Drug intelligence / Profile preview

SB772077B

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Intravenous, Topical (ophthalmic, Experimental)
01

Overview

SB772077B is a potent and selective small molecule **Rho-kinase (ROCK) inhibitor** developed as a vasodilator and anti-inflammatory agent. Its mechanism of action involves the inhibition of **ROCK1 and ROCK2** isoforms, with an IC50 of approximately 5.6 nM[1][2][3][7]. This inhibition leads to **decreased phosphorylation of myosin light chain (p-MLC)** and **inactivation of RhoA signaling**, resulting in enhanced aqueous outflow facility, reduction of extracellular matrix and fibrotic marker expression in human trabecular meshwork cells, vasodilation in pulmonary and systemic arteries, and lowering of intraocular pressure (IOP)[3][4][5][7]. SB772077B displays greater selectivity and potency relative to earlier ROCK inhibitors such as Y-27632 and fasudil[1][5]. It is being investigated chiefly for **glaucoma** and **pulmonary hypertension**[2][5].

Brand names
SB772077BSB-772077BSB 772077B
Other names
SB772077BSB-772077BSB 772077BSB77SB-77SB 77SB-772077-BSB772077-BSB 772077-B
02

Targets

ROCK2 (Rho-associated coiled-coil containing protein kinase 2)ROCK1 (Rho-associated coiled-coil containing protein kinase 1)

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