Table 2.
The definition of molecules which are assumed to be effective in the disruption of Endocytosis Pathway
| Drug name | Category | Mechanism on COVID-19 | Preclinical Study | Human clinical studies |
|---|---|---|---|---|
| Umifenovir | Broad-spectrum antiviral (in China and Russia) | Clathrin-mediated endocytosis inhibitor | in vitro [79] | NCT04260594, NCT04286503, ChiCTR2000030254 |
| Chloroquine | Anti-malaria |
Lysosomotropic agent • Increase endosomes’ pH [25]→Protease inhibition [59] • Trap the viral receptor ACE2 within perinuclear vacuoles [72] • Clathrin-mediated endocytosis inhibitor (by reducing PICALM) [3] • Autophagy inhibitor [80] |
in vitro [72–74] | Many trials including: NCT04342650, NCT04303507, NCT04328493, NCT04333628 |
| Hydroxychloroquine | Anti-malaria | Lysosomotropic agent | in vitro [73, 74] | Many trials including: NCT04340544, NCT04328272, NCT04345692, NCT04351620, NCT04342221 |
| NH4Cl | Chemical Molecule |
Lysosomotropic agent • Trap the viral receptor ACE2 within perinuclear vacuoles |
in vitro [72] | NR |
| Bafilomycin A1 | Macrolide Antibiotic |
Lysosomotropic agent • Trap the viral receptor ACE2 within perinuclear vacuoles Protease inhibitor • Endo/lysosomal V-ATPase inhibitor |
in vitro [72] | NR |
| Dapagliflozin | Antidiabetic agent | Increase endosomes’ pH, reduce viral load | NR | NCT04350593, NCT04393246 |
| Teicoplanin | Antibiotic (miscellaneous) | Cathepsin L inhibitor | in vitro [74] | NR |
| E64d | Cysteine-class proteases inhibitor | Cathepsin B/L inhibitor | in vitro [28, 78] | NR |
NR, Not Reported; ACE2, Angiotensin-converting Enzyme-2; PICALM, Phosphatidylinositol Binding Clathrin Assembly Protein; V-ATPase inhibitor, Vacuolar-Adenosine Triphosphatase inhibitor