Rho-kinase inhibitor AR-12286 reportedly lowers IOP by restoring trabecular meshwork function.

Glaucoma drugs firm Aerie Pharmaceuticals raised $30 million in a Series B round of financing led by Clarus Ventures and Sofinnova Ventures. Osage University Partners and existing investors Alta Partners and TPG Biotech also participated. Aeri plans to use the new funds to continue development of its glaucoma portfolio, and in particular progress lead candidate AR-12286 into Phase III development by the end of 2011.

AR-12286 is a highly selective Rho-kinase inhibitor (ROCK) designed to lower intraocular pressure by improving outflow of fluid via the trabecular pathway and potentially restoring normal function. Aerie says this class of compounds acts directly on the trabecular meshwork (TM), which undergoes pathological changes in patients with primary open angle glaucoma (POAG). ROCK inhibitors essentially return the TM to a state that allows normal drainage of ocular fluid and thereby reduces pressure in the eye.

A Phase II study evaluating AR-12286 in patients with POAG has previously demonstrated that treatment leads to a significant reduction in intraocular pressure. Additional Phase II trials are also planned this year.

“Despite the fact that glaucoma is a progressive disease, there has not been a drug with a new mechanism of action approved in the glaucoma field since the mid-nineties,” notes Tom van Haarlem, M.D., Aerie’s president and CEO. “Patients often need several drugs to control their disease, and physicians have limited options with these older mechanisms. We believe that AR-12286’s new MOA, strong efficacy, excellent tolerability and once-daily dosing can provide real value to patients at risk of losing their vision.”

In addition to lead clinical candidate AR-12286, Aerie is progressing a preclinical program comprising a series of dual mechanism of action compounds discovered in house. The firm claims preclinical testing suggests these compounds are more effective than known drugs at lowering eye pressure. The lead compound in this program is designated AR-13324.

Aerie’s drug programs are complemented by an ocular implant technology in development to enable sustained delivery of drugs to the front of the eye.  The firm claims the platform technology is compatible with a range of both existing and novel compounds.  Lead implant product, AR-202, is a lantanoprost implant currently in late-stage preclinical testing. 

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