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  • ||||||||||  papiliximab / Shaperon
    Papiliximab, a bispecific nanobody targeting CD47 and PDL1 retards tumor growth without hemolysis (Section 6) -  Mar 5, 2024 - Abstract #AACR2024AACR_5532;    
    These observations suggest that Papiliximab might be able to improve clinical remission more effectively than the combination of monotherapies without the risk of anemia associated with anti-CD47 MoAbs. We are now working to elucidate the mechanisms behind Papiliximab's superior efficacy and safety compared to the combination of monotherapies.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Trial completion date, Trial primary completion date:  Phase 2b/3 Trial of NuSepin (clinicaltrials.gov) -  Mar 21, 2023   
    P2b,  N=1134, Recruiting, 
    Our study demonstrated that the total amount of norepinephrine required to maintain a mean pressure was reduced by anti-inflammatory agents, NuSepin Trial completion date: Dec 2022 --> Dec 2024 | Trial primary completion date: Sep 2022 --> Nov 2024
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    New P2b trial:  Phase 2b/3 Trial of NuSepin (clinicaltrials.gov) -  Apr 28, 2022   
    P2b,  N=1134, Recruiting, 
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  Short communication: Chemical structure, concentration, and pH are key factors influencing antimicrobial activity of conjugated bile acids against lactobacilli. (Pubmed Central) -  Apr 7, 2021   
    Considerable differences were observed in the antimicrobial activity between the 6 human conjugated bile acids, including glycocholic acid, taurocholic acid, glycodeoxycholic acid, taurodeoxycholic acid, glycochenodeoxycholic acid, and taurochenodeoxycholic acid...In conclusion, chemical structure, concentration, and pH are key factors influencing antimicrobial activity of conjugated bile acids against lactobacilli. This study provides theoretical guidance and technology support for developing a scientific method for evaluating the bile tolerance ability of potentially probiotic strains of lactobacilli.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Trial completion date, Trial primary completion date:  Clinical Trial to Investigate the Efficacy and Safety of NuSepin® in COVID-19 Pneumonia Patients (clinicaltrials.gov) -  Mar 17, 2021   
    P2,  N=60, Recruiting, 
    This study provides theoretical guidance and technology support for developing a scientific method for evaluating the bile tolerance ability of potentially probiotic strains of lactobacilli. Trial completion date: Nov 2020 --> Apr 2021 | Trial primary completion date: Nov 2020 --> Apr 2021
  • ||||||||||  hyodeoxycholic acid (AHRO-001) / AtheroNova, NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  NASH-related increases in plasma bile acid levels depend on insulin resistance. (Pubmed Central) -  Feb 23, 2021   
    P=N/A
    Plasma bile acids have been proposed as NASH biomarkers. Herein, we found that plasma bile acids are only elevated in patients with NASH when significant insulin resistance is present, limiting their utility as NASH markers.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  Dietary taurine stimulates the hepatic biosynthesis of both bile acid and cholesterol in the marine teleost, tiger puffer (Takifugu rubripes). (Pubmed Central) -  Feb 17, 2021   
    The hepatic bile acid profile mainly includes taurocholic acid (94·48 %), taurochenodeoxycholic acid (4·17 %) and taurodeoxycholic acid (1·35 %), and the contents of all these conjugated bile acids were increased by dietary TAU...Taurine also stimulated the hepatic expression of lipogenic genes. In conclusion, dietary taurine stimulated the hepatic biosynthesis of both bile acid and cholesterol, and tended to regulate the lipid metabolism in multiple ways.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  The gut microbiota confers protection in the CNS against neurodegeneration induced by manganism. (Pubmed Central) -  Feb 12, 2021   
    In addition, Mn exposure altered the metabolism of tryptamine, taurodeoxycholic acid, β-hydroxypyruvic acid and urocanic acid...Fecal microbiome transplantation from normal rats could alleviate the neurotoxicity of Mn exposure by shaping the gut microbiota. Our findings highlight the role of gut dysbiosis-promoted neurotoxicity in Mn exposure and suggest a novel therapeutic strategy of remodeling the gut microbiota.
