Eyevance’s Zerviate now available as a topical treatment for itchy eyes associated with allergic conjunctivitis.

Eyevance Pharmaceuticals launched its new topical agent Zerviate (cetirizine ophthalmic solution) 0.24% for the treatment of ocular itching associated with allergic conjunctivitis. Zerviate breaks a 10-year drought of new approvals for this indication. This novel prescription drop version of the well-known antihistamine cetirizine is formulated with “Hydrella.” The company says that this vehicle, containing two common ingredients found in tear lubricants — glycerin and hydroxypropyl methylcellulose (HPMC) — delivers the active ingredient to the eye with “optimal ocular comfort.”

As the over-the-counter drug Zyrtec, the antihistamine cetirizine is widely available and commonly used in pill form. Cetirizine is highly selective in blocking the H1 receptor, and it competitively binds to histamine receptors to reduce swelling, itching and vasodilation.^1,2 The agent has a both a strong safety record and efficacy profile, revealed in world-wide exposure to millions of patients during the past 20 years.³

“I am pleased about having topical Zerviate as the newest option for allergic conjunctivitis, as cetirizine is widely recognized for its safety and efficacy and has a rapid onset of action,” says Alice Epitropoulos, MD, clinical associate professor in the Department of Ophthalmology, Ohio State University Wexner Medical Center, and in private practice at Ophthalmic Surgeons & Consultants of Ohio and the Eye Center of Columbus. “Zerviate is friendly to the ocular surface. Lastly, Eyevance is making this affordable for patients by offering a copay savings program.”

WALLET-FRIENDLY, TOO

Eyevance is the first ophthalmic company to offer a copay savings program where if patients are covered on a commercial plan, are Medicare Part D beneficiaries where Zerviate is not covered or are paying cash, the company will “buy down” the prescription for Zerviate, according to Chief Commercial Officer Julie Speed. “The cost can be as little as $45 across the board, same for all patients. Obviously, if a patient’s copay is below $45, that is wonderful — no copay assistance is needed,” she adds.

A LOOK AT THE EVIDENCE

Robust efficacy of topical cetirizine was demonstrated in three randomized, double-masked placebo-controlled clinical trials in allergic conjunctivitis patients. Two of the trials designed to evaluate onset and duration of effect showed Zerviate was associated with statistically and clinically significant reduced ocular itching vs vehicle at 15 minutes and at 8 hours after treatment in patients with moderate and severe allergic conjunctivitis.⁴ The drop also demonstrated rapid onset of action, effectively relieving ocular itching within 3 minutes,⁴ as well as more rapid relief of ocular allergic conjunctivitis symptoms compared with systemic antihistamines.^5,6

The trials revealed Zerviate to have an excellent safety profile (ages 2 and up), and patients reported it to be “highly comfortable” on instillation.⁷ Because Zerviate is topical, systemic exposure is about 100-fold lower with the drop than with cetirizine tablets.⁷ Investigators noted that this will potentially lower the incidence of somnolence, fatigue and dry mouth, which are commonly experienced antihistamine-related systemic side effects.

“In my experience, Zerviate is quite comfortable on instillation,” notes Marguerite McDonald, MD, in practice with Ophthalmic Consultants of Long Island, Oceanside, N.Y. “It is non-blurring; in one blink, the patient can see clearly,” says Dr. McDonald, clinical professor of ophthalmology at NYU Langone Medical Center, New York, and clinical professor of ophthalmology at Tulane University Health Sciences Center, La. “Zerviate is effective and works locally — on the ocular surface — rather than systemically, thereby avoiding the potential side effects of an allergy pill. Zerviate also leaves no aftertaste.”

CONCLUSION

Eyevance wished to add an ocular antihistamine to its ocular surface and anterior segment portfolio, and it was “opportunistic to launch Zerviate based on cetirizine’s legacy of safety and efficacy and the noteworthy confidence that doctors have with this molecule; it is the leading antihistamine recommended by allergists nationwide,” says Ms. Speed.

Eye-care providers now have a fast-acting topical drug to offer allergic conjunctivitis patients suffering from problematic ocular itching. A drop form of cetirizine provides an effective and targeted approach and can reduce annoying systemic side effects such as drowsiness that often accompany oral antihistamines. Based on cetirizine’s familiarity and positive safety profile, both eye-care providers and patients can feel confident using Zerviate ophthalmic solution. OM

REFERENCES

1. Charlesworth EN, Kagey-Sobotka A, Norman PS, Lichtenstein LM. Effect of cetirizine on mast cell-mediator release and cellular traffic during the cutaneous late-phase reaction. J Allergy Clin Immunol. 1989;83:905-912.
2. Levi-Schaffer F, Eliashar R. Mast cell stabilizing properties of antihistamines. J Invest Dermatol. 2009;129:2549-2551.
3. Gomes PJ, Raval Y, Schoemmell E, Welch DL. Evaluation of the onset and duration of action of Topical AC-170 (Cetirizine 0.24%) for the prevention of allergic conjunctivitis. Poster C0010 presented at: ARVO; May 4-8, 2014; Orlando, Fla.
4. Meier EJ, Torkildsen GL, Gomes PJ, Jasek MC. Phase III trials examining the efficacy of cetirizine ophthalmic solution 0.24% compared to vehicle for the treatment of allergic conjunctivitis in the Conjunctival Allergen Challenge model. Clin Ophthalmol. 2018;12:2617-2628.
5. Spangler DL, Abelson MB, Ober A, Gotnes PJ. Randomized, double-masked comparison of olopatadine ophthalmic solution, mometasone furoate monohydrate nasal spray, and fexofenadine hydrochloride tablets using the conjunctival and nasal allergen challenge models. Clin Ther. 2003;25:2245-2267.
6. Abelson MB, Welch DL. An evaluation of onset and duration of action of patanol (olopatadine hydrochloride ophthalmic solution 0.1%) compared to Claritin (loratadine 10 mg) tablets in acute allergic conjunctivitis in the conjunctival allergen challenge model. Acta Ophthalmol Scand Suppl. 1999;230:60-63.
7. Malhotra RP, Meier EJ, Torkildsen GL, Gomes PJ, Jasek MC Safety of cetirizine ophthalmic solution 0.24% for the treatment of allergic conjunctivitis in adult and pediatric subjects. Clin Ophthalmol. 2019:13:403-413.