- |||||||||| Edsivo (celiprolol) / Zevra Therap
Review, Journal: Current Evidence and Future Perspectives in the Medical Management of Vascular Ehlers-Danlos Syndrome: Focus on Vascular Prevention. (Pubmed Central) - Jul 27, 2024 In particular, celiprolol, a ?1 cardio-selective blocker with a ?2-agonist vasodilator effect, has been shown to reduce rates of vascular events in patients with vEDS...Drugs targeting the extracellular matrix organization and autophagy-lysosome pathways are currently under investigation and could play a role in the future. This narrative review aims to summarize current evidence and future perspectives on vEDS medical treatment, with a specific focus on vascular prevention.
- |||||||||| pritelivir (AIC316) / AiCuris
Journal: Evaluation of the Clinical Drug-Drug Interaction Potential of Pritelivir on Transporters and CYP450 Enzymes Using a Cocktail Approach. (Pubmed Central) - Jul 3, 2024 In another trial, the substrates repaglinide (CYP2C8) and rosuvastatin (BCRP) were administered separately...The results of these trials indicated that pritelivir has no clinically relevant effect on the exposure of substrates for the intestinal uptake transporter OATP2B1 and the CYP enzymes 3A4, 2B6, 2C9, and 2C8, and has a weak inhibitory effect on the intestinal efflux transporter BCRP. In summary, the results suggest that pritelivir has a low drug-drug interaction potential.
- |||||||||| Veozah (fezolinetant) / Astellas, osanetant (ACER-801) / Sanofi, Zevra Therap, elinzanetant (NT-814) / Bayer
Review, Journal: Systematic review of neurokinin-3 receptor antagonists for the management of vasomotor symptoms of menopause. (Pubmed Central) - Mar 25, 2024 Although prevention reduces the incidence of POA, the choice of the ideal molecule remains a challenge. Because of the high-quality evidence supporting the efficacy of fezolinetant and elinzanetant, these agents may be an effective option with mild adverse events for women seeking nonhormone treatment of VMS.
- |||||||||| osanetant (ACER-801) / Sanofi, Zevra Therap
Enrollment change, Trial completion date, Trial withdrawal, Trial primary completion date: POSH-MAP: Pilot of Osanetant to Reduce Severity of Hot Flashes in Men With Adenocarcinoma of the Prostate (clinicaltrials.gov) - Feb 21, 2024 P1, N=0, Withdrawn, Because of the high-quality evidence supporting the efficacy of fezolinetant and elinzanetant, these agents may be an effective option with mild adverse events for women seeking nonhormone treatment of VMS. N=10 --> 0 | Trial completion date: Nov 2025 --> Oct 2023 | Recruiting --> Withdrawn | Trial primary completion date: Nov 2024 --> Sep 2023
- |||||||||| osanetant (ACER-801) / Sanofi, Zevra Therap
Enrollment change, Trial completion date, Trial termination, Trial primary completion date: PORT-MAP: Pilot of Osanetant to Reduce Testosterone in Men With Adenocarcinoma of the Prostate (clinicaltrials.gov) - Feb 21, 2024 P1, N=1, Terminated, N=10 --> 0 | Trial completion date: Nov 2025 --> Oct 2023 | Recruiting --> Withdrawn | Trial primary completion date: Nov 2024 --> Sep 2023 N=10 --> 1 | Trial completion date: Nov 2025 --> Nov 2023 | Recruiting --> Terminated | Trial primary completion date: Nov 2024 --> Sep 2023; Development of the drug program has been discontinued
- |||||||||| osanetant (ACER-801) / Sanofi, Acer Therap
Journal: Activation of neurokinin-III receptors modulates human atrial TASK-1 currents. (Pubmed Central) - Nov 27, 2023 Heterologously expressed human TASK-1 channels are inhibited by neurokinin-III receptor activation in a DAG dependent fashion. Patch-clamp measurements, performed on human atrial cardiomyocytes suggest that the atrial-specific effects of neurokinin-III receptor activation on cardiac excitability are predominantly mediated via TASK-1 currents.