  • ||||||||||  hyodeoxycholic acid (AHRO-001) / AtheroNova, NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  Quantification of bile acids: A mass spectrometry platform for studying gut microbe connection to metabolic diseases. (Pubmed Central) -  Feb 9, 2021   
    BAs whose circulating levels are associated with T2DM include numerous 12α-hydroxyl BAs (taurocholic acid, taurodeoxycholic acid, glycodeoxycholic acid, deoxycholic acid and 3-ketodeoxycholic acid), while taurohyodeoxycholic acid was negatively associated with diabetes. The LC/MS/MS based platform described should serve as a robust, high throughput investigative tool for studying the potential involvement of structurally specific BAs and the gut microbiome on both physiological and disease processes.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Clinical, Journal:  Pre-diagnostic plasma bile acid levels and colon cancer risk: A prospective study. (Pubmed Central) -  Jan 9, 2021   
    This prospective study showed that pre-diagnostic levels of certain conjugated primary and secondary bile acids were positively associated with risk of colon cancer. Our findings support experimental data to suggest that a high bile acid load is colon cancer promotive.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  Investigation of chemical profile of bile acids and determination of them in cultured Bovis Calculus with UPLC-QDA (Pubmed Central) -  Dec 30, 2020   
    The results showed that nine common bile acids, cholic acid(CA), deoxycholic acid(DCA), chenodeoxycholic acid(CDCA), taurocholic acid(TCA), taurodeoxycholic acid(TDCA), taurochenodeoxycholic acid(TCDCA), glycocholic acid(GCA), glycodeoxycholic acid(GDCA) and glycochenodeoxycholic acid(GCDCA), were founded in samples and 7 bile acids were quantified except GDCA and GCDCA...As for unconjugated bile acids, CA was the most major bile acid in cultured cow-bezoar and it was about twice as much as DCA. The relative low-cost method established in the current study is accurate, rapid and sensitive, which is suitable for the studies of other drugs from animal bile.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  The reabsorption of bile acids regulated by FXR-OATP1A2 is the main factor for the formation of cholesterol gallstone. (Pubmed Central) -  Dec 16, 2020   
    The concentrations of taurodeoxycholic acid and taurolithocholic acid in the bile of patients were significantly higher than that of the controls...In conclusion, the axis of FXR-OATP1A2 that physiologically regulated the reabsorption of bile acids might play an important role in the composition of bile acids and the development of gallstone. CYP8B1 gene was irrelevant to the altered composition of bile acids in patients with gallstone.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Trial completion, Trial completion date:  A Study of HY209 in Healthy Male Volunteers for Sepsis (clinicaltrials.gov) -  Nov 30, 2020   
    P1,  N=40, Completed, 
    CYP8B1 gene was irrelevant to the altered composition of bile acids in patients with gallstone. Recruiting --> Completed | Trial completion date: Dec 2020 --> Jun 2020
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    [VIRTUAL] RHEOLOGICAL PROPERTIES OF BILE IN PATIENTS WITH NONALCOHOLIC STEATOHEPATITIS AND THYROID GLAND DYSFUNCTION (Poster Exhibition) -  Jul 19, 2020 - Abstract #UEGW2020UEGW_5025;    
    To evaluate the colloidal stability of the bile, the ratio of taurochenodeoxycholic acid (TCDCA) and taurodeoxycholic acid (TDCA) to taurocholic acid (TCA) and the ratio of glycochenodeoxycholic acid (GCDCA) and glycodeoxycholic acid (GDCA) to glycocholic acid (GCA) were calculated... Decreased coefficient of conjugation and hydroxylation, as well as the levels of glycoconjugates and tauroconjugates of the bile in patients with NASH combined with HT suggests the possible influence of hypothyroidism on colloidal properties of bile and thus indicates on an increased risk of gallstones formation.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    [VIRTUAL] CORRELATION OF BILE ACID FRACTIONS AND LIVER STRUCTURAL CHANGES IN CHILDREN WITH NON-ALCOHOLIC STEATOHEPATITIS (Poster Exhibition) -  Jul 19, 2020 - Abstract #UEGW2020UEGW_4897;    
