Zapnometinib

Zapnometinib (ATR-002) is an oral, non-ATP-competitive, small-molecule inhibitor of MEK1 and MEK2 with both antiviral and immunomodulatory properties. It is a major active metabolite of PD184352 (CI-1040) and has demonstrated superior in vivo antiviral effects against influenza virus compared to its parent compound. Zapnometinib targets the Raf/MEK/ERK signaling pathway, which is essential for the replication of various RNA viruses including influenza virus and SARS-CoV-2. By inhibiting MEK1/2, zapnometinib prevents export of viral ribonucleoproteins from the nucleus to the cytoplasm in infected cells, thereby hindering formation of new viral particles and reducing viral load. Additionally, it downregulates virus-induced expression of pro-inflammatory cytokines and chemokines that contribute to hyperinflammatory responses such as cytokine storms seen in severe COVID-19 cases. The drug has completed Phase 1 clinical trials demonstrating safety and tolerability in healthy volunteers, with ongoing development for respiratory viral infections including COVID-19[1][2][3][4][5][6][7].

Other names

PD184352 metabolitePD-184352 metabolitePD 184352 metabolite