Voclosporin (Lupkynis)_Dosage, benefits & legal status
Also known as ISA247, ISA-247, ISATX247, LX211, Lupkynis, Luveniq
Cyclosporine with one extra carbon on its first residue, approved in the US in 2021 for lupus that attacks the kidneys. Added to standard treatment, it nearly doubled full kidney responses at one year.
Common vial size is what vendors typically sell, not a recommendation. Enter your own vial in the calculator.
What is Voclosporin (Lupkynis)?
Plain language first. The technical label stays, but it never stands alone.Overview
Lupus nephritis is lupus inflaming the kidneys, and it can lead to kidney failure. Added to mycophenolate and low-dose steroids, voclosporin raised the share of people whose kidneys fully responded at one year from 22.5% to 40.8% in the 357-person AURORA 1 trial. It carries a boxed warning for cancers and serious infections, can lower kidney filtration (26% against 9% on placebo), and needs kidney blood tests every few weeks at first.
Voclosporin is a cyclic undecapeptide calcineurin inhibitor identical to cyclosporine except at residue 1, where the side chain's end methyl becomes a vinyl group (C63H111N11O12 against C62H111N11O12); the EMA says this changes how it binds calcineurin and moves its metabolism away from that residue. Isotechnika of Edmonton discovered it and Aurinia developed it, and the FDA approved it on January 22, 2021, as Lupkynis, taken with a background immunosuppressive regimen for adults with active lupus nephritis. Psoriasis, uveitis, kidney transplant and dry-eye programs all stopped short of approval.
What it's used for
A prescription capsule taken twice daily with mycophenolate and steroids by adults with active lupus nephritis, the kidney inflammation lupus can cause.
How does Voclosporin (Lupkynis) work?
What it does in the body, and where.Voclosporin switches off calcineurin, an enzyme T cells need to turn on, the same target as cyclosporine.
- 01The switchWhen a T cell recognizes a target, calcium rises inside it and turns on calcineurin, an enzyme that strips phosphate tags from other proteins. Voclosporin binds a cell protein called cyclophilin A, and the pair blocks calcineurin.
- 02The signal stopsCalcineurin normally frees the transcription factor NFAT to enter the nucleus. With it blocked, NFAT stays outside, and IL-2 and other genes that drive T-cell activation stay off.
- 03In the kidneyFewer activated T cells means less immune attack on the kidney filters. Animal studies suggest it also steadies the cytoskeleton of podocytes, the cells that keep protein out of the urine. The label says its mechanism has not been fully established.
A schematic of the compound's mechanism, not a diagnostic image.
What else is it used for?
Each group carries its own evidence level.Approved means regulators have cleared it for that purpose. Investigational means it is in trials. Early research means it is being studied and is not established.
Lupus nephritis, first year (AURORA 1)
FDA-approved- Human trial357 randomized: complete renal response at 52 weeks 40.8% against 22.5% (OR 2.65); urine protein-to-creatinine ratio of 0.5 or lower in 45.3% against 23.0%.
- Human trialThe kidney-function part of the response alone did not differ (82.1% against 75.8%).
- Human trialSerious adverse events 21% in each group; 1 death on voclosporin against 5 on placebo, none judged treatment related.
Up to 3 years (AURORA 2)
FDA-approved- Human trial216 people continued blinded for 2 more years (116 on voclosporin, 100 on placebo): complete renal response 50.9% against 39.0% (OR 1.74, 95% CI 1.00 to 3.03).
- Human trialeGFR slope over 2 years -0.2 against -5.4 mL/min/1.73 m2; adverse events 86% against 80%. Safety was the primary objective.
Dose finding (AURA-LV)
FDA-approved- Human trial265 patients: complete remission at 24 weeks 32.6% on 23.7 mg and 27.3% on 39.5 mg twice daily against 19.3% on placebo; only the lower dose was significant (OR 2.03, P=0.045). At 48 weeks the company reported 49% and 40% against 24%.
- No dataDeaths: 10 of 89 on the lower dose, 2 of 88 on the higher dose and 1 of 88 on placebo; serious adverse events 28.1%, 25.0% and 15.9%.
Psoriasis
tested-and-failed- Human trialSPIRIT, 451 patients (ClinicalTrials.gov NCT00244842): PASI-75 at 12 weeks 13.3%, 23.4% and 38.9% on 0.2, 0.3 and 0.4 mg/kg twice daily against 3.5% on placebo. The company reported seven patients (six on the highest dose) with two consecutive GFR drops of more than 30%.
- Human trialESSENCE, 642 patients: 35% clear or almost clear at 12 weeks against 6% on placebo, but 53% on cyclosporine, so noninferiority was not shown. No psoriasis filing has been found.
