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- | golexanolone (GR3027) / Karolinska Development
Preclinical, Journal: Golexanolone reduces glial activation in the striatum and improves non-motor and some motor alterations in a rat model of Parkinson's disease. (Pubmed Central) - Jul 8, 2024
Notably, golexanolone reduced the activation of microglia and astrocytes, mitigated TH loss at 5 weeks after surgery, and prevented the increase of ?-synuclein levels at 10 weeks. Golexanolone may be useful in improving both motor and non-motor symptoms that adversely affect the quality of life in PD patients, such as anxiety, depression, fatigue, motor coordination, locomotor gait, and certain cognitive alterations.
- || golexanolone (GR3027) / Karolinska Development
Review, Journal: Allopregnanolone And Its Antagonist Modulate Neuroinflammation And Neurological Impairment. (Pubmed Central) - May 9, 2024
What is surprising is the finding that both allopregnanolone, a steroid-PAM, and golexanolone, a novel GABA-A receptor modulating steroid antagonist (GAMSA), can inhibit microglia and astrocyte activation and normalize their function. This review focuses on the role of steroid-PAMs in neuroinflammation and their importance in new therapeutic approaches to CNS and liver disease.
- | golexanolone (GR3027) / Karolinska Development
Preclinical, Journal: Golexanolone improves fatigue, motor incoordination and gait and memory in rats with bile duct ligation. (Pubmed Central) - Nov 28, 2023
This review focuses on the role of steroid-PAMs in neuroinflammation and their importance in new therapeutic approaches to CNS and liver disease. Golexanolone may have beneficial effects to treat fatigue, and motor and cognitive impairment in patients with the chronic cholestatic liver disease PBC.
- || Preclinical, Review, Journal: Hepatic encephalopathy: investigational drugs in preclinical and early phase development. (Pubmed Central) - Nov 27, 2023
Current treatments are lactulose or rifaximin, acting on gut microbiota...HE may be reversed using drugs acting at any step: modulating microbiota with probiotics or fecal transplantation; reducing peripheral inflammation with anti-TNF?, autotaxin inhibitors or silymarin; reducing neuroinflammation with sulforaphane, p38 MAP kinase or phosphodiesteras 5 inhibitors, antagonists of sphingosine-1-phosphate receptor 2, enhancing meningeal lymphatic drainage or with extracellular vesicles from mesenchymal stem cells; reducing GABAergic neurotransmission with indomethacin or golexanolone...Only drugs acting on microbiota or ammonia reduction have been tested in patients. t is urgent to change the mentality on how to approach HE treatment to develop clinical trials to assess drugs acting on the immune system/peripheral inflammation, neuroinflammation or neurotransmission to improve HE.
- | golexanolone (GR3027) / Karolinska Development
Journal: Extra-Synaptic GABA Receptor Potentiation and Neurosteroid-Induced Learning Deficits Are Inhibited by GR3027, a GABA Modulating Steroid Antagonist. (Pubmed Central) - Oct 28, 2023
GR3027 treatment did not change other functions in the rat compared to the vehicle group. GR3027 functions in vitro as an inhibitor of GABA receptors holding ?5?3?2L and ?1?2?2L, in vivo, in the rat, as a dose-dependent inhibitor toward AP's negative effects on LoR and learning in the MWM.
- golexanolone (GR3027) / Karolinska Development
Golexanolone, a GABA receptor-modulating steroid antagonist, improves peripheral inflammation, fatigue, locomotor gait, motor incoordination and short-term memory in rats with cholestasis and hepatic encephalopathy due to bile duct ligation (Poster Area) - Apr 12, 2023 - Abstract #EASLILC2023EASL_ILC_1817;
This is associated with improvement in fatigue, locomotor gait and coordination, and short-term memory. Golexanolone may have beneficial effects to treat symptomatic alterations such as fatigue, and motor-, and cognitive impairment in patients with cholestatic liver disease, or hepatic encephalopathy
- golexanolone (GR3027) / Karolinska Development
GABA-A RECEPTOR MODULATING STEROIDS IMPAIR MEMORY, PROMOTES DEMENTIA, AND ANTAGONIZED BY GABA-A RECEPTOR MODULATING STEROID ANTAGONISTS. (On-Demand Oral Gallery E) - Dec 23, 2022 - Abstract #ADPD2023ADPD_507;
References: Bengtsson, et al. Neurobi ology of Stress , 2020; 12,100206:1 -20.
- | golexanolone (GR3027) / Karolinska Development
Preclinical, Journal: Golexanolone, a GABA receptor modulating steroid antagonist, restores motor coordination and cognitive function in hyperammonemic rats by dual effects on peripheral inflammation and neuroinflammation. (Pubmed Central) - Oct 7, 2022
Reducing GABA receptors activation with golexanolone reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in hyperammonemic rats. The effects identified would also occur in patients with hepatic encephalopathy and, likely, in other pathologies associated with neuroinflammation.