    Decreased coefficient of conjugation and hydroxylation, as well as the levels of glycoconjugates and tauroconjugates of the bile in patients with NASH combined with HT suggests the possible influence of hypothyroidism on colloidal properties of bile and thus indicates on an increased risk of gallstones formation. Revealed association of liver structure, bile acids content, carbohydrate metabolism features demonstrated the possibility to influence the liver fibrosis progression by bile acids ratio regulation.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    [VIRTUAL] RHEOLOGICAL PROPERTIES OF BILE IN PATIENTS WITH NONALCOHOLIC STEATOHEPATITIS AND THYROID GLAND DYSFUNCTION (Poster Exhibition) -  Jul 19, 2020 - Abstract #UEGW2020UEGW_3049;    
    To evaluate the colloidal stability of the bile, the ratio of taurochenodeoxycholic acid (TCDCA) and taurodeoxycholic acid (TDCA) to taurocholic acid (TCA) and the ratio of glycochenodeoxycholic acid (GCDCA) and glycodeoxycholic acid (GDCA) to glycocholic acid (GCA) were calculated... Decreased coefficient of conjugation and hydroxylation, as well as the levels of glycoconjugates and tauroconjugates of the bile in patients with NASH combined with HT suggests the possible influence of hypothyroidism on colloidal properties of bile and thus indicates on an increased risk of gallstones formation.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    [VIRTUAL] CORRELATION OF BILE ACID FRACTIONS AND LIVER STRUCTURAL CHANGES IN CHILDREN WITH NON-ALCOHOLIC STEATOHEPATITIS (Poster Exhibition) -  Jul 19, 2020 - Abstract #UEGW2020UEGW_2921;    
    Decreased coefficient of conjugation and hydroxylation, as well as the levels of glycoconjugates and tauroconjugates of the bile in patients with NASH combined with HT suggests the possible influence of hypothyroidism on colloidal properties of bile and thus indicates on an increased risk of gallstones formation. Revealed association of liver structure, bile acids content, carbohydrate metabolism features demonstrated the possibility to influence the liver fibrosis progression by bile acids ratio regulation.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    [VIRTUAL] RHEOLOGICAL PROPERTIES OF BILE IN PATIENTS WITH NONALCOHOLIC STEATOHEPATITIS AND THYROID GLAND DYSFUNCTION (Poster Exhibition) -  Jul 19, 2020 - Abstract #UEGW2020UEGW_1065;    
    To evaluate the colloidal stability of the bile, the ratio of taurochenodeoxycholic acid (TCDCA) and taurodeoxycholic acid (TDCA) to taurocholic acid (TCA) and the ratio of glycochenodeoxycholic acid (GCDCA) and glycodeoxycholic acid (GDCA) to glycocholic acid (GCA) were calculated... Decreased coefficient of conjugation and hydroxylation, as well as the levels of glycoconjugates and tauroconjugates of the bile in patients with NASH combined with HT suggests the possible influence of hypothyroidism on colloidal properties of bile and thus indicates on an increased risk of gallstones formation.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    [VIRTUAL] CORRELATION OF BILE ACID FRACTIONS AND LIVER STRUCTURAL CHANGES IN CHILDREN WITH NON-ALCOHOLIC STEATOHEPATITIS (Poster Exhibition) -  Jul 19, 2020 - Abstract #UEGW2020UEGW_937;    
    Decreased coefficient of conjugation and hydroxylation, as well as the levels of glycoconjugates and tauroconjugates of the bile in patients with NASH combined with HT suggests the possible influence of hypothyroidism on colloidal properties of bile and thus indicates on an increased risk of gallstones formation. Revealed association of liver structure, bile acids content, carbohydrate metabolism features demonstrated the possibility to influence the liver fibrosis progression by bile acids ratio regulation.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  Trace level analyses of selected perfluoroalkyl acids in food: Method development and data generation. (Pubmed Central) -  Jul 11, 2020   
    The method was shown effective to eliminate taurodeoxycholic acid (TDC), a bile acid that is an endogenous interference compound in egg samples causing ionization suppression and false positive result for PFOS when 499 > 80 transition was used for quantification...This method can be applied to enforce potential future limit values for PFOS and PFOA as a consequence of the recent European Food Safety Authority (EFSA) recommendation where the tolerable intakes have been drastically lowered. Further method development is needed for foods of plant origin such as vegetables, flour, nuts, or bread.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  American eels produce and release bile acid profiles that vary across life stage. (Pubmed Central) -  Jun 28, 2020   