Eye disease
tested-and-failed- RegulatoryUveitis (Luveniq): Lux Biosciences announced on August 4, 2010, that the FDA regarded one of two pivotal trials as positive and had issued a complete response letter; in the EU the CHMP recommended refusal in June 2011.
- Human trialAUDREY, 508 people with dry eye: a Schirmer tear-test gain of at least 10 mm at week 4 in 10%, 9% and 11% on the 0.05%, 0.1% and 0.2% drops against 5% on vehicle (P=0.09, 0.28 and 0.13). The program was suspended.
It is often described as a synthetic 11-amino-acid peptide derived from cyclosporine. The count is right, but seven of the eleven residues carry a methyl group on the backbone nitrogen and two are not among the standard amino acids; it differs from cyclosporine by one carbon on residue 1, and the EMA says it is made from cyclosporine A in five main chemical steps, so 'derived from cyclosporine' is accurate. The often-quoted '41% against 23%' is AURORA 1 rounded from 40.8% (73 of 179) and 22.5% (40 of 178); the odds ratio is 2.65 in the Lancet and 2.7 in the label. 'Second-generation calcineurin inhibitor' is the company's description, not a regulatory class. Summaries of the AURA-LV phase 2b often leave out its deaths: 10 of 89 on the lower dose against 2 of 88 on the higher dose and 1 of 88 on placebo. In psoriasis it beat placebo but did not show it was as good as cyclosporine in ESSENCE, a trial unrelated to the cyclosporine eye-drop trials of the same name.
The published record
Papers and trials about Voclosporin (Lupkynis)
153 papers tagged human · 62 not reviews or lab · 17 clinical trial publications
28 registered trials · 10 with posted results
Furthest stage reached: Approved in the US
Counted from Europe PMC indexing, not read by a person; a human tag can land on reviews, commentary or lab papers; clinical trial publications is the narrower count.
At a glance
Four things to know about Voclosporin (Lupkynis)
Evidence
FDA-approved
Category
Immune support
Common vial
Varies
Half-life
About 30 hours
How much, and do you cycle it?
The range, and whether you take breaks.23.7 mg (three 7.9 mg capsules) per dose (label), twice daily, about 12 hours apart, on an empty stomach. Continuous, set by the prescription FDA label
Taken every day with mycophenolate and steroids; the label says to consider stopping if there is no benefit by 24 weeks. The trials and their extension ran for up to 3 years.
About 30 hoursFDA label
Peak levels about 1.5 hours after a fasting dose (range 1 to 4). Food cuts peak levels by 29 to 53% and total exposure by 15 to 25%, hence the empty stomach. 97% protein-bound and broken down mainly by CYP3A4; 92.7% of a dose leaves in the feces and 2.1% in the urine. Ketoconazole raised exposure more than 18-fold in a study reviewed by the EMA.
Source: Lupkynis prescribing information, section 12.3
You can compare this against the whole library to see where it sits.
What does it cost?
Typical dose and cost, in plain numbers.Voclosporin (Lupkynis) is not injected
It is taken by mouth (capsule). Three 7.9 mg capsules (23.7 mg) by mouth twice daily, on an empty stomach about 12 hours apart and at least 8 hours between doses, with mycophenolate mofetil and steroids; grapefruit is avoided. A missed dose can be taken within 4 hours; otherwise it is skipped. eGFR is checked every 2 weeks for the first month, every 4 weeks through the first year, then every 3 months. If eGFR is below 60 and has fallen more than 20% but less than 30% from baseline, the dose drops by 7.9 mg twice daily and is reassessed within 2 weeks, with a second 7.9 mg cut if it is still down more than 20%; at a fall of 30% or more it is stopped, and may restart at 7.9 mg twice daily once eGFR is back to at least 80% of baseline, rising in 7.9 mg steps no higher than the starting dose. Severe kidney impairment at the start, or mild to moderate liver impairment (Child-Pugh A or B): 15.8 mg twice daily; avoided in Child-Pugh C. With moderate CYP3A4 inhibitors such as verapamil, fluconazole or diltiazem: 15.8 mg in the morning and 7.9 mg in the evening; strong inhibitors are contraindicated, and strong and moderate CYP3A4 inducers are avoided. Stopping is considered if there is no benefit by 24 weeks. Supplied as 7.9 mg capsules in blister wallets, so the vial calculator does not apply.
How do you store it?
Before mixing, and after.Room temperature. Cool, dry, out of light.
Voclosporin (Lupkynis) is taken as a pill or capsule. Keep it in its original container at room temperature, away from heat, humidity, and direct sun. No fridge or mixing needed. Check the expiration date on the bottle.
What are the side effects and cautions?