- |||| golexanolone (GR3027) / Karolinska Development
New P1/2 trial: A two-part study to investigate the effects in adults of two doses of a new drug called golexanolone in patients with primary biliary cholangitis with fatigue and cognitive dysfunction K (EUDRACT) - Jul 26, 2022
P1/2, N=101, Ongoing, Sponsor: Umecrine Cognition AB
- || golexanolone (GR3027) / Karolinska Development, sepranolone (UC1010) / Asarina Pharma
Clinical, Review, Journal: Positive GABA receptor modulating steroids and their antagonists: Implications for clinical treatments. (Pubmed Central) - Apr 20, 2022
The progesterone metabolite allopregnanolone (Allo) is a positive GABA receptor modulating steroid with potent effects...We have demonstrated that isoallopregnanolone (Isoallo), the 3β-OH sibling of Allo, functions as a GABA receptor modulating steroid antagonist (GAMSA) but without any effects of its own on GABA receptors...In humans, vigilance, cognition and pathological electroencephalogram were improved in patients with hepatic encephalopathy on treatment with GR3027. In conclusion GAMSAs are a new possible treatment for disorders and symptoms caused by hyperactivity in the GABA system.
- || golexanolone (GR3027) / Karolinska Development
Clinical, Journal: A pilot study of Golexanolone, a new GABA-A receptor modulating steroid antagonist, in patients with covert hepatic encephalopathy. (Pubmed Central) - Feb 5, 2022
P1/2
Golexanolone was well tolerated and associated with improvement in cognitive performance. The results implicate GABA-A receptor modulating neurosteroids in the pathogenesis of HE and suggest that golexanolone deserves further study as a potential therapeutic.
- ||| golexanolone (GR3027) / Karolinska Development
Golexanolone est un de nouveaux médicaments qui pouvant améliorer l’encéphalopathie hépatique( études en cours). Les premières résultats sont favorables pour l’instant. Lecture de @JasmohanBajaj #TLMdX #livertwitter (Twitter) - Nov 14, 2020
- ||| golexanolone (GR3027) / Karolinska Development
Golexanoloneأحد الأدوية الحديثة التي يتم دراستها على سموم الكبد (بدايات غيبوبة الكبد في تليف الكبد المتقدم) والنتائج الأولية تبدو مبشرة ) حسنت من التركيز والنشاط أثناء اليوم) نحتاج دراسات أكثر و أدوية لهذه الفئة من المرضى لتساعدهم من محاضرة @JasmohanBajaj #TLMdX #livertwitter (Twitter) - Nov 14, 2020
- |||| Xifaxan (rifaximin) / Alfa Wassermann, Bausch Health, Norgine, ASKA Pharma, golexanolone (GR3027) / Karolinska Development
just finished #hepaticencephalopathy session #TLMdX ✴️ new diagnoses: Flicker-App, speech ✴️ new gut-based Rx: #FMT, Soluble rifaximin ✴️ new brain-targeted Rx: Golexanolone ⛔️ neurosteroids The field is vibrant! 🙏 to all participants Great discussion and presentations! (Twitter) - Nov 14, 2020
- golexanolone (GR3027) / Karolinska Development
[VIRTUAL] A PILOT STUDY OF GOLEXANOLONE, A NOVEL GABA-A RECEPTOR MODULATING STEROID ANTAGONIST, IN PATIENTS WITH CIRRHOSIS AND COVERT HEPATIC ENCEPHALOPATHY (HE). () - Oct 11, 2020 - Abstract #AASLD2020AASLD_1735;
Golexanolone was well tolerated and psychometric tests improved in golexanolone and placebo groups. The effects of 21 days’ treatment with golexanolone vs. placebo on EEG and sleepiness are consistent with those observed following a single oral dose in healthy adults after allopregnanolone challenge and suggest a role for neurosteroids in HE-related sleepiness, as well as a role for golexanolone in the treatment of neurosteroid-mediated cognitive disorders.
- allopregnanolone (LJPC-0712) / La Jolla Pharma
GOLEXANOLONE EXHIBITS LITTLE GENDER DIFFERENCE IN PHARMACOKINETICS AND IS WELL TOLERATED BY PATIENTS WITH CIRRHOSIS AT PLASMA LEVELS SHOWN TO MITIGATE THE CNS EFFECTS OF ALLOPREGNANOLONE. (Hynes Convention Center, Hall B) - Sep 29, 2019 - Abstract #AASLD2019AASLD_2215;
In ongoing studies, the safety and PK characteristics of golexanolone in females are comparable to those in males. In patients with cirrhosis, golexanolone appears well tolerated at doses and systemic exposure within the range demonstrated in healthy adults to mitigate the brain inhibitory effects of the neurosteroid, allopregnanolone.