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Research Bibliography

Reflecting core values of scientific rigor, scientific exchange, and research transparency, Aerie Pharmaceuticals continues to publish the results of its studies in the peer review medical literature and/or present them at leading eye care congresses around the world.

Copies of papers or presentations cited below can be requested by contacting Aerie Medical Affairs.

Bibliography

Asrani S, McKee H, Scott SS, Lewis R, Kopczynski C, Heah T. Pooled Phase 3 efficacy analysis of a once-daily fixed-dose combination of netarsudil 0.02% and latanoprost 0.005% in ocular hypertension and open-angle glaucoma. Poster #2210. Presented at the 13th European Glaucoma Society Congress, Florence, Italy, May 19-22, 2018.

Bacharach J, Holland E, Sheng H, Scott BS, Lewis R, Kopczynski, Heah T. Pooled safety analysis of a once-daily fixed-dose combination of netarsudil 0.02% and latanoprost 0.005% in ocular hypertension and open-angle glaucoma. Poster #2211. Presented at the 13th European Glaucoma Society Congress, Florence, Italy, May 19-22, 2018.

Carbajal KS, Weksler M, Moore L, Ding J, Kopczynski CC, Lin C. AR-13305 enhances the efficacy of aflibercept in a mouse model of proliferative diabetic retinopathy. Poster #200-C0011. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, April 29 – May 3, 2018, Honolulu, HI.

Ding J, Foley BE, Kopczynski CC, Lin C. ROCK/PKC inhibitor AR-13305 inhibits angiogenesis and protects the barrier function of retinal pigment epithelium. Poster #205-C0016. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, April 29 – May 3, 2018, Honolulu, HI.

Glendenning A, Crews K, Sturdivant J, DeLong MA, Kopczynski C, Lin C. Sustained release, biodegradable PEA implants for intravitreal delivery of ROCK/PKC inhibitor AR-13305. Poster # 5672-A0391. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, April 29 – May 3, 2018, Honolulu, HI.

Halasz E, Sugino I, Zarbin M, Townes-Anderson E. AR-13503, a novel ROCK inhibitor, reduces rod axon retraction during retinal detachment. Abstract # 4221. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, April 29 – May 3, 2018, Honolulu, HI.

Haley J, Tully J, Yang M, Williams S, Hansen J. Development of dissolution assays for ocular implants. Poster # 5674-A0393. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, April 29 – May 3, 2018, Honolulu, HI.

Lin C, Foley BE, Carbajal KS, Kopczynski CC. Evaluation of the potential of AR-13324 and AR-13503 to induce phospholipidosis. Poster #6145-C0244. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, April 29 – May 3, 2018, Honolulu, HI.

Sandahl M, Melton D, Tully J, Yang M, Garcia A, Trevino L, Williams S. Evaluation of reproducibility and uniformity of PRINT implant manufacturing. Poster # 5671-A0390. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, April 29 – May 3, 2018, Honolulu, HI.

Tully J, Melton D, Robeson R, Yang M, Verhoeve R, Williams S. AR-1105 dexamethasone extended release and pharmacokinetics in the non-human primate. Poster # 5673-A0392. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, April 29 – May 3, 2018, Honolulu, HI.

Fechtner RD, Myers JS, Erickson K, McKee H, Scott BS, Lewis RA, Heah T, Kopczynski CC. Pooled efficacy analysis of once-daily netarsudil ophthalmic solution 0.02% in patients with ocular hypertension or open-angle glaucoma. Podium presentation at the ASCRS-ASOA Annual Meeting, April 13-17, 2018, Washington, DC.

Singh IP, Kim T, Erickson K, Sheng H, Scott BS, Lewis RA, Heah T, Kopczynski CC. Pooled safety profile of once-daily netarsudil ophthalmic solution 0.02% in patients with ocular hypertension or open-angle glaucoma. Podium presentation at the ASCRS-ASOA Annual Meeting, April 13-17, 2018, Washington, DC.

Kazemi A, McLaren JW, Kopczynski CC, Heah TG, Novack GD, Sit AJ. The effects of netarsudil ophthalmic solution on aqueous humor dynamics in a randomized study in humans. J Ocul Pharmacol Ther. 2018 Feb 22. doi: 10.1089/jop.2017.0138. [Epub ahead of print]

Serle JB, Katz LJ, McLaurin E, Heah T, Ramirez-Davis N, Usner DW, Novack GD, Kopczynski CC; ROCKET-1 and ROCKET-2 Study Groups. Two Phase 3 clinical trials comparing the safety and efficacy of netarsudil to timolol in patients with elevated intraocular pressure: Rho kinase Elevated IOP Treatment Trial 1 and 2 (ROCKET-1 and ROCKET-2). Am J Ophthalmol. 2018 Feb; 186:116-127. doi: 10.1016/j.ajo.2017.11.019. Epub 2017 Dec 1.

