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OC-01 is a nasally administered formulation of varenicline, developed as a highly selective cholinergic agonist for the treatment of signs and symptoms of dry eye disease. Unlike oral varenicline (used for smoking cessation), OC-01 is delivered as a preservative-free multidose nasal spray. Its mechanism involves binding to nicotinic acetylcholine receptors in the trigeminal parasympathetic pathway within the nasal cavity, stimulating natural tear film production by activating lacrimal functional units. This results in increased basal tear secretion and improved ocular surface health. The drug was developed by Oyster Point Pharma and is marketed under the brand name Tyrvaya in the United States[1][2][7]. Clinical trials have also explored its use for neurotrophic keratopathy[5]. Varenicline acts as a partial agonist at α4β2 and α4α6β2 nicotinic acetylcholine receptors, moderate agonist at α3β4 and α3α5β4 receptors, and full agonist at α7 receptor[2].
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