2023

Sparsentan

by cyb2025

RODRIGO SOUZA
Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University of Rio de Janeiro, Rio de Janeiro, Brazils

Sparsentan (Filspari) is an endothelin and angiotensin II receptor antagonist indicated to reduce proteinuria in adults with primary immunoglobulin A nephropathy. IgA nephropathy (IgAN) is a rare kidney disorder characterized by the buildup of immunoglobulin A (IgA) in the kidneys. Deposits of IgA in the kidneys cause a breakdown of the normal filtering mechanisms, leading to proteinuria and hematuria. Other symptoms may include kidney pain, edema, and high blood pressure. Sparsentan is a Dual Endothelin Angiotensin Receptor Antagonist (DEARA) that works to reduce proteinuria in IgAN by selectively targeting the endothelin A receptor (ETAR) and the angiotensin II subtype 1 receptor (AT1R). Blockade of the endothelin type A and angiotensin II type 1 pathways limits IgA nephropathy progression by reducing proteinuria, protecting podocytes, and preventing glomerulosclerosis and mesangial cell proliferation. FDA approval was granted to Travere Pharmaceuticals. The company was once called Retrophin but rebranded in 2020 to free itself from any ties with its founder, the “pharma bro” Martin Shkreli. As for Sparsentan, the drug has changed hands many times. It was originally developed by Bristol Myers Squibb and then licensed to Pharmacopeia LCC, which was acquired by Ligand Pharmaceuticals. Travere got the drug from Ligand in 2012.

 

 

ABOUT THE AUTHOR

Rodrigo Souza – Since I started my independent career, I have pursuit the development of new technologies to guide research by innovative ideas. We have been working at Federal University of Rio de Janeiro on the establishment of continuous flow technology for active pharmaceutical ingredients (API) synthesis in Brazil, showing that is possible to reduce costs on production allowing the reduction of the final price of the medicine.

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