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Project Description

Please note that we are a research service provider, not a pharmacy or clinic, so we are unable to see patients and do not offer diagnostic and treatment services for individuals.

Small Molecule Drug Development Service

Great strides have been made in recent years in the field of ophthalmology, especially in creating small molecule drugs tailored for various eye conditions. Protheragen offers comprehensive services in developing small molecule drugs for ophthalmic diseases.

Small Molecule Drug for Ophthalmic Diseases

Small molecule drugs are medical agents of small molecular weight which interact precisely with certain cellular targets. Compared with conventional therapies, these compounds have several benefits such as better bioavailability, improved delivery to tissues, and the possibility of more localized effects. In ophthalmology, small molecules have emerged as promising candidates for the therapeutics of complex ocular diseases due to their ability to modulate important biological pathways involved in disease progression.

Fig.1 Schematic diagram of the anatomy of the eye. (Ahmed S., et al., 2023)

Small Molecule Drugs in Development

There has been a considerable improvement in the development of small-molecule drugs for ocular diseases due to progress in medicinal chemistry, pharmacology, and clinical research. For instance, the application of rho kinase inhibitors provides an excellent example, as these agents have been shown to reduce IOP by facilitating the outflow of aqueous humor through the trabecular meshwork. Further, there is considerable effort focused on the design of small-molecule inhibitors that target the complement pathway, which is an important contributor to the pathogenesis of AMD.

Table 1. Summary of small molecule drugs for ophthalmic diseases. (Cheng K. J., et al., 2020)

Drug Name	Indication	Target	R&D Status
Netarsudil	Glaucoma	Rho-associated kinase (ROCK) and norepinephrine transporter	Approved
Latanoprostene Bunod (LBN)	Glaucoma and ocular hypertension	Prostaglandin F2α analog with nitric oxide (NO) donor	Approved
Acrizanib	Wet age-related macular degeneration (AMD)	VEGFR-2 inhibitor	Phase 2
TG100801	Wet age-related macular degeneration (AMD)	VEGFR-2 inhibitor	Phase 1
Haloperidol Metabolite II Valproate Ester	Wet age-related macular degeneration (AMD)	VEGFR-2 inhibitor	Preclinical
Deguelin Analogues	Wet age-related macular degeneration (AMD)	HSP90 inhibitor	Preclinical
Fenretinide Derivatives	AMD and Stargardt disease	Retinol-binding protein 4 (RBP4) antagonist	Preclinical
Nonretinoid RBP4 Antagonists	AMD and Stargardt disease	RBP4 antagonist	Preclinical
NCX 470	Glaucoma	NO-donating bimatoprost analog	Preclinical
NCX 125	Glaucoma	NO-donating latanoprost analog	Preclinical
NCX 667	Glaucoma	NO-donating compound	Preclinical
NCX 1741	Glaucoma	NO-donating PDE5 inhibitor	Preclinical
Rosmarinic Acid	Lens transparency restoration	Potential cataract treatment	Preclinical
Emodin	Diabetic cataract	Aldose reductase inhibitor	Preclinical

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 specializes in end-to-end small molecule drug development for ophthalmic indications, offering:

Target Identification & Candidate Screening

Genomic & Proteomic Analysis: Identifying disease-relevant pathways (e.g., VEGF in AMD, ROCK in glaucoma).
High-Throughput Screening (HTS): Rapid identification of lead compounds from proprietary libraries.

Medicinal Chemistry & Lead Optimization

Structure-Activity Relationship (SAR) Studies: Enhancing potency and ocular penetration.
Prodrug Design: Improving corneal absorption.

Preclinical Development

Formulation & Delivery Optimization

Nanocarriers: Liposomes, polymeric nanoparticles for sustained release.
Ocular Inserts & Implants: Punctal plugs, biodegradable matrices.

Types of Small Molecule Drug Development

Proteolysis-Targeting Chimera Development
Encompassing expertise in linker design, E3 ligase selection, and target protein engagement to create highly specific and efficacious degraders for ophthalmic targets.

Molecular Glue Degraders Development
Protheragen's capabilities in molecular glue discovery involve sophisticated screening and rational design strategies to identify compounds with the desired degradation profiles for ophthalmic applications.

Small Molecule Drug Conjugates (SMDCs) Development
Protheragen possesses the expertise in conjugation chemistry and targeting ligand selection necessary to design and develop effective SMDCs for a range of ophthalmic indications.

Utilizing next-generation medicinal chemistry, sophisticated delivery mechanisms, and comprehensive preclinical studies, Protheragen is developing next-generation ophthalmic therapeutics with enhanced efficacy and safety profiles. If you are interested in our services, please feel free to contact us.

References

Ahmed, Sadek, Maha M. Amin, and Sinar Sayed. "Ocular drug delivery: a comprehensive review." AAPS PharmSciTech 24.2 (2023): 66.
Cheng, Kuei-Ju, et al. "Ocular disease therapeutics: design and delivery of drugs for diseases of the eye." Journal of medicinal chemistry 63.19 (2020): 10533-10593.