| Toxin/Therapeutic target | Type of inhibitor and specifications | Potential mechanism of action | Phase of development | Ref |
| α-hemolysin | Anti-Hla MAb MAbs 7B8 & 1A9 | Antagonizes the toxin activity and block the formation of α-hemolysin oligomer on the target | Mice pneumonia model | [44] |
| Anti-Hla MAb High affinity MAb 2A3.1 | Inhibits toxin mediated cell lysis by blocking the formation of toxin heptamers on erythrocyte membranes | Independent animal models, S.aureus mouse dermonecrotic model and pneumonia model | [45] | |
| MAb MAb LTM14 | Prevents the binding of toxin to the plasma membrane of susceptible host cells | Mice pneumonia, skin and bacteremia models | [47] | |
| Chemical compound ANBOβCD (β-cyclodextrin derivatives) | Blocks the trans membrane pores and prevents the ion leakage through the pores | Mice pneumonia model | [49] | |
| Chemical compound Isatin-Schiff copper (II) complexes | Prevents the formation of ion channels by obstructing the constriction region of the hemolysin channel | In vitro assays | [52] | |
| Chemical compound ADAM10 inhibitor (GI254023X) | Inhibits binding of α-hemolysin to its host receptor (ADAM10) | Mice model of recurrent skin and soft tissue infection | [57] | |
| Natural compound Oroxylin A, Oroxin A and Oroxin B | Binds to the stem region of α-hemolysin and prevents conformational transition of toxin from monomer to oligomer | In vitro assays | [51] | |
| Natural compound Morin hydrate | Inhibits self-assembly of the heptameric trans membrane pore of α-hemolysin | Mice pneumonia model | [53] | |
| Natural compound Curcumin | Inhibits the pore forming | Mice pneumonia model | [58] | |
| Natural compound Baicalin | Interrupts the formation of heptamer | In vivo assays | [59] |