bilirubin nanoparticle (OPTA-INFLA oral) / Bilix - LARVOL DELTA

Renoprotective effects of synthetic bilirubin nanomedicine against ischemia-reperfusion injury after kidney transplantation. (PubMed, Clin Sci (Lond)) - "In the present study, we investigated renoprotective effects of BX-001N, a synthetic polyethylene glycol-conjugated bilirubin nanoparticle, against renal IRI after kidney transplantation...It also inhibited renal fibrosis and suppressed epithelial-mesenchymal transition with decreased expression of α-smooth muscle actin, while preserving E-cadherin expression. In conclusion, BX-001N effectively mitigates IRI-induced renal injury by reducing oxidative stress, inflammation, and fibrosis, indicating its potential therapeutic value in kidney transplantation."

Journal • Acute Kidney Injury • Cardiovascular • Fibrosis • Immunology • Inflammation • Nephrology • Renal Disease • Reperfusion Injury • Transplantation • CDH1 • HMOX1 • IFNG • TNFA

Renoprotective Effects of BX-001N Against Cold Ischemia-Reperfusion Injury in a Murine Model of Kidney Transplantation: Transplantation (KSN 2025) - "In this study, BX-001N, a synthetic PEGylated bilirubin nanoparticle, demonstrated promising renoprotective effects through its antioxidant and anti-inflammatory properties...Conclusions : BX-001N effectively attenuates cold IRI-induced renal injury by reducing oxidative stress, inflammation, and fibrosis while promoting renal repair. These findings suggest BX-001N as a promising therapeutic candidate for improving outcomes in renal cold IRI during kidney transplantation."

Preclinical • Acute Kidney Injury • Cardiovascular • Fibrosis • Immunology • Nephrology • Oncology • Renal Disease • Reperfusion Injury • Transplantation • CDH1 • CXCL1 • HMOX1 • TNFA • VIM

Synthetic Bilirubin-Based Nanomedicine Protects Against Renal Ischemia/Reperfusion Injury Through Antioxidant and Immune-Modulating Activity. (PubMed, Adv Healthc Mater) - "In conclusion, BX-001N, the first Good Manufacturing Practice-grade synthetic bilirubin-based nanomedicine attenuates acute renal injury and chronic fibrosis by suppressing ROS generation and inflammation after IRI. It shows adequate safety profiles and holds promise as a new therapy for renal IRI."

Journal • Acute Kidney Injury • Cardiovascular • Fibrosis • Immune Modulation • Immunology • Inflammation • Nephrology • Renal Disease • Reperfusion Injury • TNFA

Investigation of pharmacokinetic properties of a PEGylated bilirubin nanoparticle in male Sprague-Dawley rats using liquid chromatography-quadrupole time-of-flight mass spectrometry. (PubMed, Xenobiotica) - "Polyethylene glycol (PEG) was introduced into synthetic bilirubin 3α and a PEGylated bilirubin 3α nanoparticle (BX-001N, Brixelle®) was developed for the first time.An in vitro microsomal stability study, in vivo PK studies with intravenous bolus (IV) and subcutaneous injection (SC), and a semi-mass balance study of BX-001N were investigated to evaluate its pharmacokinetic (PK) properties in male Sprague-Dawley (SD) rats using developed liquid chromatography-quadrupole time-of-flight mass spectrometry (LC-qTOF/MS).Following IV administration at 10 or 30 mg/kg, BX-001N showed very low clearance (0.33-0.67 mL/min/kg) with predominant distribution in the vascular system (Vd = 51.73-83.02 mL/kg). BX-001N was also very stable in vitro liver microsomal stability study.Following SC administration at 10 or 30 mg/kg, the bioavailability of BX-001N in plasma at 10 mg/kg was around 43% and showed the less dose-proportionality at 30 mg/kg dose.BX-001N was mainly excreted via..."

Journal • PK/PD data • Preclinical