Known cautions and warnings for this compound.Solubility, computed: 18% charged residues, 82% hydrophobic. Organic co-solvent likely.
A first-pass rule from peptide manufacturers' guidance. It does not account for disulfide bridges, salt form or how the powder was dried, and it predicts what should be easy rather than what will happen in your vial.
Who should avoid it
- Taking a strong CYP3A4 inhibitor, such as ketoconazole, itraconazole or clarithromycin
- A past serious allergic reaction, including anaphylaxis, to voclosporin or any ingredient
- Use with cyclophosphamide: safety and efficacy not established, and the label advises against it
- Starting with an eGFR of 45 mL/min/1.73 m2 or lower unless the benefit outweighs the risk, or with blood pressure above 165/105 mmHg or a hypertensive emergency
- Severe liver impairment (Child-Pugh C), where the label says to avoid it
- Pregnancy: the label advises avoiding it because each capsule contains 21.6 mg of alcohol
Stop and get help
- Fever, chills or other signs of a serious infection
- Seizures or other new nervous system symptoms: the label warns of neurotoxicity, including PRES
- Swelling of the face, lips or throat, or trouble breathing
Common effects
- GFR decreased in 26% against 9% on placebo (two trials pooled, 267 against 266 people)
- High blood pressure 19% against 9%, diarrhea 19% against 13% and headache 15% against 8%
- Anemia 12% against 6%, cough 11% against 2% and urinary tract infection 10% against 6%
- Serious infections in 27 people in each group (11.9 against 12.0 per 100 patient-years)
Where this page says nothing is established, that means nobody has studied it, not that a compound is safe.
Is Voclosporin (Lupkynis) approved?
And where the numbers on this page come from.Yes. Voclosporin (Lupkynis) is FDA approved and available on prescription in the United States. It is also approved in the European Union and Japan.
- Approval statusFDA-approved
- RouteBy mouth (capsule)
- Checked21 October 2026
- Approved outside the USEuropean Union, Japan: EU authorization on September 15, 2022 (Otsuka Pharmaceutical Netherlands B.V.), with mycophenolate mofetil for adults with active class III, IV or V lupus nephritis, including mixed III/V and IV/V. Aurinia announced Japanese approval with mycophenolate mofetil on September 24, 2024; Otsuka holds the Japanese rights. Also approved in the US.This does not change the United States position above.
- DoseFrom the drug label. The manufacturer tested this range and a regulator reviewed it.
- Vial sizeFrom what vendors typically list; not a recommendation.
- SourcesLupkynis prescribing information, DailyMed (revised 8/2026)Drugs@FDA, NDA 213716FDA approval letter, NDA 213716FDA GSRS substance record, voclosporin (UNII 2PN063X6B1)EMA, Lupkynis EPAREMA, Luveniq withdrawal assessment reportRovin BH et al., Lancet 2021;397:2070-2080 (AURORA 1)Saxena A et al., Arthritis and Rheumatology 2024;76:59-67 (AURORA 2)ClinicalTrials.gov, AURA-LV results (NCT02141672); Rovin BH et al., Kidney International 2019;95:219-231Aurinia, AURA-LV 48-week results (April 20, 2017)Busque S et al., American Journal of Transplantation 2011;11:2675-2684 (PROMISE)Isotechnika, ESSENCE psoriasis results (April 28, 2009)Aurinia, AUDREY dry-eye results (November 2, 2020)Nasdaq/RTT, Lupkynis approval in Japan (September 24, 2024)
What has happened recently
FDA-approved on January 22, 2021 (NDA 213716, Aurinia), a new molecular entity, with a background immunosuppressive regimen for adults with active lupus nephritis; the label says use with cyclophosphamide is not recommended. The approval letter required pediatric studies from age 5 to 17 (waived under 5), a lactation study and the final AURORA 2 report, and Aurinia committed to an OATP1B1 drug interaction study. An efficacy labeling update followed on April 29, 2024, and the current label includes the 2-year extension; hypersensitivity reactions were added to the warnings in October 2025. The EU authorized Lupkynis on September 15, 2022 (holder Otsuka Pharmaceutical Netherlands B.V.), with mycophenolate mofetil for class III, IV or V lupus nephritis, and Aurinia announced Japanese approval with mycophenolate mofetil on September 24, 2024. Isotechnika discovered it, licensed it for lupus to Vifor in January 2012 and announced a merger with Aurinia on February 5, 2013; in 2020 Aurinia licensed it to Otsuka for the EU, Japan, the UK and other markets. An earlier uveitis filing by Lux Biosciences, as Luveniq, drew an FDA complete response letter (announced August 4, 2010) and a negative CHMP opinion in the EU (June 23, 2011); Lux withdrew the EU application during re-examination on October 13, 2011. No generic is listed.
