Voclosporin

Voclosporin

IUPAC Name:	Hidden
Other Names:	VCS, ISA247, Luveniq
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What is Voclosporin?

• Voclosporin (LUPKYNIS) is a calcineurin-inhibitor immunosuppressant.

What are the uses of this medicine?

• This medicine is indicated in combination with a background immunosuppressive therapy regimen for the treatment of adult patients with active lupus nephritis (LN).

How does this medicine work?

• LUPKYNIS is a calcineurin-inhibitor immunosuppressant.
• The mechanism of voclosporin suppression of calcineurin has not been fully established.
• Activation of lymphocytes involves an increase in intracellular calcium concentrations that bind to the calcineurin regulatory site and activate calmodulin binding catalytic subunit and through dephosphorylation activates the transcription factor, Nuclear Factor of Activated T-Cell Cytoplasmic (NFATc).
• The immunosuppressant activity results in inhibition of lymphocyte proliferation, T-cell cytokine production, and expression of T-cell activation surface antigens.

Who Should Not Use this medicine ?

This medicine cannot be used in :

• Patients concomitantly using strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin)
• Patients who have had a known serious or severe hypersensitivity reaction to LUPKYNIS or any of its excipients.

Limitations of Use: Safety and efficacy of LUPKYNIS have not been established in combination with cyclophosphamide. Use of LUPKYNIS is not recommended in this situation.

What drug interactions can this medicine cause?

• Co-administration of LUPKYNIS with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) is contraindicated .
• Reduce LUPKYNIS dosage when co-administered with moderate CYP3A4 inhibitors (e.g., verapamil, fluconazole, diltiazem) .
• Avoid food or drink containing grapefruit when taking LUPKYNIS.
• Avoid co-administration of LUPKYNIS with strong or moderate CYP3A4 inducers.

Is this medicine FDA approved?

• It was approved for use in the United States in 2021.

How should this medicine be used?

• Establish an accurate baseline estimated glomerular filtration rate (eGFR). Use of LUPKYNIS is not recommended in patients with a baseline eGFR ≤45 mL/min/1.73 m2.
• Check blood pressure (BP) at baseline. Do not initiate LUPKYNIS in patients with BP >165/105 mmHg

Recommended Dosage

• The recommended starting dose of LUPKYNIS is 23.7 mg twice a day.
• Use LUPKYNIS in combination with mycophenolate mofetil (MMF) and corticosteroids.
• If the patient does not experience therapeutic benefit by 24 weeks, consider discontinuation of LUPKYNIS.

Dosage Recommendations in Patients with Renal and Hepatic Impairment

• In patients with mild and moderate hepatic impairment (Child-Pugh A and Child-Pugh B), the recommended dose is 15.8 mg twice daily.
• If used in patients with severe renal impairment at baseline, the recommended starting dose is 15.8 mg twice a day.

Administration LUPKYNIS capsules must be swallowed whole and must not be opened, crushed, or divided. • LUPKYNIS should be taken on an empty stomach consistently as close to a 12-hour schedule as possible, and with a minimum of 8 hours between doses. • If a dose is missed, instruct the patient to take it as soon as possible within 4 hours after missing the dose. Beyond the 4-hour time frame, instruct the patient to wait until the usual scheduled time to take the next regular dose. Instruct the patient not to double the next dose. • Instruct patients to avoid eating grapefruit or drinking grapefruit juice while taking LUPKYNIS

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form: As Capsules: 7.9 mg (voclosporin)

This medicine is available in fallowing brand namesː

• *LUPKYNIS

What side effects can this medication cause?

The most common side effects of this medicine include:

• glomerular filtration rate decreased
• hypertension
• diarrhea
• headache
• anemia
• cough
• urinary tract infection
• abdominal pain upper
• dyspepsia
• alopecia
• renal impairment
• abdominal pain
• mouth
• ulceration
• fatigue
• tremor
• acute kidney injury
• decreased appetite

What special precautions should I follow?

• Nephrotoxicity (acute and/or chronic) may occur due to LUPKYNIS or concomitant nephrotoxic drugs. Monitor renal function; consider dosage reduction.
• This medicine may cause hypertension.
• This medicine may cause neurotoxicity. Monitor for neurologic abnormalities; reduce dosage or discontinue LUPKYNIS.
• This medicine may cause hyperkalemia. Monitor serum potassium levels.
• This medicine may cause QT Prolongation.
• Avoid live vaccines during usage of this medicine.
• This medicine may cause pure red cell aplasia.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• tremor
• headache
• nausea and vomiting
• infections
• tachycardia
• urticaria
• lethargy
• increases in blood urea nitrogen
• serum creatinine, and alanine aminotransferase levels

Management for overdosage:

• No specific antidote to LUPKYNIS therapy is available.
• If overdose occurs, general supportive measures and symptomatic treatment should be conducted, including stopping treatment with LUPKYNIS and assessing blood urea nitrogen, serum creatinine, eGFR and alanine aminotransferase levels.
• Consider contacting a poison center (1-800-221-2222) or medical toxicologist for advice and review of overdosage management recommendations.

Can this medicine be used in pregnancy?

• The available data on the use of LUPKYNIS in pregnant patients are insufficient to determine whether there is a drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes.

Can this medicine be used in children?

• The safety and efficacy of LUPKYNIS in pediatric patients has not been established.

What should I know about storage and disposal of this medication?

• Store at controlled room temperature 20ºC to 25ºC (68ºF to 77ºF); excursions permitted to 15ºC to 30ºC (59ºF to 86ºF).
• Do not put LUPKYNIS in another container. Keep capsules in their original packaging until ready to be taken.

What is the history of this medicine?

• Voclosporin is an experimental immunosuppressant drug being developed by Isotechnika and Lux Biosciences. It is being studied for use in solid organ transplantation and autoimmune diseases such as psoriasis. It is an analog of ciclosporin that has enhanced action against calcineurin and greater metabolic stability.
• Voclosporin was discovered by Dr. Robert T. Foster and his team at Isotechnika in the mid 1990's (US patent 6,605,593). Isotechnika was founded in 1993. Initially, voclosporin was a mixture of equal proporations of cis and trans geometric isomers of amino acid-1 modified cyclosporine A. Later, in collaboration with Roche, Basle, Switzerland, voclosporin's manufacturing was changed to yield the predominantly trans geometric isomer. The trans isomer possesses most of the beneficial effect of the drug (immunosuppression) in the treatment of organ transplantation and autoimmune disease(s).

• Dailymed label info on Voclosporin
• FDA Voclosporin

Voclosporin Resources
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