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. 2022 Sep 24;5(4):pbac024. doi: 10.1093/pcmedi/pbac024

Table 2.

Properties of small molecule inhibitors approved or evaluated in clinical trials for COVID-19 therapy: host-targeted inhibitors and immune response modulators.

Chemical structure Generic name (trade name) Code name Molecular formula Targets Effective spectrum Highest phase Corporation or trial originator
graphic file with name pbac024figu23.jpg Camostat mesylate (Foipan) FOY305 FOY-S980 C20H22N4O5. CH4O3S TMPRSS2 SARS-CoV, MERS-CoV, HCoV-229E, SARS-CoV-2 Phase III Ono Pharmaceutical
graphic file with name pbac024figu24.jpg Nafamostat mesylate (Futhan) DS-2319 FUT-175 C19H17N5O2. 2CH4O3S TMPRSS2 SARS-CoV-2, MERS-CoV Phase III Multiple originators
graphic file with name pbac024figu25.jpg Proxalutamide GT0918 C24H19F4N5O2S Host protease inhibitor (androgen receptor antagonist) SARS-CoV-2 Phase III Kintor Pharmaceutical
graphic file with name pbac024figu26.jpg Chloroquine C18H26ClN3 Endosome acidification agent HCoV-229E, HCoV-OC43, HIV, Ebola virus, SARS-CoV, MERS-CoV, SARS-CoV-2 EUA by FDA at early outbreak Multiple originators
graphic file with name pbac024figu27.jpg Hydroxychloroquine C18H26ClN3O Endosome acidification agent SARS-CoV, MERS-CoV, SARS-CoV-2 Phase IV Multiple originators
graphic file with name pbac024figu28.jpg Mefloquine C17H16F6N2O Endosome acidification agent MERS-CoV, SARS-CoV Phase II/III Multiple originators
graphic file with name pbac024figu29.jpg Apilimod STA-5326 C23H26N6O2 Host endosomal inhibitor (PIKfyve kinase inhibitor) Ebola virus, Lassa virus, Marburg virus, SARS-CoV-2 Phase II AI Therapeutics
graphic file with name pbac024figu30.jpg Dexamethasone (Hexadecadrol, Prednisolone F) AR-1105 BDI-1 ISV-305 C22H29FO5 Immune response modulator SARS-CoV-2 Phase IV Multiple originators
graphic file with name pbac024figu31.jpg Baricitinib (Olumiant) LY3009104 INCB028050 C16H17N7O2S Immune response modulator (JAK inhibitor) SARS-CoV-2 EUA in the USA Eli Lilly and Company/Incyte
graphic file with name pbac024figu32.jpg Ruxolitinib (Jakfi) INCB18424 C17H18N6 Immune response modulator (JAK inhibitor) SARS-CoV-2 Phase III Novartis/Incyte
graphic file with name pbac024figu33.jpg Tofacitinib CP-690550 C16H20N6O Immune response modulator (JAK inhibitor) SARS-CoV-2 Phase III Pfizer
graphic file with name pbac024figu34.jpg Nitazoxanide (Alinia/Colufase/Cryptaz) NT-300 NTZ PH-5776 C12H9N3O5S Immune response modulator (IFN inducer) Influenza virus, Hepatitis B, Hepatitis C, HIV, SARS-CoV, MERS-CoV, SARS-CoV-2 Phase IV Multiple originators