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Last update 08 May 2025

Veralipride

Last update 08 May 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Veralipride (INN), Agradil

+ [1]

Target-

Action-

Mechanism-

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Active Indication-

Inactive Indication-

Originator Organization-

Active Organization-

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First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC17H25N3O5S

InChIKeyRYJXBGGBZJGVQF-UHFFFAOYSA-N

CAS Registry66644-81-3

100 Clinical Results associated with Veralipride

100 Translational Medicine associated with Veralipride

100 Patents (Medical) associated with Veralipride

135

Literatures (Medical) associated with Veralipride

24 Mar 2025·Expert Opinion on Pharmacotherapy

Polypharmacology of carbonic anhydrase inhibitors and activators

Review

Author: Bonardi, Alessandro ; Supuran, Claudiu T.

INTRODUCTIONCarbonic anhydrases (CAs) are enzymes involved in many physiologic and pathological processes connected with a diversity of conditions. Many of their inhibitors are used clinically for the management of glaucoma, epilepsy, obesity, and cancer. Some of these compounds also show significant polypharmacological effects. CA activators (CAAs) are not in clinical use.AREAS COVEREDPubMed and ScienceDirect databases were searched for articles published over the past 20 years. Several antiepileptics (topiramate, zonisamide, lacosamide, and levetiracetam), some atypical antipsychotics (sulpiride, veralipride), celecoxib, polmacoxib, pazopanib, the antiulcer agent famotidine, and compounds in clinical trials (epacadostat and PCI-27483) as antitumor agents significantly inhibit several CA isoforms of the 15 human ones, apart their action on several other targets. The possible role of CA inhibition in the therapeutic effects of these drugs, their side effects, and the possibility to use this information for drug design are discussed. CAAs belonging to a variety of aminergic classes (histaminergic, dopaminergic, and serotoninergic) are also discussed.EXPERT OPINIONPolypharmacology involving CA inhibitors/CAAs is understood from the chemical, structural, and pharmacological viewpoints. The many other drug targets with which these modulators of activity interact allow for de novo design of such agents for the management of multifactorial conditions in need of innovative drugs.

01 Nov 2024·Journal of Biological Chemistry

Comprehensive characterization of the OCT1 phenylalanine-244-alanine substitution reveals highly substrate-dependent effects on transporter function

Article

Author: Schröder, Sophie ; Brockmöller, Jürgen ; Gebauer, Lukas ; Wittern, Carla Isabel ; Jensen, Ole

Organic cation transporters (OCTs) can transport structurally highly diverse substrates. The molecular basis of this extensive polyspecificity has been further elucidated by cryo-EM. Apparently, in addition to negatively charged amino acids, aromatic residues may contribute to substrate binding and substrate selectivity. In this study, we provide a comprehensive characterization of phenylalanine 244 in OCT1 function. We analyzed the uptake of 144 OCT1 substrates for the phenylalanine 244 to alanine substitution compared to WTOCT1. This substitution had highly substrate-specific effects ranging from transport reduced to 10% of WT activity up to 8-fold increased transport rates. Four percent of substrates showed strongly increased uptake (>200% of WT) whereas 39% showed strongly reduced transport (<50% of WT). Particularly with larger, more hydrophobic, and more aromatic substrates, the Phe244Ala substitution resulted in higher transport rates and lower inhibition of the transporter. In contrast, substrates with a lower molecular weight and less aromatic rings showed generally decreased uptake rates. A comparison of our data to available transport kinetic data demonstrates that generally, high-affinity low-capacity substrates show increased uptake by the Phe244Ala substitution, whereas low-affinity high-capacity substrates are characterized by reduced transport rates. Altogether, our study provides the first comprehensive characterization of the functional role of an aromatic amino acid within the substrate translocation pathway of OCT1. The pleiotropic function further highlights that phenylalanine 244 interacts in a highly specific manner with OCT1 substrates and inhibitors.

01 Oct 2024·iScience

Few-shot meta-learning applied to whole brain activity maps improves systems neuropharmacology and drug discovery

Article

Author: Cheng, Shuk Han ; Zeng, Shangzhi ; Wang, Xin ; Zhang, Wenchong ; Zhang, Jin ; Liu, Zhen ; Luo, Xuan ; Haggarty, Stephen J ; Li, Honglin ; Haggarty, Stephen J. ; Shi, Peng ; Ding, Yanyun ; Cao, Yi

In this study, we present an approach to neuropharmacological research by integrating few-shot meta-learning algorithms with brain activity mapping (BAMing) to enhance the discovery of central nervous system (CNS) therapeutics. By utilizing patterns from previously validated CNS drugs, our approach facilitates the rapid identification and prediction of potential drug candidates from limited datasets, thereby accelerating the drug discovery process. The application of few-shot meta-learning algorithms allows us to adeptly navigate the challenges of limited sample sizes prevalent in neuropharmacology. The study reveals that our meta-learning-based convolutional neural network (Meta-CNN) models demonstrate enhanced stability and improved prediction accuracy over traditional machine-learning methods. Moreover, our BAM library proves instrumental in classifying CNS drugs and aiding in pharmaceutical repurposing and repositioning. Overall, this research not only demonstrates the effectiveness in overcoming data limitations but also highlights the significant potential of combining BAM with advanced meta-learning techniques in CNS drug discovery.

100 Deals associated with Veralipride

External Link

KEGG	Wiki	ATC	Drug Bank
D07311	Veralipride	N05AL06	DB13523

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