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 |
---|---|---|---|---|---|---|---|
![]() |
Camostat mesylate (Foipan) | FOY305 FOY-S980 | C20H22N4O5. CH4O3S | TMPRSS2 | SARS-CoV, MERS-CoV, HCoV-229E, SARS-CoV-2 | Phase III | Ono Pharmaceutical |
![]() |
Nafamostat mesylate (Futhan) | DS-2319 FUT-175 | C19H17N5O2. 2CH4O3S | TMPRSS2 | SARS-CoV-2, MERS-CoV | Phase III | Multiple originators |
![]() |
Proxalutamide | GT0918 | C24H19F4N5O2S | Host protease inhibitor (androgen receptor antagonist) | SARS-CoV-2 | Phase III | Kintor Pharmaceutical |
![]() |
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 |
![]() |
Hydroxychloroquine | – | C18H26ClN3O | Endosome acidification agent | SARS-CoV, MERS-CoV, SARS-CoV-2 | Phase IV | Multiple originators |
![]() |
Mefloquine | – | C17H16F6N2O | Endosome acidification agent | MERS-CoV, SARS-CoV | Phase II/III | Multiple originators |
![]() |
Apilimod | STA-5326 | C23H26N6O2 | Host endosomal inhibitor (PIKfyve kinase inhibitor) | Ebola virus, Lassa virus, Marburg virus, SARS-CoV-2 | Phase II | AI Therapeutics |
![]() |
Dexamethasone (Hexadecadrol, Prednisolone F) | AR-1105 BDI-1 ISV-305 | C22H29FO5 | Immune response modulator | SARS-CoV-2 | Phase IV | Multiple originators |
![]() |
Baricitinib (Olumiant) | LY3009104 INCB028050 | C16H17N7O2S | Immune response modulator (JAK inhibitor) | SARS-CoV-2 | EUA in the USA | Eli Lilly and Company/Incyte |
![]() |
Ruxolitinib (Jakfi) | INCB18424 | C17H18N6 | Immune response modulator (JAK inhibitor) | SARS-CoV-2 | Phase III | Novartis/Incyte |
![]() |
Tofacitinib | CP-690550 | C16H20N6O | Immune response modulator (JAK inhibitor) | SARS-CoV-2 | Phase III | Pfizer |
![]() |
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 |