A Phase IIa, Multicenter, Randomized, Controlled, Open Label Study to Evaluate the Efficacy of SENS-401 to Prevent the Ototoxicity Induced by Cisplatin in Adult Subjects With a Neoplastic Disease

This study is intended to evaluate the ability of SENS-401 to prevent the ototoxicity induced by cisplatin in subjects with a neoplastic disease. It is a multicenter, randomized, controlled, two-arm, open-label efficacy and safety study in adults with neoplastic disease requiring treatment with cisplatin as part of the chemotherapy protocol plan.

Start Date30 Dec 2022

Sponsor / Collaborator

Sensorion SA

NCT05258773 / CompletedPhase 2

A Phase IIa, Multicenter, Randomized, Controlled, Open-label Study to Evaluate the Presence of SENS-401 in the Perilymph After 7 Days of Repeated Oral Administration in Adult Participants Scheduled for Cochlear Implantation

The aim of this study is to detect the presence of SENS-401 in the perilymph of participants undergoing cochlear implant surgery after 7 days of oral administration of SENS-401.

Start Date10 Aug 2022

Sponsor / Collaborator

Sensorion SA

100 Clinical Results associated with H4 receptor x 5-HT3 receptor

100 Translational Medicine associated with H4 receptor x 5-HT3 receptor

0 Patents (Medical) associated with H4 receptor x 5-HT3 receptor

Literatures (Medical) associated with H4 receptor x 5-HT3 receptor

26 May 2015·Journal of Chemical Information and ModelingQ2 · CHEMISTRY

Combinatorial Consensus Scoring for Ligand-Based Virtual Fragment Screening: A Comparative Case Study for Serotonin 5-HT₃A, Histamine H₁, and Histamine H₄Receptors

Q2 · CHEMISTRY

Article

Author: Leurs, Rob ; Vischer, Henry F. ; de Esch, Iwan J. P. ; Schultes, Sabine ; Nijmeijer, Saskia ; Kooistra, Albert J. ; de Graaf, Chris ; Haaksma, Eric E. J.

In the current study we have evaluated the applicability of ligand-based virtual screening (LBVS) methods for the identification of small fragment-like biologically active molecules using different similarity descriptors and different consensus scoring approaches. For this purpose, we have evaluated the performance of 14 chemical similarity descriptors in retrospective virtual screening studies to discriminate fragment-like ligands of three membrane-bound receptors from fragments that are experimentally determined to have no affinity for these proteins (true inactives). We used a complete fragment affinity data set of experimentally determined ligands and inactives for two G protein-coupled receptors (GPCRs), the histamine H1 receptor (H1R) and the histamine H4 receptor (H4R), and one ligand-gated ion channel (LGIC), the serotonin receptor (5-HT3AR), to validate our retrospective virtual screening studies. We have exhaustively tested consensus scoring strategies that combine the results of multiple actives (group fusion) or combine different similarity descriptors (similarity fusion), and for the first time systematically evaluated different combinations of group fusion and similarity fusion approaches. Our studies show that for these three case study protein targets both consensus scoring approaches can increase virtual screening enrichments compared to single chemical similarity search methods. Our cheminformatics analyses recommend to use a combination of both group fusion and similarity fusion for prospective ligand-based virtual fragment screening.

01 Apr 2013·Drug Discovery TodayQ2 · MEDICINE

Small and colorful stones make beautiful mosaics: fragment-based chemogenomics

Q2 · MEDICINE

Article

Author: Rob Leurs ; Paul J. England ; Jacqueline E. van Muijlwijk-Koezen ; Mark H.P. Verheij ; Chris de Graaf ; Gerdien E. de Kloe ; Henry F. Vischer ; Albert J. Kooistra ; Martien Kuijer ; Iwan J.P. de Esch ; Saskia Nijmeijer

Smaller stones with a wide variety of colors make a higher resolution mosaic. In much the same way, smaller chemical entities that are structurally diverse are better able to interrogate protein binding sites. This feature article describes the construction of a diverse fragment library and an analysis of the screening of six representative protein targets belonging to three diverse target classes (G protein-coupled receptors ADRB2, H1R, H3R, and H4R, the ligand-gated ion channel 5-HT3R, and the kinase PKA) using chemogenomics approaches. The integration of experimentally determined bioaffinity profiles across related and unrelated protein targets and chemogenomics analysis of fragment binding and protein structure allow the identification of: (i) unexpected similarities and differences in ligand binding properties, and (ii) subtle ligand affinity and selectivity cliffs. With a wealth of fragment screening data being generated in industry and academia, such approaches will contribute to a more detailed structural understanding of ligand-protein interactions.

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