Targeted Therapy Development Service
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Targeted Therapy Development Service

Targeted therapy in ophthalmic disease is an advanced technique that aims to improve the effectiveness of the therapeutics by administering therapeutic agents directly to the affected tissues or cells in the eye while reducing systemic side effects. Protheragen is dedicated to advancing the field of ophthalmic targeted therapies through innovative research, advanced drug delivery systems, and comprehensive services.

Targeted Therapy for Ophthalmic Diseases

Ophthalmic diseases cover various ailments that affect the eye, its structure, and function, for instance, age-related macular degeneration (AMD), diabetic retinopathy, glaucoma, and inflammatory and infectious diseases. Targeted therapy for ophthalmic diseases is a novel development in the domain of ophthalmology guided by the local administration of the drugs to pre-defined locations in the eye. The objective of this technique is to optimize the therapeutic effect while reducing systemic adverse effects in order to improve efficacy.

Systematic evolution of ligand exponential enrichment.Fig.1 Process of systematic evolution of ligands by exponential enrichment. (Cao J., et al., 2023)

The Delivery System of Ophthalmic Disease Drugs

  • Topical Delivery
    For anterior segment disorders, eye drops, eye gels, and ointments are employed widely. At the same time, their effectiveness is hampered by swift tear turnover and insufficient posterior segment penetration.
  • Intravitreal Injections
    The most known approach for treating diseases in the posterior segment of the eye such as AMD and DR is by Directly injecting a drug into the vitreous humor of the eye. This approach provides great concentration of the drug into the retina, but it is invasive and needs to be repeated often.
  • Implants and Devices
    Sustained implantable devices like Ozurdex and Retisert enable chronic drug delivery to the posterior segment. These implants are either biodegradable or non-biodegradable and can deliver medications for several months or even years.
  • Nanoparticles and Nanomedicines
    Nano-enabled delivery systems like liposomes, micelles, and nanoparticles improve drug targeting, bioavailability, and stability. For instance, dexamethasone-loaded nanoparticles achieve prolonged drug release within the vitreous cavity.
  • Aptamer-Based Delivery
    Drugs or nanoparticles can be conjugated with aptamers to increase specificity with delivery. For instance, CD44 or nucleolin-specific aptamers can target and deliver drugs to retinal pigment epithelial cells or tumor cells.
  • Hydrogels
    Hydrogels that respond to stimuli can be injected into the eye where they gelat after injection, thus providing sustained drug release. These gels are biocompatible and can be tailored to respond to pH, temperature, and other stimuli.

Table 1. Selected ophthalmic devices/systems for controlled delivery of medicines to the anterior segment of the eye. (Barar J., et al., 2016)

Drug delivery system Sponsor/Collaborator Clinical trial description Clinical indication Phase ID
Gamunex-C    University of Utah Subconjunctival IVIg (Gamunex-C) Injection for Corneal Neovascularization and Inflammatory Conditions Corneal Neovascularization; Corneal Graft Failure; Anterior Segment Inflammation Phase 1 NCT02042027
Sirolimus National Eye Institute (NEI) Subconjunctival Sirolimus for the Therapeutics of Autoimmune Active Anterior Uveitis Anterior Uveitis - NCT00876434
L-PPDS Mati Therapeutics Inc. Comparison of Latanoprost PPDS with Timolol Maleate GFS in Subjects with Ocular Hypertension or Open-Angle Glaucoma Ocular hypertension (OH); Open-angle Glaucoma (OAG) Phase 2 NCT02014142
L-PPDS Mati Therapeutics Inc. A Safety Study of the Latanoprost Punctal Plug Delivery System (L-PPDS) in Subjects with Ocular Hypertension or Open Angle Glaucoma Glaucoma; Ocular Hypertension (OH); Open-angle Glaucoma (OAG) Phase 2 NCT00820300
Punctal plug Allergan Safety and Efficacy of Punctal Plug Insertion in Patients with Dry Eye Dry Eye Phase 4 NCT01684436

Disclaimer: Protheragen focuses on providing preclinical research service. This table is for information exchange purposes only. This table is not a treatment plan recommendation. For guidance on treatment options, please visit a regular hospital.

Our Services

Protheragen offers bespoke solutions to its clients. From novel aptamer development to drug delivery system optimization, we provide solutions that best serve your project's objectives.

Anti-VEGF Therapy

At Protheragen, we specialize in developing anti-VEGF therapies to inhibit abnormal blood vessel growth and leakage in the retina.

Anti-PDGF Therapy

We have developed aptamers like E10030 that target platelet-derived growth factor (PDGF), another angiogenic factor that interacts with VEGF.

Anti-FGF2 Therapy

Fibroblast growth factor 2 (FGF2) promotes angiogenesis and fibrosis. Our aptamers are designed to inhibit FGF2 and reduce neovascularization and fibrosis in retinal diseases.

Complement Inhibition

Complement component 5 (C5) is involved in inflammation and AMD. Our aptamers like avacincaptad pegol target C5 to reduce inflammation and geographic atrophy in AMD.

Anti-TGF-β Therapy

Transforming growth factor-beta (TGF-β) is involved in fibrosis, particularly after glaucoma filtration surgery. Our aptamers target TGF-β receptor II to prevent fibrosis and improve surgical outcomes.

Anti-Nucleolin Therapy

Nucleolin is a protein involved in cell proliferation and is targeted by our aptamers to inhibit choroidal neovascularization in AMD and tumor growth in ocular cancers.

Solutions for Ophthalmic Diseases

Protheragen's expertise in aptamer development, advanced drug delivery systems, and preclinical testing ensures that we deliver innovative and effective solutions for our clients. If you are interested in our services, please feel free to contact us.

References

  • Cao, Jiamin, Feng Zhang, and Wei Xiong. "Discovery of aptamers and the acceleration of the development of targeting research in ophthalmology." International Journal of Nanomedicine (2023): 4421-4430.
  • Barar, Jaleh, et al. "Advanced drug delivery and targeting technologies for the ocular diseases." BioImpacts: BI 6.1 (2016): 49.