- |||||||||| Edsivo (celiprolol) / Acer Therap
Biomarker, Clinical, Clinical guideline, Retrospective data, Review, Clinical Trial,Phase II, Journal: Celiprolol and sympatho-immune interface in COVID-19. (Pubmed Central) - Nov 6, 2023 Patch-clamp measurements, performed on human atrial cardiomyocytes suggest that the atrial-specific effects of neurokinin-III receptor activation on cardiac excitability are predominantly mediated via TASK-1 currents. No abstract available
- |||||||||| osanetant (ACER-801) / Sanofi, Zevra Therap
Enrollment closed: Dose-ranging, PK, Safety, Efficacy Study of Osanetant in Patients With Moderate/Severe VMS Associated With Menopause (clinicaltrials.gov) - Mar 17, 2023 P2a, N=56, Active, not recruiting, Active, not recruiting --> Completed Recruiting --> Active, not recruiting
- |||||||||| Edsivo (celiprolol) / Acer Therap, Visken (pindolol) / Novartis, bevantolol (SOM3355) / SOM Biotech
Journal: β-arrestin2 recruitment by β-adrenergic receptor agonists and antagonists (Pubmed Central) - Jan 4, 2023 β2-AR selective antagonists butoxamine showed β-arrestin2 recruitment at β1-AR. These results provide some clues for the potential action of β-AR drugs, and lay a foundation for the screening of β-arrestin-biased β-AR ligands.
- |||||||||| Edsivo (celiprolol) / Acer Therap
Journal: Vascular Ehlers Danlos Syndrome: Pathological Variants, Recent Discoveries, and Theoretical Approaches. (Pubmed Central) - Oct 12, 2022 Mice with vEDS traits treated with a beta-blocker celiprolol showed significant improvements in their thoracic aorta biomechanical strength...Similarly, an embryonic homeobox transcription factor Nanog upregulates the wild-type COL3A1 expression through activation of the transforming growth factor-beta pathway, which increases type III collagen synthesis. Despite numerous advancements, more studies are to be performed to incorporate these discoveries into clinical settings, and eventually, more personalized treatments can be created.
- |||||||||| Edsivo (celiprolol) / Acer Therap, Invirase (saquinavir) / Roche, Crixivan (indinavir sulfate) / Merck (MSD)
Review, Journal: Phytochemicals That Interfere With Drug Metabolism and Transport, Modifying Plasma Concentration in Humans and Animals. (Pubmed Central) - Sep 29, 2022 Interactions between Pchs and drugs affect the gene expression and enzymatic activity of CYP3A and P-gp transporter, which has an impact on their bioavailability; such that co-administration of drugs with food, beverages and food supplements can cause a subtherapeutic effect or overdose. Therefore, it is important for the clinician to consider these interactions to obtain a better therapeutic effect.
- |||||||||| osanetant (ACER-801) / Sanofi, Zevra Therap
Enrollment status, Trial completion date, Trial primary completion date: Dose-ranging, PK, Safety, Efficacy Study of Osanetant in Patients With Moderate/Severe VMS Associated With Menopause (clinicaltrials.gov) - Sep 15, 2022 P2a, N=56, Recruiting, Enrolling by invitation --> Recruiting Enrolling by invitation --> Recruiting | Trial completion date: Sep 2022 --> Jan 2023 | Trial primary completion date: Aug 2022 --> Dec 2022
- |||||||||| osanetant (SR 142801) / Sanofi, Acer Therap
Preclinical, Journal: Nk3R blockade has sex-divergent effects on memory in mice. (Pubmed Central) - Jun 20, 2022 Trial completion date: Dec 2022 --> Sep 2022 These data propose novel ideas on functional interactions between Nk3R, sex hormones, estrogen receptors, and androgen receptors in memory consolidation.
- |||||||||| SRX246 / Azevan, osanetant (SR 142801) / Sanofi, Acer Therap
Chair (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_6814; Finally, we will present data from human subjects showing that highly selective vasopressin 1A receptor antagonist SRX246 reduces anxiety but not fear-potentiated startle in male and female participants. This mini-symposium will address sex-specific effects of limbic neuropeptides in both rodents and humans and the importance of sex-specific pharmacotherapies for PTSD.