You can compare this against the whole library, or read how to check a seller.
What else is like Voclosporin (Lupkynis)?
Others in Immune support, side by side.If you're weighing Voclosporin (Lupkynis), it's worth reading Cyclosporine (Sandimmune, Restasis), Omiganan (MBI-226), and Thymalin in the same class.
Cyclosporine with one extra carbon on its first residue, approved in the US in 2021 for lupus that attacks the kidneys. Added to standard treatment, it nearly doubled full kidney responses at one year.
- Dose
- 23.7 mg (three 7.9 mg capsules) per dose (label)
- How often
- Twice daily, about 12 hours apart, on an empty stomach
A ring of 11 unusual amino acids from a soil fungus, approved for transplants in 1983 and as dry-eye drops since 2002. The drops barely reach the blood; the capsules and infusion carry boxed warnings.
- Dose
- One drop in each eye (eye drops, label)
- How often
- Twice daily
A short, tryptophan- and arginine-rich peptide gel that disrupts microbial membranes. Two catheter-site phase 3 trials missed their primary endpoints, and its two rosacea phase 3 trials split, one positive and one negative.
- Dose
- 1% gel at catheter sites, 1.6% gel on rosacea (phase 3 trials)
- How often
- Each dressing change (catheters) or once daily (rosacea)
A thymus peptide taken in courses to refresh immune function and aging.
- Dose
- 5 up to 10 mg per day (start low, increase slowly)
- How often
- 10-day courses
Guides for this compound
- mcg vs mg: The Peptide Dosing Mistake to Avoid
Your vial says mg and your protocol says mcg. Here is the conversion and how to check it.
Sources
- Lupkynis prescribing information, DailyMed (revised 8/2026)(2026)23.7 mg twice daily; eGFR rules; boxed warning for malignancies and serious infections; GFR decreased 26% against 9%; half-life about 30 hours; C63H111N11O12.
- Drugs@FDA, NDA 213716(2026)Approved January 22, 2021, as a new molecular entity; label supplements in 2024 and 2025.
- FDA approval letter, NDA 213716(2021)Indication with a background immunosuppressive regimen; pediatric, lactation and AURORA 2 studies required; an OATP1B1 interaction study committed.
- FDA GSRS substance record, voclosporin (UNII 2PN063X6B1)(2026)CAS 515814-01-4; C63H111N11O12, MW 1214.62; names ISA247, LX211 and Lupkynis; SMILES showing the diene on residue 1.
- EMA, Lupkynis EPAR(2026)EU authorization September 15, 2022, with mycophenolate mofetil for class III, IV or V lupus nephritis; Otsuka Pharmaceutical Netherlands B.V.
- EMA, Luveniq withdrawal assessment report(2011)Uveitis filing; residue-1 change alters calcineurin binding and metabolism; at least 90% trans isomer; ketoconazole raised exposure more than 18-fold.
- Rovin BH et al., Lancet 2021;397:2070-2080 (AURORA 1)(2021)357 randomized: complete renal response at 52 weeks 40.8% against 22.5% (OR 2.65, 95% CI 1.64 to 4.27); deaths 1 against 5.
- Saxena A et al., Arthritis and Rheumatology 2024;76:59-67 (AURORA 2)(2024)216 continued for 2 more years: complete renal response 50.9% against 39.0%; eGFR slope -0.2 against -5.4 mL/min/1.73 m2.
- ClinicalTrials.gov, AURA-LV results (NCT02141672); Rovin BH et al., Kidney International 2019;95:219-231(2021)265 patients: week-24 remission 32.6% and 27.3% against 19.3%; deaths 10 of 89, 2 of 88 and 1 of 88.
- Aurinia, AURA-LV 48-week results (April 20, 2017)(2017)Complete remission at week 48: 49% and 40% against 24% on placebo.
- Busque S et al., American Journal of Transplantation 2011;11:2675-2684 (PROMISE)(2011)334 kidney recipients, three voclosporin exposures against tacrolimus over 6 months: rejection 10.7%, 9.1% and 2.3% against 5.8%.
- Isotechnika, ESSENCE psoriasis results (April 28, 2009)(2009)642 patients: 35% clear or almost clear against 6% on placebo; noninferiority to cyclosporine (53%) not met.
- Aurinia, AUDREY dry-eye results (November 2, 2020)(2020)508 patients: primary endpoint missed (10%, 9% and 11% against 5%); dry-eye program suspended.
- Nasdaq/RTT, Lupkynis approval in Japan (September 24, 2024)(2024)Japanese approval for lupus nephritis with mycophenolate mofetil announced; Otsuka holds the rights.
Beyond these, 250 records are indexed. Browse the records