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Dinifedriton

From Wikipedia, the free encyclopedia
Dinifedriton
Clinical data
Other namesHU6
Legal status
Legal status
  • Investigational
Identifiers
  • 5-[(2,4-Dinitrophenoxy)methyl]-1-methyl-2-nitroimidazole
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC11H9N5O7
Molar mass323.221 g·mol−1
3D model (JSmol)
  • CN1C(=CN=C1[N+](=O)[O-])COC2=C(C=C(C=C2)[N+](=O)[O-])[N+](=O)[O-]
  • InChI=1S/C11H9N5O7/c1-13-8(5-12-11(13)16(21)22)6-23-10-3-2-7(14(17)18)4-9(10)15(19)20/h2-5H,6H2,1H3
  • Key:LRJQZGXEGNOHBH-UHFFFAOYSA-N

Dinifedriton, also known as HU6, is a prodrug of the mitochondrial uncoupler 2,4-dinitrophenol (DNP) that is intended to "minimize the rapid absorption and high peak blood concentrations of DNP to provide a wider therapeutic index and improve safety."[1] Developed by Rivus Pharmaceuticals, the drug is tested to reduce weight and liver fat in humans with risk factors for metabolic dysfunction-associated steatohepatitis. In a phase 2a trial, the higher dosage levels reduced liver fat on average by more than 30 percent and also reduced body weight significantly.[2][3] A phase 2b trial was launched in late 2023.[4] A phase 2b trial in patients with metabolic dysfunction-associated steatohepatitis was subsequently initiated.[5] Data from this study are expected to be reported in 2025. Additionally, a phase 2a study was performed in patients suffering from heart failure with preserved ejection fraction, a disease that is mediated by visceral fat and obesity. The study achieved the primary endpoint of weight loss, as well as a number of secondary endpoints.[6]

References

[edit]
  1. Noureddin, Mazen; Khan, Shaharyar; Portell, Francisco; Jorkasky, Diane; Dennis, Jameel; Khan, Omer; Johansson, Lars; Johansson, Edvin; Sanyal, Arun J (December 2023). "Safety and efficacy of once-daily HU6 versus placebo in people with non-alcoholic fatty liver disease and high BMI: a randomised, double-blind, placebo-controlled, phase 2a trial". The Lancet Gastroenterology & Hepatology. 8 (12): 1094–1105. doi:10.1016/S2468-1253(23)00198-X. PMID 37806314.
  2. Harrison, Stephen A.; Loomba, Rohit; Dubourg, Julie; Ratziu, Vlad; Noureddin, Mazen (July 2023). "Clinical Trial Landscape in NASH". Clinical Gastroenterology and Hepatology. 21 (8): 2001–2014. doi:10.1016/j.cgh.2023.03.041. PMID 37059159.
  3. Noureddin, Mazen; Khan, Shaharyar; Portell, Francisco; Jorkasky, Diane; Dennis, Jameel; Khan, Omer; Johansson, Lars; Johansson, Edvin; Sanyal, Arun J (December 2023). "Safety and efficacy of once-daily HU6 versus placebo in people with non-alcoholic fatty liver disease and high BMI: a randomised, double-blind, placebo-controlled, phase 2a trial". The Lancet Gastroenterology & Hepatology. 8 (12): 1094–1105. doi:10.1016/S2468-1253(23)00198-X. PMID 37806314.
  4. "Rivus Pharmaceuticals Announces Expansion of HU6 Clinical Program and New Leadership Appointments". Yahoo Finance. 15 November 2023. Retrieved 3 December 2023.
  5. "Rivus Pharmaceuticals Announces Expansion of HU6 Clinical Program and New Leadership Appointments". Yahoo Finance. 15 November 2023. Retrieved 3 December 2023.
  6. "Rivus Pharmaceuticals Announces New Clinical Data from Phase 2a HuMAIN Trial Demonstrating Significant Weight Loss with HU6 in Patients with Obesity-Related HeartFailure" (PDF). September 30, 2024.