Grandpharma (00512) announced that its innovative ophthalmic drug GPN01768 has received marketing approval from the Macao Special Administrative Region Government's Drug Regulatory Authority, representing a significant advancement in the company's ophthalmology pipeline. The approval positions the Hong Kong-listed pharmaceutical company to address a substantial unmet medical need in the Greater China region.
Novel Mechanism Targets Demodex Mites
GPN01768, also known as TP-03 or Loteprednol Etabonate Eye Drops 0.25%, functions as a selective non-competitive antagonist of the γ-aminobutyric acid-gated chloride channel (GABA-Cl) in insects and arachnids. The drug paralyzes and kills Demodex mites by selectively inhibiting GABA-Cl within the parasites, directly addressing the underlying cause of Demodex blepharitis.
The formulation's high lipophilicity enhances absorption in the lipid-rich environment of eyelash follicles where Demodex mites reside, optimizing therapeutic efficacy at the site of infection.
Proven Commercial Success in U.S. Market
Originally developed by Tarsus Pharmaceuticals, GPN01768 became the first and only FDA-approved treatment for Demodex blepharitis. The drug demonstrated strong commercial performance in 2024, generating approximately $180 million in U.S. revenue with about 163,000 bottles sold. First quarter 2025 results showed continued momentum with $78.3 million in revenue, representing an 18% increase compared to the fourth quarter of 2024.
Addressing Significant Unmet Medical Need
Demodex blepharitis affects more than two-thirds of all blepharitis cases and represents a chronic inflammatory condition caused by Demodex mite infection of the eyelid margins. The disease primarily impacts eyelid skin, eyelash follicles, and meibomian glands, presenting with symptoms including eyelid itching, foreign body sensation, dryness, eyelid margin congestion, and characteristic sleeve-like secretions at the eyelash base.
Currently, over 40 million patients in China suffer from Demodex blepharitis, with no targeted therapies available in the market. This creates an urgent clinical need for effective treatment options that directly address the parasitic cause of the condition.
Expanded Therapeutic Potential
Beyond Demodex blepharitis, the drug shows promise for treating meibomian gland dysfunction caused by Demodex mites. This condition affects over 70 million patients in China and can lead to permanent tear film changes and progressive gland function loss if left untreated. Phase II clinical studies in the United States for this indication have shown positive topline results.
Strategic Partnership and Regional Expansion
In March 2024, Grandpharma secured exclusive development, production, and commercialization rights for GPN01768 in Greater China through a strategic cooperation agreement with Tarsus Pharmaceuticals. The partnership covers mainland China, Hong Kong, Macao, and Taiwan for both Demodex blepharitis and meibomian gland dysfunction indications.
The company submitted a new drug application to China's National Medical Products Administration in December 2024, which has been accepted for review. The Macao approval is expected to facilitate regulatory pathways in the Guangdong-Hong Kong-Macao Greater Bay Area and support eventual mainland China market entry.
Comprehensive Ophthalmology Pipeline
Grandpharma has positioned ophthalmology as a key strategic focus, developing a specialized portfolio targeting multiple conditions including myopia, dry eye, pterygium, and post-operative inflammation. The company's pipeline includes several innovative products expected to reach market approval within the next three years.
Notable pipeline assets include varenicline nasal spray for dry eye treatment, which received approval in November 2024 and is already being sold in the Greater Bay Area, and hormone nano-suspension eye drops for anti-inflammatory applications, which completed Phase III clinical endpoints in November 2024.