Lin CW, Sherman B, Moore LA, Laethem CL, Lu DW, Pattabiraman PP, Rao PV, deLong MA, Kopczynski CC. Discovery and preclinical development of netarsudil, a novel ocular hypotensive agent for the treatment of glaucoma. J Ocul Pharmacol Ther. 2018 Jan/Feb;34(1-2):40-51. doi: 10.1089/jop.2017.0023. Epub 2017 Jun 13.

Carbajal KS, Ding J, Weksler M, Moore L, Kopczynski C, Lin C. Enhancing efficacy and continuous delivery of AR-13154(S) in an animal model of proliferative diabetic retinopathy. Poster #1977-B0481. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, May 7-11, 2017, Baltimore, MD.

deLong MA, Sturdivant JM, Lichorowic CL, Lin C, Foley B, Vick K, Laethem CL, Sherman B, Heintzelman GR, Kopczynski CC. Discovery and preliminary SAR of a new class of Rho kinase inhibitors for the treatment of eye diseases. Abstract #4610. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, May 7-11, 2017, Baltimore, MD.

Khouri AS, Heah T, Kopczynski CC, Novack GD, and the ROCKET-4 Investigator Group. A double-masked, randomized, parallel study of netarsudil ophthalmic solution, 0.02% QD compared to timolol maleate ophthalmic solution, 0.5% BID in patients with elevated intraocular pressure (ROCKET-4). Presentation #2461. Podium presentation at the Association for Research in Vision and Ophthalmology Annual Meeting, May 7-11, 2017, Baltimore, MD.

Peace JH, Kopczynski CC, Heah T. Ocular hypotensive efficacy of netarsudil ophthalmic solution 0.02% over a 24-hour period: A pilot study. Presentation #2460. Podium presentation at the Association for Research in Vision and Ophthalmology Annual Meeting, May 7-11, 2017, Baltimore, MD.

Serle J. 3-month interim report of a prospective 12-month safety and efficacy study of topical PG324 (fixed combination of netarsudil 0.02% and latanoprost 0.005%) compared to the individual components in subjects with elevated intraocular pressure. Presentation #2462. Podium presentation at the Association for Research in Vision and Ophthalmology Annual Meeting, May 7-11, 2017, Baltimore, MD.

Sit AJ, Kazemi A, McLaren JW, Kopczynski C, Heah T, Novack GD. The effects of netarsudil ophthalmic solution on aqueous humor dynamics in humans. Abstract 2112-A0173. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, May 7-11, 2017, Baltimore, MD.

Asrani S, Kopczynski C, Heah T. A 3-month interim report of a prospective, double-masked, randomized, multicenter, active-controlled, parallel-group, 12-month study assessing the safety and ocular hypotensive efficacy of PG324 ophthalmic solution. Presented at the American Glaucoma Society 27th Annual Meeting, March 2-5, 2017, Coronado, CA.

Sit AJ, Kazemi A, McLaren JW, Kopczynski C, Heah T, Novack GD. Aqueous humor dynamics of netarsudil ophthalmic solution 0.02% in healthy volunteers. Presented at the American Glaucoma Society 27th Annual Meeting, March 2-5, 2017, Coronado, CA.

Ren R, Li G, Le TD, Kopczynski C, Stamer WD, Gong H. Netarsudil increases outflow facility in human eyes through multiple mechanisms. Invest Ophthalmol Vis Sci. 2016 Nov 1;57(14):6197-6209. doi: 10.1167/iovs.16-20189.

Li G, Mukherjee D, Navarro I, Ashpole NE, Sherwood JM, Chang J, Overby DR, Yuan F, Gonzalez P, Kopczynski CC, Farsiu S, Stamer WD. Visualization of conventional outflow tissue responses to netarsudil in living mouse eyes. Eur J Pharmacol. 2016 Sep 15; 787:20-31. doi: 10.1016/j.ejphar.2016.04.002. Epub 2016 Apr 13.

Shaw PX, Sang A, Wang Y, Ho D, Douglas C, Dia L, Goldberg JL. Topical administration of a Rock/Net inhibitor promotes retinal ganglion cell survival and axon regeneration after optic nerve injury. Exp Eye Res. 2017 May; 158:33-42. doi: 10.1016/j.exer.2016.07.006. Epub 2016 Jul 18.

Sturdivant JM, Royalty SM, Lin CW, Moore LA, Yingling JD, Laethem CL, Sherman B, Heintzelman GR, Kopczynski CC, deLong MA. Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma. Bioorg Med Chem Lett. 2016 May 15;26(10):2475-2480. doi: 10.1016/j.bmcl.2016.03.104. Epub 2016 Apr 1.

Kopczynski CC, Ahmed F, Bharali DJ, Torrejon KY, Lin C. Anti-fibrotic effects of AR-13324 in a 3D bioengineered human trabecular meshwork model of steroid-induced glaucoma. Presentation #D0222. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, May 1-5, 2016, Seattle, WA.

