Table 3.

Conventional therapeutic strategies for regulating the NLRP3 inflammasome.

Medication	Application in disease therapy	Mechanism	Stage	Reference
anakinra	CAPS and rheumatoid arthritis	IL-1R antagonist	Clinical trial	(86)
Canakinumab	CAPS, atherosclerotic diseases, arthritis and gout	IL-1β-neutralizing antibody		(86)
rilonacept	CAPS	decoy receptor that binds both IL-1β and IL-1α		(89)
Tranilast	allergy, asthma and hypertrophic scars	binds the NACHT domain of NLRP3, affects the oligomerization (without affecting the ATPase activity)		(20)
VX-740 and VX-765	murine osteoarthritis, delayed-type hypersensitivity	reversible caspase-1 inhibitor	Pre-clinical	(20, 86)
Glyburide	efficiently prevent endotoxic-shock-induced lethality	mechanism unknown, though functions downstream of the P2X7 receptor and upstream of NLRP3		(90)
MCC950	CAPS and EAE	blocks ASC oligomerization; directly binds to the NACHT domain and changes NLRP3 conformation		(86, 90–92)
BHB	Muckle–Wells syndrome, familial cold autoinflammatory syndrome and urate crystal–induced peritonitis	preventing potassium efflux and reducing ASC oligomerization and speck formation		(90, 93)
JC171	delayed the progression and reduced the severity of multiple sclerosis	interfering interaction with ASC		(86)
CY-09	CAPS and type 2 diabetes	directly binds to NLRP3 NACHT domain and inhibits NLRP3 ATPase activity		(83)
OLT1177	degenerative arthritis	directly binds to NLRP3 and inhibits ATPase activity		(94)
ibrutinib	ischemic brain injury, metabolic inflammation and SCD	a BTK inhibitor, suppresses NLRP3 activation and IL-1β release		(95–97)
Disulfiram	LPS-induced sepsis	blocking GSDMD pore formation		(98)

CAPS, cryopyrin-associated periodic syndromes; VX-740, Pralnacasan; VX-765, Belnacasan; MCC950, CP-456773; EAE, experimental autoimmune encephalitis; BHB, β-hydroxybutyrate; SCD, sickle cell disease; BTK, Bruton tyrosine kinase.