Drug intelligence / Profile preview

camostat mesylate + remdesivir

Development stage
Preclinical
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral (camostat Mesylate), Intravenous (remdesivir)
01

Overview

Camostat mesylate + remdesivir is an investigational combination of two antiviral drugs intended for the treatment of SARS-CoV-2 infection (COVID-19). Camostat mesylate is an orally available serine protease inhibitor that targets and inhibits the host cell surface enzyme TMPRSS2, thereby blocking viral entry by preventing spike protein priming and fusion, a critical step for SARS-CoV-2 and other coronaviruses. Remdesivir is a nucleotide analog antiviral agent administered intravenously; it inhibits the viral RNA-dependent RNA polymerase, resulting in the suppression of viral replication. The combination is based on the rationale that camostat mesylate disrupts cell entry while remdesivir inhibits replication after entry, providing a potential synergistic antiviral effect. Both drugs have individually been studied in COVID-19 patients; however, while remdesivir has regulatory approval for COVID-19, camostat mesylate has not shown significant clinical benefit when used as monotherapy in large randomized controlled trials. The combination remains under investigation and is not currently standard therapy.

02

Targets

RdRp (Coronavirus RNA-dependent RNA polymerase)TMPRSS2 (Transmembrane protease serine 2)TTSP (Type II transmembrane serine protease)

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