nelotanserin (RVT-102) / Roivant 
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  • ||||||||||  nelotanserin (RVT-102) / Roivant
    Preclinical, Journal:  Nelotanserin, a selective 5-HT2A receptor inverse agonist, attenuates aspects of nicotine withdrawal but not reward in mice. (Pubmed Central) -  May 6, 2024   
    However, nelotanserin had no effect on anxiety-like behavior and failed to reduce nicotine reward as measured in the conditioned place preference test. Our results suggest that inverse agonism of the 5-HT2A receptor may be a feasible novel mechanism for smoking cessation by reducing both physical withdrawal and thermal hyperalgesia associated with nicotine abstinence but may require complementary pharmacotherapies targeting affective and reward-associated decrements to improve cessation outcomes.
  • ||||||||||  nelotanserin (RVT-102) / Roivant, Nuplazid (pimavanserin) / Acadia Pharma
    Journal:  Ligand bias and inverse agonism on 5-HT2A receptor-mediated modulation of G protein activity in post-mortem human brain. (Pubmed Central) -  Apr 22, 2024   
    The results reveal the existence of constitutively active 5-HT2A receptors in human pre-frontal cortex and demonstrate different pharmacological profiles of various 5-HT2A receptor drugs previously considered antagonists. These findings indicate that altanserin and pimavanserin possess biased inverse agonist profile towards 5-HT2A receptor activation of Gi1 proteins.
  • ||||||||||  nelotanserin (RVT-102) / Roivant
    Effect of the 5-HT2A/2C inverse agonist nelotanserin on dyskinesia in the MPTP-lesioned marmoset () -  Aug 30, 2023 - Abstract #MDSCongress2023MDS_Congress_1488;    
    These findings indicate that altanserin and pimavanserin possess biased inverse agonist profile towards 5-HT2A receptor activation of Gi1 proteins. These results provide incremental pre-clinical evidence that 5-HT antagonism is an efficacious anti-dyskinetic approach.
  • ||||||||||  Review, Journal:  Lewy Body Dementia: An Overview of Promising Therapeutics. (Pubmed Central) -  Aug 12, 2023   
    Of symptomatic therapies for psychosis recently investigated, pimavanserin shows promise in LBD, but studies of nelotanserin have been suspended. Although the discovery of novel symptomatic and disease-modifying therapeutics remains a significant challenge, recently published and upcoming trials signify promising strides toward that aim.
  • ||||||||||  Journal:  An overview of the active clinical trials for Parkinson's disease psychosis. (Pubmed Central) -  Jul 9, 2022   
    Tweetable abstract An overview of the active clinical trials for Parkinson's disease psychosis. In this article, we review the drugs currently undergoing clinical testing for Parkinson's disease psychosis and offer some perspectives on the treatment of the condition.
  • ||||||||||  nelotanserin (RVT-102) / Roivant, Nuplazid (pimavanserin) / Acadia Pharma
    [VIRTUAL] Functional selectivity of different serotonin 5-HT2A receptor antagonists in human post-mortem brain cortex (Poster Area) -  Aug 5, 2020 - Abstract #ECNP2020ECNP_915;    
    These findings also demonstrate that altanserin and pimavanserin display preferential inverse agonist effect on 5-HT2AR coupling to Gai1-proteins, with no effect on Gaq/11-proteins. If the hypothesis of an increase in 5-HT2AR pre-coupling to Gai1-proteins in schizophrenia was finally demonstrated, these two drugs would be a good starting point to develop a new generation of antipsychotic drugs, with potential improved efficacy and, perhaps, a lower adverse effect profile.
  • ||||||||||  nelotanserin (RVT-102) / Roivant, Nuplazid (pimavanserin) / Acadia Pharma
    [VIRTUAL] Functional selectivity of different serotonin 5-HT2A receptor antagonists in human post-mortem brain cortex (Room 2) -  Jul 10, 2020 - Abstract #ECNP2020ECNP_226;    
    These findings also demonstrate that altanserin and pimavanserin display preferential inhibition of 5-HT2A R coupling to Ga i1 -proteins vs canonical Ga q/11 -proteins. The information about functional selectivity in native tissue will help to develop new generation of antipsycothics, considering that the Ga i1 -protein pathway has been implicated in schizophrenia.
  • ||||||||||  nelotanserin (RVT-102) / Roivant
    Trial completion date, Trial termination, Trial primary completion date:  Open-label Study of Nelotanserin in Lewy Body Dementia With Visual Hallucinations or REM Sleep Behavior Disorder (clinicaltrials.gov) -  Mar 27, 2019   
    P2,  N=80, Terminated, 
    The information about functional selectivity in native tissue will help to develop new generation of antipsycothics, considering that the Ga i1 -protein pathway has been implicated in schizophrenia. Trial completion date: Jul 2019 --> Jan 2019 | Active, not recruiting --> Terminated | Trial primary completion date: Jul 2019 --> Jan 2019; Changes to the overall development program for the study medication
  • ||||||||||  nelotanserin (RVT-102) / Roivant
    Trial completion, P2 data, Trial completion date, Trial primary completion date:  Study Evaluating Nelotanserin for Treatment of REM Sleep Behavior Disorder in Subjects With Dementia (DLB or PDD) (clinicaltrials.gov) -  Oct 23, 2018   
    P2,  N=29, Completed, 
    Trial completion date: Jul 2019 --> Jan 2019 | Active, not recruiting --> Terminated | Trial primary completion date: Jul 2019 --> Jan 2019; Changes to the overall development program for the study medication Active, not recruiting --> Completed | Trial completion date: Aug 2018 --> May 2018 | Trial primary completion date: Aug 2018 --> May 2018
  • ||||||||||  nelotanserin (RVT-102) / Roivant
    Enrollment closed, P2 data, Enrollment change, Trial completion date, Trial primary completion date:  Study Evaluating Nelotanserin for Treatment of REM Sleep Behavior Disorder in Subjects With Dementia (DLB or PDD) (clinicaltrials.gov) -  Feb 14, 2018   
    P2,  N=29, Active, not recruiting, 
    Enrolling by invitation --> Active, not recruiting Recruiting --> Active, not recruiting | N=60 --> 29 | Trial primary completion date: Mar 2018 --> Aug 2018 | Trial completion date: Mar 2018 --> Aug 2018
  • ||||||||||  nelotanserin (RVT-102) / Roivant
    Trial completion date, Trial primary completion date:  Open-label Study of Nelotanserin in Lewy Body Dementia With Visual Hallucinations or REM Sleep Behavior Disorder (clinicaltrials.gov) -  Feb 14, 2018   
    P2,  N=80, Enrolling by invitation, 
    Recruiting --> Active, not recruiting | N=60 --> 29 | Trial primary completion date: Mar 2018 --> Aug 2018 | Trial completion date: Mar 2018 --> Aug 2018 Trial primary completion date: Jul 2018 --> Jul 2019 | Trial completion date: Jul 2018 --> Jul 2019