    Taurochenodeoxycholic acid, taurodeoxycholic acid, cholic acid, deoxycholic acid, taurolithocholic acid and taurocholic acid were detected in whole tissue of American glass eels and elvers, and in liver, intestine and gallbladder samples of late-stage yellow eels...This study is novel because little was previously known about bile acids produced and emitted into the environment by American eels. Future behavioural studies could evaluate whether any bile acids produced by American eels influence conspecific migratory behaviour.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    CIGARETTE SMOKE PROMOTES COLORECTAL CANCER THROUGH MODULATION OF GUT MICROBIOTA AND RELATED METABOLITES () -  May 4, 2020 - Abstract #DDW2020DDW_4120;    
    Metabolites profiling revealed increased nicotine and secondary bile acid including taurodeoxycholic acid, which could together promote colon carcinogenesis, in smoke-exposed mice... Cigarette smoke promotes colon tumorigenesis by inducing gut microbiota dysbiosis and alteration of metabolites, resulting in gut barrier dysfunction, MDSCs infiltration and pro-oncogenic MAPK signaling activation
  • ||||||||||  Acomplia (rimonabant) / Sanofi, NuSepin (taurodeoxycholic acid) / Shaperon
    Endocannabinoids Induce Endoplasmic Reticulum Stress in Hepatocytes and Human Coronary Artery Endothelial Cells (ENDOExpo) -  Apr 1, 2020 - Abstract #ENDO2020ENDO_4082;    
    ER stress in cells treated with AN and 2-AG, but not TM, was inhibited by the CNR1 antagonist rimonabant...Finally, AN and 2-AG treatment induced CNR1 expression in both cell lines. These results strongly suggest that EC's promote ER stress and potentially induce liver and endothelial cell dysfunction.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Journal:  MALDI-Mass Spectrometry Imaging to Investigate Lipid and Bile Acid Modifications Caused by Lentil Extract Used as a Potential Hypocholesterolemic Treatment. (Pubmed Central) -  Feb 25, 2020   
    This indicates that the lentil extract lowers the total cholesterol level in two synergic ways: (i) it increases the excretion of bile acids; hence, new bile acids are produced in the liver from serum cholesterol and (ii) the prebiotic effect leads to free taurine which upregulates the de novo synthesis of bile acid from cholesterol while activating LDL receptors. We demonstrate here that mass spectrometry imaging is a valuable tool for a better understanding of the effects of treatments such as for the synergistic cholesterol-lowering effect of the lentil extract.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    Duodenal bile salts and mucosal changes are linked with gastric emptying and symptoms in functional dyspepsia patients. (Room TIFFANY/SHAH) -  Feb 24, 2020 - Abstract #BWG2020BWG_91;    
    A significant effect of the secondary bile salt taurodeoxycholic acid was found on paracellular dextran-passage (F=7.19, p=0.016) and T1/2 (F=7.82, p=0.014), but the effect on gastric emptying was not mediated by dextran-passage (F=0.19, p=0.67)...Indeed, symptoms are associated with duodenal eosinophils in FD patients. Although duodenal bile salts have significant associations with both gastric emptying and symptoms, the mechanisms do not seem to involve duodenal barrier or immune function and require further study in FD.
  • ||||||||||  NuSepin (taurodeoxycholic acid) / Shaperon
    DUODENAL BILE SALTS AND MUCOSAL CHANGES ARE LINKED WITH GASTRIC EMPTYING AND SYMPTOMS IN FUNCTIONAL DYSPEPSIA PATIENTS () -  Jan 28, 2020 - Abstract #DDW2020DDW_3407;    
    A significant effect of the secondary bile salt taurodeoxycholic acid was found on paracellular dextran-passage (F=7.19, p=0.016) and T1/2 (F=7.82, p=0.014), but the effect on gastric emptying was not mediated by dextran-passage (F=0.19, p=0.67)...Indeed, symptoms are associated with duodenal eosinophils in FD patients. Although duodenal bile salts have significant associations with both gastric emptying and symptoms, the mechanisms do not seem to involve duodenal barrier or immune function and require further study in FD.
  • ||||||||||  NuGel (taurodeoxycholic acid) / Shaperon
    Trial completion date, Trial primary completion date:  Shaperon: A Phase I Study of HY209 Gel in Healthy Male Volunteers for Atopic Dermatitis (clinicaltrials.gov) -  Apr 10, 2019   
    P1,  N=56, Enrolling by invitation, 
    Although duodenal bile salts have significant associations with both gastric emptying and symptoms, the mechanisms do not seem to involve duodenal barrier or immune function and require further study in FD. Trial completion date: Dec 2018 --> Aug 2019 | Trial primary completion date: Sep 2018 --> Jul 2019