- |||||||||| SRX246 / Azevan, osanetant (SR 142801) / Sanofi, Acer Therap
The role of Angiotensin II in Fear Memory and therapeutic opportunities for PTSD (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_6803; Finally, we will present data from human subjects showing that highly selective vasopressin 1A receptor antagonist SRX246 reduces anxiety but not fear-potentiated startle in male and female participants. This mini-symposium will address sex-specific effects of limbic neuropeptides in both rodents and humans and the importance of sex-specific pharmacotherapies for PTSD.
- |||||||||| SRX246 / Azevan, osanetant (SR 142801) / Sanofi, Acer Therap
Clinical translation of oxytocin neuroscience to the treatment of anxiety and posttraumatic stress disorders (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_6802; Finally, we will present data from human subjects showing that highly selective vasopressin 1A receptor antagonist SRX246 reduces anxiety but not fear-potentiated startle in male and female participants. This mini-symposium will address sex-specific effects of limbic neuropeptides in both rodents and humans and the importance of sex-specific pharmacotherapies for PTSD.
- |||||||||| SRX246 / Azevan, osanetant (SR 142801) / Sanofi, Acer Therap
Sex-opposite effects of the neurokinin 3 receptor neuropeptide in memory consolidation (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_6800; Finally, we will present data from human subjects showing that highly selective vasopressin 1A receptor antagonist SRX246 reduces anxiety but not fear-potentiated startle in male and female participants. This mini-symposium will address sex-specific effects of limbic neuropeptides in both rodents and humans and the importance of sex-specific pharmacotherapies for PTSD.
- |||||||||| SRX246 / Azevan, osanetant (SR 142801) / Sanofi, Acer Therap
Stress-enhanced fear learning, violence, and the neuropeptide Tac2 (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_6799; Finally, we will present data from human subjects showing that highly selective vasopressin 1A receptor antagonist SRX246 reduces anxiety but not fear-potentiated startle in male and female participants. This mini-symposium will address sex-specific effects of limbic neuropeptides in both rodents and humans and the importance of sex-specific pharmacotherapies for PTSD.
- |||||||||| SRX246 / Azevan, osanetant (SR 142801) / Sanofi, Acer Therap
Co Chair (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_6798; Finally, we will present data from human subjects showing that highly selective vasopressin 1A receptor antagonist SRX246 reduces anxiety but not fear-potentiated startle in male and female participants. This mini-symposium will address sex-specific effects of limbic neuropeptides in both rodents and humans and the importance of sex-specific pharmacotherapies for PTSD.
- |||||||||| SRX246 / Azevan, osanetant (SR 142801) / Sanofi, Acer Therap
Chair (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_6797; Finally, we will present data from human subjects showing that highly selective vasopressin 1A receptor antagonist SRX246 reduces anxiety but not fear-potentiated startle in male and female participants. This mini-symposium will address sex-specific effects of limbic neuropeptides in both rodents and humans and the importance of sex-specific pharmacotherapies for PTSD.
- |||||||||| Edsivo (celiprolol) / Zevra Therap
Trial completion, Trial completion date, Trial primary completion date: CPET1: Chronic Beta-blockade and Cardiopulmonary Exercise in COPD (clinicaltrials.gov) - Jun 24, 2019 P4, N=10, Completed, The research provided estimates of DDI with ACER-801 and tamoxifen and what clinical experiments would be needed to confirm those estimates. Active, not recruiting --> Completed | Trial completion date: Aug 2019 --> Apr 2019 | Trial primary completion date: Aug 2019 --> Apr 2019
- |||||||||| Edsivo (celiprolol) / Zevra Therap
Enrollment closed: CPET1: Chronic Beta-blockade and Cardiopulmonary Exercise in COPD (clinicaltrials.gov) - Mar 27, 2019 P4, N=10, Active, not recruiting, Active, not recruiting --> Completed | Trial completion date: Aug 2019 --> Apr 2019 | Trial primary completion date: Aug 2019 --> Apr 2019 Recruiting --> Active, not recruiting
- |||||||||| Edsivo (celiprolol) / Zevra Therap
Trial completion date, Trial primary completion date: CPET1: Chronic Beta-blockade and Cardiopulmonary Exercise in COPD (clinicaltrials.gov) - Sep 17, 2018 P4, N=10, Recruiting, Recruiting --> Active, not recruiting Trial completion date: Aug 2018 --> Aug 2019 | Trial primary completion date: Aug 2018 --> Aug 2019
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