Safety and Efficacy of Ophthalmic Phentolamine Mesylate in Glaucoma

Placebo-controlled double-masked, multiple dose Phase 2 study in 40 patients with IOP ≥ 22 and ≤30 mmHg, evaluating ocular and systemic safety and efficacy following administration of Phentolamine mesylate 1.0% QD at 8PM to 10PM in both eyes for 14 days.

Inclusion criteria

• 18 years of age or greater
• Diagnosis of open angle glaucoma (OAG) or ocular hypertension (OHT). A reported history of untreated OHT with IOP ≥22mmHg and ≤ 30mmHg is preferred.
• Untreated or treated OAG/OHT with 2 or fewer ocular hypotensive medications.
• Untreated (post-washout) mean IOP ≥ 22mmHg and ≤30mmHg in the study eye at the Qualification Visit (8AM).
• Corrected visual acuity in each eye +1.0 logMAR or better by Early Treatment Diabetic Retinopathy Study (ETDRS) in each eye (equivalent to 20/200 or better) at the Screening Visit and Qualification Visit.
• Otherwise healthy and well-controlled subjects.
• Able and willing to give signed informed consent and follow study instructions.
• Able to self-administer study medication or to have study medication administered by a caregiver throughout the study period.

Exclusion criteria

• Closed or very narrow angles (Grade 0-1, Shaffer)
• Glaucoma: pseudo-exfoliation or pigment dispersion component
• Known hypersensitivity to any α-adrenoceptor antagonists
• Previous laser and/or non-laser glaucoma surgery or procedure in either eye
• Refractive surgery in either eye
• Ocular trauma in either eye within the 6 months prior to Screening, or ocular surgery or non-refractive laser treatment within the 3 months prior to Screening
• Recent or current evidence of ocular infection or inflammation in either eye
• Ocular medication in either eye of any kind within 30 days of Screening
• Clinically significant ocular disease in either eye
• History of diabetic retinopathy
• Contact lens wear within 3 days prior to and for the duration of the study
• Central corneal thickness in either eye >600 μm at Screening
• Any abnormality in either eye preventing reliable applanation tonometry
• Known hypersensitivity or contraindication to α- and/or β-adrenoceptor antagonists
• Clinically significant systemic disease that might interfere with the study
• Participation in any investigational study within 30 days prior to Screening
• Use of any topical or systemic adrenergic or cholinergic drugs up to 30 days prior to Screening, or during the study
• Changes in systemic medication that could have an effect on IOP within 30 days prior to Screening
• Women of childbearing potential who are pregnant, nursing, planning a pregnancy, or not using a medically acceptable form of birth control
• Resting heart rate outside the normal range (50-110 beats per minute) at Screening or Qualification Visit
• Hypertension with resting diastolic blood pressure (BP) > 105 mmHg or systolic BP > 160 mmHg at the Screening or Qualification Visit