sparsentan
FIC oral, once-daily, dual ETA/AT1 antagonist FDA-approved for proteinuria reduction in primary IgAN opt. of known ETA/AT1 antagonist FDA accelerated approval, February 17, 2023 Travere Therapeutics, San Diego, CA
Other molecules you may be interested in
daprodustat
Daprodustat is the first HIF-prolyl hydroxylase domain (PHD) inhibitor that has been approved for the treatment of anemia in chronic kidney disease (CKD) and marks the first novel anemia treatment approved in the US in >30 years. PHDs have been attractive targets for treating anemia, especially in CKD patients, because the enzymes regulate levels of hypoxia-inducible factors (HIFs) including HIF-2, which induces the production of erythropoietin that in turn stimulates red blood cell production. The small molecule drug has similar safety and activity as epoetin alfa, an injected biologic.
vadadustat (VAFSEO)
Vadadustat (Vafseo) from Akebia Therapeutics is an oral hypoxia-inducible factor prolyl-4-hydroxylase domain (HIF-PHD) inhibitor developed for anemia in patients with chronic kidney disease (CKD). It received FDA approval on March 27th, 2024 for patients on dialysis for at least three months, after regulatory challenges including an earlier complete response letter due to safety concerns. This makes vadadustat the second FDA-approved HIF-PHD inhibitor for the treatment of anemia in CKD for dialysis-dependent patients after GSK’s daprodustat’s approval in Feb. 2023.
TP0472993
The arachidonic acid (AA) metabolite, 20-hydroxy-5,8,11,14-eicosatetranoic acid (20-HETE), has been extensively studied as a modulator of kidney function and a mediator of kidney diseases over decades. The receptor for 20-HETE, the G-coupled protein receptor GPR75, was only recently identified (2017), and GPR75/20-HETE pathway modulators are of industry interest in many disease areas including obesity (e.g. 2020 Regeneron patent filing) and kidney diseases (e.g. 2018 Taisho patent filing).
"Compound 19" (iron-binder)
“Compound 19” (iron-binder) is an oral inhibitor of the hypoxia-inducible factor (HIF) propyl hydroxylase domain (HIF-PHD), increasing HIF levels to activate EPO transcription and promote hematopoiesis for treatment of anemia. Interestingly, this compound is modeled to make a bi-dentate interaction with an iron co-factor of HIF-PHD via a [...]
BI 685509
A newly disclosed sGC activator in Ph. II for CKD/DKD. This month, researchers at BI reported promising preclinical results for a newly disclosed sGC activator, BI-685509, which is in several Ph. II trials including for treatment of chronic kidney disease (CKD) and diabetic kidney disease (DKD) ( NCT04736628 , NCT04750577 ). In rodents, the [...]
