INO-8875 (formerly PJ-875) is a potent and highly selective activator of the adenosine 1 (A1) receptor, a G-protein coupled receptor (GPCR). A1 receptor stimulation induces a broad range of biological responses including global suppression of metabolic activity, depression of AV nodal conduction and lowering of intraocular pressure. A number of preclinical studies in normotensive rabbits, monkeys, and cats have clearly demonstrated that application of selective A1 agonists reduces IOP. INO-8875 has exhibited promising preclinical results. INO-8875 is entering clinical development as a topical agent for treatment of elevated intraocular pressure associated with open angle glaucoma and ocular hypertension. Phase 1 studies are ongoing.