Delving into the Latest Updates on CIDD-0150610 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

oxamniquine derivatives(University of Texas at San Antonio/University of Texas Health Science Center San Antonio/Texas BioMedical Research Institute)

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Target

Bacterial DNA gyrase

Mechanism

Bacterial DNA gyrase inhibitors

Therapeutic Areas

Infectious DiseasesOther Diseases

Active Indication

Schistosomiasis

Inactive Indication-

Originator Organization

The University of Texas System

Active Organization

Texas Biomedical Research Institute

The University of Texas System

University of Texas Health Science Center At San Antonio

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Oxamniquine (OXA) is a prodrug activated by a sulfotransferase (SULT) that was only active against Schistosoma mansoni. We have reengineered OXA to be effective against S. haematobium and S. japonicum. Three derivatives stand out, CIDD-0066790, CIDD-0072229, and CIDD-0149830 as they kill all three major human schistosome species. However, questions remain. Is the OXA mode of action conserved in derivatives? RNA-interference experiments demonstrate that knockdown of the SmSULT, ShSULT, and SjSULT results in resistance to CIDD-0066790. Confirming that the OXA-derivative mode of action is conserved. Next is the level of expression of the schistosome SULTs in each species, as well as changes in SULT expression throughout development in S. mansoni. Using multiple tools, our data show that SmSULT has higher expression compared to ShSULT and SjSULT. Third, is the localization of SULT in the adult, multicellular eucaryotic schistosome species. We utilized fluorescence in situ hybridization and uptake of radiolabeled OXA to determine that multiple cell types throughout the adult schistosome worm express SULT. Thus, we hypothesize the ability of many cells to express the sulfotransferase accounts for the ability of the OXA derivatives to kill adult worms. Our studies demonstrate that the OXA derivatives are able to kill all three human schistosome species and thus will be a useful complement to PZQ.

100 Deals associated with CIDD-0150610

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Schistosomiasis	Preclinical	US	Texas Biomedical Research Institute	-
Schistosomiasis	Preclinical	US	The University of Texas System	-
Schistosomiasis	Preclinical	US	University of Texas Health Science Center At San Antonio	-