First lupus nephritis (LN) oral drug! Lupkynis, the best-in-class calcium-adjusted neurophosphatase inhibitor, has been approved by the FDA!

26, 2021 // / -- Aurinia Pharma is a biopharmaceutical company dedicated to the development of innovative therapies for kidney disease and autoimmune diseases.
recently, the company announced that the U.S. Food and Drug Administration (FDA) has approved Lupkynis (voclosporin), a joint background immunosuppressive therapy for the treatment of active lupus nephritis (LN) adult patients.
LN is one of the most serious and common complications of systemic lupus (SLE), an autoimmune disease that causes irreversible kidney damage and significantly increases the risk of kidney failure, heart events, and death.
December 2020, GlaxoSmithKline antibody drug Benlysta (Beliten, generic name: belimumab, injection with bellevue monoantigen) was approved by the U.S. FDA as the first drug to treat LN.
Lupkynis is the first oral treatment approved by the FDA to treat LN.
In key clinical trials, patients treated with Lupkynis in a joint treatment with Standard Care (SoC) were more than twice as likely to achieve kidney remission as patients treated with typical SoC, and patients with a urinary protein creatinine ratio (UPCR) decreased twice as fast as those treated with typical SoC.
UPCR is a standard measurement method for monitoring kidney protein levels.
early intervention and kidney remission are associated with better long-term outcomes and prevention of irreversible kidney damage.
patients treated with Lupkynis showed improved response rates in all parameters of the LN immunoactive category studied.
Lupus Nephritis (LN) is a severe kidney inflammation caused by the autoimmune disease systemic lupus erythematosus (SLE), which represents a serious advance in SLE and, if left uncontroversized, can lead to permanent, irreversible tissue damage in the kidneys, leading to end-stage renal disease (ESRD), which is life-threatening.
December 2020, GlaxoSmithKline Benlysta was approved by the U.S. FDA as the first drug to treat LN, which is suitable for adult patients with active LN who are receiving standard treatment.
was approved in 2011 as the first new drug approved for the treatment of systemic lupus erythematosus (SLE) in more than 50 years.
in China, Benlysta was approved in July 2019.
as the world's first biological agent approved for treatment of SLE, Pereid has been approved in China in a joint with conventional treatment for adult patients with SLE who are still highly active and self-antibody-positive on the basis of conventional treatment.
approval of the oral drug Lupkynis, based on the support of a wide range of clinical development projects, including key Phase III ARORA studies and key Phase II AURALV studies.
AURORA is a global, placebo-controlled, critical Phase III study that showed that voclosporin improved the near-term and long-term prognosis of patients with lupus nephritis when combined with mycophenolic acid (MMF) and low-dose oral corticosteroids compared to placebo.
specific data were: voclosporin significantly increased the rate of renal remission (primary endpoint: 40.8% vs 22.5%, p<0.001) compared to placebo, and was equally statistically significant in terms of all pre-specified hierarchical endpoints.
study, the security of the voclosporin scheme is compared with that of the standard scheme.
voclosporin structure (Photo: Aurinia) voclosporin is a research drug, a new, potential best-in-class calcium-adjusted neurophosphatase inhibitor (CNI) with clinical data on more than 2,600 patients with multiple adaptations.
voclosporin is an immunosuppressant with synergetic and dual mechanisms.
called voclosporin stabilizes renal foot cells (podocyte) by inhibiting calcium-adjusted neurophosphatase (CN), blocking the expression of IL-2 and the Immune response mediated by T-cells.
voclosporin has a more predictable pharmacodynamic and pharmacological relationship (which may not require therapeutic drug monitoring), increased pot (compared to cyclosporine) and improved metabolic spectrum compared to traditional

structurally, voclosporin is a similar to cyclosporine A, with an additional single-stranded carbon extension with a double bond (ene bond) on the single-carbon chain.
voclosporin binds to the procycline protein A (cyclophilin A) to form an isopolymer complex, which then binds and inhibits calcium-adjusted phosphatase for immunosuppressive action.
voclosporin and cyclosporine A have the same binding affinity to human procycline protein, but voclosporin's ene-bond side chain induces structural changes in calcium-modulated phosphatase during binding, which can lead to enhanced immunosuppressive activity compared to cyclosporine A.
addition to lupus nephritis (LN), Aurinia is also developing voclosporin eye drops (VOS) for the treatment of dry eye disease (DES).
currently, there are three FDA-approved prescription drugs for DES treatment, two of which are CNI.
has the potential to improve the treatment of DES by reducing the time to achieve objective and subjective remission of DES symptoms and signs.
() Original source: FDA approves Aurinia Pharmaceuticals' LUPKYNIS™ for Adult Patients with Active Lupus Nephritis