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- || enerisant (TS-091) / Taisho
PK/PD data, Journal: Pharmacokinetic and pharmacodynamic assessment of histamine H receptor occupancy by enerisant: a human PET study with a novel H binding ligand, [C]TASP457. (Pubmed Central) - Apr 27, 2022
P1
The preliminary time-course investigation showed persistently high brain occupancy with high doses of enerisant despite the decreasing plasma concentration of the drug. Five milligrams or less dose would be appropriate for the treatment for narcolepsy with initially high occupancy allowing for effective treatment of narcolepsy, and then the occupancy level would be expected to decrease to a level to avoid this drug's unwanted side effect of insomnia at night, although further research is warranted to confirm the statement since the expected decrease is based on the finding in one subject.
- || enerisant (TS-091) / Taisho
Clinical, Journal: Optimal dose determination of enerisant (TS-091) for patients with narcolepsy: two randomized, double-blind, placebo-controlled trials. (Pubmed Central) - Apr 12, 2022
P2
The optimal dose of enerisant could not be determined in these two studies. Although enerisant has a favorable pharmacokinetic profile, it is thought to have large interindividual variabilities in terms of efficacy and safety, suggesting the necessity of tailored dosage adjustments.
- || enerisant (TS-091) / Taisho
Clinical, PK/PD data, Journal: Drug-drug interaction potential and clinical pharmacokinetics of enerisant, a novel potent and selective histamine H receptor antagonist. (Pubmed Central) - Jun 16, 2021
The urinary excretion of enerisant within 48 h after administration was 64.5% to 89.9% of the dose, indicating that most of the absorbed enerisant was excreted in the urine without being metabolized.Based on the plasma concentrations at the estimated clinical dose, enerisant is unlikely to cause CYP-mediated, clinically relevant DDI. Although the possibility of transporter-mediated, clinically relevant DDI cannot be ruled out, there is little or no risk of side effects.
- | enerisant (TS-091) / Taisho
Preclinical, Journal: A Novel Potent and Selective Histamine H3 Receptor Antagonist Enerisant: In Vitro Profiles, In Vivo Receptor Occupancy, Wake-Promoting and Pro-cognitive Effects in Rodents. (Pubmed Central) - Dec 16, 2020
Significance Statement Enerisant is a novel histamine H3 receptor antagonist/inverse agonist that exerts wake-promoting and pro-cognitive effects in addition to increasing the release of neurotransmitters related to these pharmacological effects in rodents. Moreover, an in vivo receptor binding study revealed that the in vivo occupancy of the histamine H3 receptor required to exert the pharmacological effects of enerisant varied, and such variations in required occupancy should be taken into account when performing dose selection in clinical studies.
- || enerisant (TS-091) / Taisho
New P1 trial: Clinical Study on Histamine H3 Receptor Occupancy of TS-091 by PET Examination in Healthy Adult Subjects (clinicaltrials.gov) - Nov 17, 2020
P1, N=12, Completed, Sponsor: Taisho Pharmaceutical Co., Ltd.
- | enerisant (TS-091) / Taisho
Trial completion, Trial completion date: A Study to Evaluate the Safety and Efficacy of TS-091 in Patients With Narcolepsy (clinicaltrials.gov) - Oct 11, 2019
P2, N=53, Completed, Sponsor: Taisho Pharmaceutical Co., Ltd.
Moreover, an in vivo receptor binding study revealed that the in vivo occupancy of the histamine H3 receptor required to exert the pharmacological effects of enerisant varied, and such variations in required occupancy should be taken into account when performing dose selection in clinical studies. Active, not recruiting --> Completed | Trial completion date: Mar 2019 --> Aug 2019
- | enerisant (TS-091) / Taisho
Enrollment closed: A Study to Evaluate the Safety and Efficacy of TS-091 in Patients With Narcolepsy (clinicaltrials.gov) - Dec 10, 2018
P2, N=48, Active, not recruiting, Sponsor: Taisho Pharmaceutical Co., Ltd.
Active, not recruiting --> Completed | Trial completion date: Mar 2019 --> Aug 2019 Recruiting --> Active, not recruiting
- | enerisant (TS-091) / Taisho
Enrollment open: A Study to Evaluate the Safety and Efficacy of TS-091 in Patients With Narcolepsy (clinicaltrials.gov) - Sep 5, 2017
P2, N=48, Recruiting, Sponsor: Taisho Pharmaceutical Co., Ltd.
Recruiting --> Active, not recruiting Not yet recruiting --> Recruiting
- | enerisant (TS-091) / Taisho
New P2 trial: A Study to Evaluate the Safety and Efficacy of TS-091 in Patients With Narcolepsy (clinicaltrials.gov) - Aug 30, 2017
P2, N=48, Not yet recruiting, Sponsor: Taisho Pharmaceutical Co., Ltd.