REDWOOD CITY, Calif.–(BUSINESS WIRE)–Graybug Vision, Inc., a clinical stage pharmaceutical company developing potentially transformative long-acting therapies for ocular diseases, including wet age-related macular degeneration (wet AMD), diabetic macular edema (DME), retinal vein occlusion (RVO), and primary open angle glaucoma (POAG), today announced the initiation of its Phase 2b study (ALTISSIMO) with GB-102 in patients with wet AMD.

Graybug Vision initiates Phase 2b study (ALTISSIMO) with GB-102 in patients with wet AMD, a pan-VEGF receptor inhibitor and potential twice-per-year therapy. GB-102 is Graybug’s microparticle depot formulation of sunitinib malate for IVT injection.

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AMD is the world’s leading cause of blindness among the elderly. While currently available anti-Vascular Endothelial Growth Factor agents (VEGF) have revolutionized care in patients with wet AMD, the need for frequent intravitreal (IVT) injections is burdensome for patients, their caregivers, and treating physicians.

GB-102, a pan-VEGF receptor inhibitor and potential twice-per-year therapy, is targeted to reduce the need for frequent IVT injections in retinal diseases, including wet AMD, DME, and RVO. GB-102 seeks to reduce the significant treatment burden and sub-optimal visual outcomes experienced in real-world practice due to the challenge patients face in visiting the retinal specialist several times a year for needed injections and eye examinations.

ALTISSIMO is a 12-month, 3-arm, randomized controlled study evaluating two dose levels of GB-102 (1 mg and 2 mg) administered every six months compared to aflibercept (2 mg) administered every two months in patients with wet AMD. The study will enroll 160 patients at more than 100 clinical centers in the United States. For more information, please refer to: https://clinicaltrials.gov/ct2/show/NCT03953079.

“Retinal specialists around the world are seeking longer lasting treatments to help better manage the growing number of patients presenting with wet AMD and other conditions,” said Arshad Khanani, M.D., M.A., Director of Clinical Research at Sierra Eye Associates, Reno, Nev., and clinical investigator for the ALTISSIMO study. “The ability to potentially offer a twice-per-year therapy using a simple intravitreal injection would be a significant advancement for ophthalmologists and their patients.”

Graybug Vision completed a Phase 1/2a study (ADAGIO) of GB-102 in the first quarter of 2019 which met its primary endpoint of safety and tolerability, and provided evidence of a durable biological signal of six months or longer from a single IVT injection in wet AMD patients. GB-102 is also being evaluated in an ongoing Phase 2a study in patients with macular edema secondary to DME or RVO.

About GB-102

GB-102 is Graybug Vision’s microparticle depot formulation of sunitinib malate for intravitreal (IVT) injection. The formulation consists of microparticles made from poly-lactic-co-glycolic acid (PLGA) combined with the company’s proprietary surface treatment designed to eliminate inflammation typically associated with ocular administration of PLGA. The surface treatment facilitates microparticle aggregation upon IVT injection to form a depot in the inferior vitreous. After IVT injection, the microparticles gradually release sunitinib malate and biodegrade into lactic and glycolic acid which are naturally cleared from the body.

Sunitinib malate, a small molecule receptor tyrosine kinase inhibitor, is a potent inhibitor of VEGFR-1, -2, and -3, receptors known to play an influential role in the development and progression of wet AMD.

About the Phase 1/2a ADAGIO Study and Phase 2a Macular Edema Study

The ADAGIO clinical trial was an open-label, single dose study with 32 patients from eight centers located in the United States, completed in January 2019. Patients enrolled in the study were previously treated with at least three prior IVT injections of an anti-VEGF agent (aflibercept, bevacizumab or ranibizumab). They received a single intravitreal dose of GB-102 (0.25, 0.5, 1, or 2 mg) in escalating dose cohorts with eight patients in each cohort who were followed monthly for eight consecutive months. Depending on the dosages, between 50 and 88 percent of patients required no additional IVT injections of any anti-VEGF for six months after a single administration of GB-102.

A Phase 2a study of GB-102 in patients with macular edema secondary of DME and RVO was initiated in September 2019 and will enroll 20 patients from five centers in the United States. Eligible patients will receive a single IVT injection of either 1 or 2 mg GB-102 and will be followed for six consecutive months. The primary objective is to evaluate the safety, tolerability, and pharmacodynamic response. For more information, please refer to: https://clinicaltrials.gov/ct2/show/NCT04085341.

About Wet Age-related Macular Degeneration (wet AMD)

Wet AMD is the leading cause of blindness in the developed world in individuals aged 50 years or older. It is caused by the formation of abnormal and leaky new blood vessels behind the retina, termed choroidal neovascularization. The leakage of fluid and protein from the vessels causes retinal degeneration and leads to severe and rapid loss of vision. According to the National Eye Institute, the prevalence of wet AMD among adults 40 years or older in the United States alone is estimated at 1.75 million people. In addition, an estimated 20 million adults are affected by wet AMD worldwide.

About Diabetic Macular Edema (DME)

DME is caused by a complication of diabetes called diabetic retinopathy (DR) and is a leading cause of irreversible blindness in individuals 50 years and younger. Diabetes can lead to abnormal retinal blood vessels that can leak fluid causing swelling of the retina (DME) and subsequent vision loss. Of an estimated 285 million people with diabetes worldwide, approximately one third are impacted by vision-threatening DME. These estimates are expected to rise further due to the increasing prevalence of diabetes, aging of the population and increasing life expectancy of those with diabetes.

About Retinal Vein Occlusion (RVO)

RVO is a condition in which the main vein or its branches that drains blood from the retina closes off partially or completely. Blockage of the blood vessels can lead to swelling of the retina (macular edema) leading to vision loss. The incidence of RVO is estimated at 180,000 eyes per year in the United States, while branched blockages account for nearly 80 percent. An estimated 16 million adults are affected by RVO worldwide.

About Graybug Vision

Graybug Vision is a clinical stage pharmaceutical company developing novel products for the treatment of ocular diseases. The company’s proprietary injectable products are designed to enable less frequent administration to reduce the burden of treatment for patients and their treating physicians. The company’s lead clinical-stage injectable product, GB-102, has the potential to achieve six-month dosing in the treatment of retinal diseases, such as wet AMD, DME and RVO. GB-401 has the potential to achieve four to six-month dosing in the treatment of elevated intraocular pressure (IOP) associated with POAG, a sight-threatening condition that affects over 30 million people worldwide. For more information, please visit www.graybug.com.