Table 1.
Representative agents of efferocytosis-targeted therapy
| Agents | Sub-types | Mechanisms or effects | References |
|---|---|---|---|
| Annexin A5 | Natural occurring ligands for PS | Inhibit PS-dependent phagocytic activity, produce proinflammatory mediators and not produce sufficient factors related with tissue repair. | [20] |
| Bavituximab | Antibody binding specifically to PS | [88–90] | |
| UNC2025 | Tyrosine kinase inhibitor against MerTK | Cause visual impairment, produce proinflammatory mediators and not produce sufficient factors related with tissue repair. | [91] |
| BGB324, SGI-7079, TP-0903, DAXL-88, DP3975 and NA80xl | small-molecule TKIs against Axl | Produce proinflammatory mediators and not produce sufficient factors related with tissue repair; some TKIs cause fatigue, diarrhea, hypertension, hematologic events, and palmar-plantar erythrodysesthesia syndrome. | [38, 92] |
| GL21.T | Nucleotide aptamer binding specifically to Axl | Produce proinflammatory mediators and not produce sufficient factors related with tissue repair. | [38] |
| YW327.6S2, D9 and E8 | Monoclonal antibody binding specifically to Axl | [38] | |
| Soluble Axl | Inhibiting the transmembrane Axl and Gas6 signaling | [38, 93] | |
| Celastrol, dihydroartemisinin | Natural compound inhibiting Axl | [38, 94, 95] | |
| Warfarin | Oral anticoagulant suppressing Gas6 activity | Cause hemorrhage, produce proinflammatory mediators and not produce sufficient factors related with tissue repair. | [47] |
| Small interfering RNA | Nucleotide aptamer binding specifically to MFG-E8 | Produce proinflammatory mediators and not produce sufficient factors related with tissue repair. | [96] |
| HMGB1, extracellular matrix ligands | Inhibiting αvβ3/αvβ5 integrins | [97, 98] | |
| B6H12.2, BRIC126 | Anti-CD47 antibodies | Induce the phagocytosis of live and normal cells. | [49, 99, 100] |
| ICAM-1 | Transmembrane glycoprotein inhibiting efferocytosis | Not mentioned. | [101] |
Abbreviations: PS, phosphatidylserine; TKI, tyrosine kinase inhibitor; MFG-E8, Milk fat globule epidermal growth factor-8; CD, cluster of differentiation; Gas, growth arrest-specific protein 6; ICAM-1, intercellular cell adhesion molecule-1; HMGB1, high-mobility group box 1