase the concentration of OATP1B1 substrates; monitor for adverse reactions of OATP1B1 substrates when concomitantly used
• Vaccines
  • Live attenuated vaccines during treatment: Avoid the use
  • Inactivated vaccines: Noted safe for administration; however, may not be sufficiently immunogenic during treatment
• QT prolongation
  • Prolongs QTc interval in a dose-dependent manner after single-dose administration at a dose higher than the recommended therapeutic dose
  • Use in combination with other drugs that are known to prolong QTc may result in clinically significant QT prolongation
  • Consider obtaining electrocardiograms and monitoring electrolytes in patients at high risk

Pregnancy and Lactation

• Avoid use in pregnant females; formulation contains alcohol (21.6 mg of dehydrated ethanol per capsule for a dose of 129.4 mg/day); studies have demonstrated that alcohol is associated with fetal harm (. g, central nervous system abnormalities, behavioral disorders, impaired intellectual development)
• Insufficient data available on use in pregnant females to determine drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes
• May be used in combination with an immunosuppressive therapy regimen that includes MMF; information for MMF regarding pregnancy, pregnancy testing, contraception, and infertility also applies to this combination regimen; refer to MMF prescribing information for more information
• There are risks (. g, worsening of the underlying disease, premature birth, miscarriage, intrauterine growth restriction) to the mother and fetus associated with systemic lupus erythematosus
• Lactation
  • No available data other presence in human milk, effects on breastfed infants, or effects on milk production
  • Present in the milk of lactating rats; therefore, the drug is likely to be present in human milk
  • Breastfeeding is not recommended during treatment and for at least 7 days after the last dose (approximately 6 elimination half-lives)