Voclosporin
Lupus Nephritis
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Drug Status
Government Approvals
US(FDA)
WHO Essential Medicine
NO
Known Teratogen
NO
Pharmaceutical Class
Calcineurin Inhibitor Immunosuppressant
Controlled Drug Substance
No
Voclosporin
Summary
Voclosporin is used to treat lupus nephritis, a condition where the immune system attacks the kidneys, causing inflammation and damage.
Voclosporin is an immunosuppressant. It works by decreasing the activity of the immune system, specifically by inhibiting a protein called calcineurin. This helps reduce inflammation and prevent further damage to the kidneys.
The usual dose for adults is 23.7 mg, taken twice a day. It is taken orally and should be taken on an empty stomach, either 1 hour before or 2 hours after a meal.
Common side effects include diarrhea, headache, hypertension (high blood pressure), and urinary tract infections. More serious side effects can include kidney toxicity, neurotoxicity, high potassium levels, and changes in heart rhythm.
Voclosporin should not be used by patients taking certain medications, including strong CYP3A4 inhibitors. It should also be avoided during pregnancy and by those with known hypersensitivity to the drug. It can increase the risk of serious infections and certain types of cancer.
Indications and Purpose
How does Voclosporin work?
Voclosporin is a calcineurin-inhibitor immunosuppressant that works by inhibiting the activity of calcineurin, a protein involved in activating T-cells of the immune system. By suppressing calcineurin, Voclosporin reduces the proliferation of lymphocytes, production of T-cell cytokines, and expression of T-cell activation surface antigens. This decreases the immune system's activity, helping to prevent it from attacking the kidneys in lupus nephritis.
Is Voclosporin effective?
Voclosporin has been shown to be effective in treating lupus nephritis in adults. In clinical trials, a higher proportion of patients taking Voclosporin achieved complete renal response compared to those taking a placebo. The primary efficacy endpoint was the proportion of patients achieving complete renal response at Week 52, with 40.8% of patients in the Voclosporin group achieving this compared to 22.5% in the placebo group. This demonstrates the effectiveness of Voclosporin in managing lupus nephritis.
What is Voclosporin?
Voclosporin is an immunosuppressant used in combination with other medications to treat lupus nephritis, an autoimmune disease affecting the kidneys. It works by decreasing the activity of the immune system to prevent it from attacking the kidneys. This helps reduce inflammation and damage, improving kidney function. Regular monitoring is essential to ensure its effectiveness and manage potential side effects.
Directions for Use
For how long do I take Voclosporin?
Voclosporin is typically taken twice a day for up to 1 year. It is not known if taking it for longer than one year is safe, so it's important to discuss the benefits and risks of continuing treatment with your doctor after 1 year.
How do I take Voclosporin?
Voclosporin should be taken on an empty stomach, either 1 hour before or 2 hours after a meal, and as close to a 12-hour schedule as possible, with at least 8 hours between doses. It is important to avoid grapefruit and grapefruit juice while taking this medication, as they can affect how the medicine works. Always follow your doctor's instructions and consult them if you have any questions about your treatment.
How should I store Voclosporin?
Voclosporin should be stored at room temperature, between 68°F to 77°F (20°C to 25°C). It should be kept in its original packaging until ready to be taken and should not be transferred to another container. The medication should be kept out of reach of children and away from excess heat and moisture, such as in a bathroom. Proper storage ensures the medication remains effective and safe to use.
What is the usual dose of Voclosporin?
The usual daily dose for adults is 23.7 mg taken twice a day. Voclosporin is not recommended for use in children as its safety and efficacy have not been established in pediatric patients.
Warnings and Precautions
Can I take Voclosporin with other prescription drugs?
Voclosporin is a sensitive CYP3A4 substrate, and its exposure can be significantly increased by strong CYP3A4 inhibitors like ketoconazole, itraconazole, and clarithromycin, which are contraindicated. Moderate CYP3A4 inhibitors like verapamil and fluconazole require dosage adjustments. Strong CYP3A4 inducers like rifampin can decrease its efficacy. Voclosporin also increases exposure of P-gp substrates, so dosage adjustments of these substrates may be necessary. Always consult a healthcare provider before starting or stopping any medication.
Can Voclosporin be taken safely while breastfeeding?
Voclosporin can pass into breast milk, and while the amount is small, the effects on the breastfed infant or milk production are not well understood. The decision to use Voclosporin while breastfeeding should consider the benefits of breastfeeding, the mother's need for the medication, and any potential risks to the infant. It is important to discuss with a healthcare provider to make an informed decision about breastfeeding while on Voclosporin.
Can Voclosporin be taken safely while pregnant?
Voclosporin should be avoided during pregnancy due to its alcohol content and potential risks. There is insufficient data on its use in pregnant patients to determine the risk of birth defects or miscarriage. However, animal studies have shown embryocidal and fetocidal effects at certain doses. If Voclosporin is used with mycophenolate mofetil, which is known to cause fetal harm, additional precautions are necessary. Pregnant women should consult their healthcare provider to discuss potential risks and alternative treatments.
Is it safe to drink alcohol while taking Voclosporin?
Voclosporin capsules contain a small amount of alcohol, and it is not known what effect it can have on an unborn baby if taken during pregnancy. However, there is no specific mention of alcohol consumption affecting the safety or effectiveness of Voclosporin in adults. It is always best to consult with a healthcare provider regarding alcohol consumption while on this medication.
Is Voclosporin safe for the elderly?
There is no specific information on the use of Voclosporin in elderly patients. However, in general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. It is important for elderly patients to be closely monitored by their healthcare provider while taking this medication.
Who should avoid taking Voclosporin?
Voclosporin can increase the risk of serious infections and certain types of cancer, such as skin cancer and lymphoma. It may also cause nephrotoxicity, hypertension, neurotoxicity, hyperkalemia, and QTc prolongation. It is contraindicated in patients using strong CYP3A4 inhibitors and those with known hypersensitivity to the drug. Patients should avoid live vaccines and grapefruit products. Regular monitoring of kidney function, blood pressure, and potassium levels is essential during treatment.
