Vimirogant hydrochloride (VTP-43742) is a highly potent, selective, oral RORγt inverse agonist with Ki/IC50 of 3.5/17 nM respectively. VTP-43742 exhibits >1,000-fold selectivity versus the RORα and RORβ. VTP-43742 inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. VTP-43742 inhibits the secretion of IL-17A from activated hPBMCs (IC50=18 nM) and human whole blood (IC50=192 nM). VTP-43742 shows potential for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis.
