By inducing an inflammatory response, Demodex infestation of eyelid tissue has been implicated as a causal or exacerbating factor of meibomian gland dysfunction (MGD) and therefore represents a reasonable therapeutic target in MGD management.1 Lotilaner is a potent noncompetitive antagonist of insect and arachnid gamma-aminobutyric acid chloride channels that causes paralysis and death of Demodex mites.2 Lotilaner, 0.25%, ophthalmic solution is a recently available treatment for Demodex blepharitis, with a recommended dosage frequency of twice daily for 6 weeks.3

In the Saturn-1 and Saturn-2 pivotal trials investigating topical lotilaner, the primary end point of complete collarette cure was achieved by 44% of 209 patients receiving lotilaner in Saturn-1 vs 7% of 204 patients receiving vehicle and by 56% of 193 patients receiving lotilaner in Saturn-2 vs 12.5% of 200 patients receiving vehicle (P < .0001 for both comparisons).4,5 Statistically significant differences (P ≤ .0001) favoring lotilaner were also achieved in secondary end points analyzing rates of clinically meaningful collarette cure, mite eradication, and lid erythema cure (Table).4,5 Lotilaner was generally safe and well tolerated. Instillation site pain/burning/stinging was the most common treatment-related ocular adverse event.

Table. Results of Secondary End Points in the Saturn-1 and Saturn-2 Trials*4,5
 Saturn-1 (Pivotal Phase 2b/3)4Saturn-2 (Pivotal Phase 3)5Combined Pivotal Data

Clinically meaningful collarette cure
(grade 0 or 1)

81% vs 23%
(P < .0001)

89% vs 33%
(P < .0001)

85% vs 28%

Mite eradication

68% vs 18%
(P < .0001)

52% vs 15%
(P < .0001)

60% vs 16.5%

Lid erythema cure

19% vs. 7%
(P = .0001)

31% vs 9%
(P < .0001)

25% vs 8%

* All data for lotilaner vs vehicle

References

  1. Zhang AC, Muntz A, Wang MTM, Craig JP, Downie LE. Ocular Demodex: a systematic review of the clinical literature. Ophthalmic Physiol Opt. 2020;40(4):389-432.
  2. Gonzalez-Salinas R, Karpecki P, Yeu E, et al. Safety and efficacy of lotilaner ophthalmic solution, 0.25% for the treatment of blepharitis due to demodex infestation: a randomized, controlled, double-masked clinical trial. Cont Lens Anterior Eye. 2022;45(4):101492.
  3. Lotilaner ophthalmic solution. Package insert. US National Library of Medicine. Updated July 26, 2023. Accessed July 3, 2024. https://dailymed.nlm.nih.gov/dailymed
  4. Yeu E, Wirta DL, Karpecki P, Baba SN, Holdbrook M; Saturn I Study Group. Lotilaner ophthalmic solution, 0.25%, for the treatment of Demodex blepharitis: results of a prospective, randomized, vehicle-controlled, double-masked, pivotal trial (Saturn-1). Cornea. 2023;42(4):435-443.
  5. Gaddie IB, Donnenfeld ED, Karpecki P, et al; Saturn-2 Study Group. Lotilaner ophthalmic solution 0.25% for Demodex blepharitis: randomized, vehicle-controlled, multicenter, phase 3 trial (Saturn-2). Ophthalmology. 2023;130(10):1015-1023.

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