Li G, Mukherjee D, Navarro I, Ashpole NE, Sherwood JM, Chang J, Overby DR, Yuan F, Gonzalez P, Kopczynski CC, Farsiu S, Stamer WD. Visualization of tissue response to netarsudil in living mouse eyes. Presentation # 6426-D0146. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, May 1-5, 2016, Seattle, WA.

Lin C, Sturdivant JM, deLong MA, Kopczynski C. Effectiveness of AR-13154 monotherapy ad combination therapy in animal models of wet age-related macular degeneration and proliferative diabetic retinopathy. Abstract 5639/Poster D0222. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, May 1-5, 2016, Seattle, WA.

Ren R, Li G, Le TD, Kopczynski C, Stamer WD, Gong H. The mechanisms of increasing outflow facility by AR-13324M in human eyes. Abstract 6426/Poster D0146. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, May 1-5, 2016, Seattle, WA.

Goldberg J, Shaw P, Sang A, Wang Y. Topical administration of a ROCK/NET inhibitor promotes retinal ganglion cell survival and axon regeneration. Presented at the American Glaucoma Society 26th Annual Meeting, March 3-6, 2016, Fort Lauderdale, FL.

Gong H, Ren R, Li G, Kopczynski C, Stamer D. The mechanisms of increased outflow facility by AR-13324M in human eyes. Presented at the American Glaucoma Society 26th Annual Meeting, March 3-6, 2016, Fort Lauderdale, FL.

Lin C, Ahmed F, Bharali D, Torrejon K, Kopczynski C. Anti-fibrotic effects of AR-13324 in a 3D bioengineered human trabecular meshwork model. Abstract/Paper PA9. Presented at the American Glaucoma Society 26th Annual Meeting, March 3-6, 2016, Fort Lauderdale, FL.

Lewis RA, Levy B, Ramirez N, Kopczynski CC, Usner DW, Novack GD; PG324-CS201 Study Group. Fixed-dose combination of AR-13324 and latanoprost: a double-masked, 28-day, randomised, controlled study in patients with open-angle glaucoma or ocular hypertension. Br J Ophthalmol. 2016 Mar;100(3):339-44. doi: 10.1136/bjophthalmol-2015-306778. Epub 2015 Jul 24. Erratum in: Br J Ophthalmol. 2016 Jul;100(7):1016.

Levy B, Ramirez N, Novack GD, Kopczynski C. Ocular hypotensive safety and systemic absorption of AR-13324 ophthalmic solution in normal volunteers. Am J Ophthalmol. 2015 May;159(5):980-5.e1. doi: 10.1016/j.ajo.2015.01.026. Epub 2015 Jan 28.

Kiel JW, Kopczynski CC. Effect of AR-13324 on episcleral venous pressure in Dutch belted rabbits. J Ocul Pharmacol Ther. 2015 Apr;31(3):146-51. doi: 10.1089/jop.2014.0146. Epub 2015 Mar 10.

Lin C, Sturdivant JM, deLong MA, Kopczynski CC. Selective multi-kinase inhibitor of ROCK/JAK/PDGFR-β reduces laser-induced CNV in rats. Presented at the Association for Ocular Pharmacology and Therapeutics 12th Biennial International Conference, February 26-March 1, 2015, Charleston, SC.

Pattabiraman PP, Rao P, Lin C, Kopczynski C. Effects of Rho kinase inhibitor AR-13324 on actin cytoskeleton ad TGFβ2- ad CTGF-induced fibrogenic activity in human trabecular meshwork cells. Presented at the Association for Ocular Pharmacology and Therapeutics 12th Biennial International Conference, February 26-March 1, 2015, Charleston, SC.

Wang RF, Williamson JE, Kopczynski C, Serle JB. Effect of 0.04% AR-13324, a ROCK, and norepinephrine transporter inhibitor, on aqueous humor dynamics in normotensive monkey eyes. J Glaucoma. 2015 Jan;24(1):51-4. doi: 10.1097/IJG.0b013e3182952213.

Bacharach J, Dubiner HB, Levy B, Kopczynski CC, Novack GD; AR-13324-CS202 Study Group. Double-masked, randomized, dose-response study of AR-13324 versus latanoprost in patients with elevated intraocular pressure. Ophthalmology. 2015 Feb;122(2):302-7. doi: 10.1016/j.ophtha.2014.08.022. Epub 2014 Sep 27.

Weiss M, et al. Evaluation of AR-13324, a Novel Dual Mechanism Agent, in Lowering of IOP in Glaucoma and Ocular Hypertension. Abstract/Poster 754. Presented at the Annual Meeting of the Association for Research in Vision and Ophthalmology, May 5-9, 2013, Seattle, WA.

deLong MA, Yingling JD, Lin C, Sherman BW, Sturdivant JM, Heintzelman GR, Laetham CL, van Haarlem T, Kopczynski CC. Discovery and SAR of a class of ocularly-active compounds displaying a dual mechanism of activity in the treatment of glaucoma. Abstract 867/Poster A567. Presented at the Association for Research in Vision and Ophthalmology Annual Meeting, May 6-10, 2012, Fort Lauderdale, FL.