Delving into the Latest Updates on DTP-338 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CAIX

Mechanism

CAIX inhibitors(Carbonic anhydrase IX inhibitors)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

Ecole Nationale Supérieure de Chimie de Montpellier

Active Organization-

Inactive Organization

Ecole Nationale Supérieure de Chimie de Montpellier

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Carbonic anhydrase (CA) IX is a hypoxia inducible enzyme that is highly expressed in solid tumours. Therefore, it has been considered as an anticancer target using specific chemical inhibitors. The nitroimidazoles DTP338 and DTP348 have been shown to inhibit CA IX in nanomolar range in vitro and reduce extracellular acidification in hypoxia, and impair tumour growth. We screened these compounds for toxicity using zebrafish embryos and measured their in vivo effects on human CA IX in Xenopus oocytes. In the toxicity screening, the LD₅₀ for both compounds was 3.5 mM. Neither compound showed apparent toxicity below 300 µM concentration. Above this concentration, both compounds altered the movement of zebrafish larvae. The IC₅₀ was 0.14 ± 0.02 µM for DTP338 and 19.26 ± 1.97 µM for DTP348, suggesting that these compounds efficiently inhibit CA IX in vivo. Our results suggest that these compounds can be developed as drugs for cancer therapy.

100 Deals associated with DTP-338

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