Drug intelligence / Profile preview

chloroquine diphosphate

Development stage
Approved
Lead developer
Fundação de Medicina Tropical Dr. Heitor Vieira Dourado
Modality
Small Molecules
Administration
Oral
01

Overview

Chloroquine diphosphate is a small molecule aminoquinoline traditionally used as an antimalarial and for certain autoimmune conditions. During the COVID-19 pandemic, it was investigated by the Fundação de Medicina Tropical Dr. Heitor Vieira Dourado in Brazil as a potential antiviral treatment for SARS-CoV-2. The mechanism of action involves increasing endosomal pH, which interferes with viral fusion, and potentially inhibiting the glycosylation of the SARS-CoV-2 cellular receptor, ACE2. In the CloroCovid-19 Phase IIb trial, the drug was evaluated at high and low dosages in hospitalized patients with severe respiratory symptoms. However, the high-dosage arm was prematurely halted due to safety concerns, including QTc interval prolongation and increased mortality.

Other names
chloroquineCQ
02

Targets

TLR9 (Toll-like receptor 9)DNABiological membraneHemeACE2 (Angiotensin-converting enzyme 2)TLR7 (Toll-like receptor 7)

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