Antifungal Drug Development Service

The therapeutics of systemic and ocular fungal infections, which pose considerable risks to the general population and several medical disciplines, including ophthalmology, are crucial for public health. These infections can involve skin and mucosal candidiasis or invasive candidiasis which can result in the destruction of important organs. Protheragen provides a comprehensive range of services for the development of antifungal drugs tailored to the particular requests of our customers.

Overview of Ophthalmic Antifungal Drugs

Antifungal agents are essential in managing ocular infections that can be devastating to sight and eye health in the case of ophthalmic diseases. Ocular fungal infections that commonly tend to occur include keratomycosis, endophthalmitis, and fungal infections of the conjunctiva and cornea. Some yeasts and fungi responsible for these pathological conditions are Candida species, Aspergillus species, and Fusarium species. For ophthalmic use, effective antifungal agents that are capable of penetrating ocular tissues and achieving therapeutic concentrations with minimal systemic side effects are required.

Fig.1 New antifungal drugs and targets. (Mota Fernandes C., et al., 2021)

Antifungal Drug Development for Ophthalmic Diseases

Ocular infections are managed with many categories of antifungal agents. Use of class polyene agents such as amphotericin B which binds to ergosterol in the membrane of the fungal cell, as well as azole agents which classify as ergosterol biosynthesis inhibitors are included. Other classes that are used comprise: echinocandins which inhibit the synthesis of β-d-glucan in the cell wall of the fungus, as well as pyrimidine derivatives like flucytosine which act on the DNA and RNA synthesis of fungi. Each class has its own advantages and limitations, with varying degrees of efficacy and toxicity.

Table 1. The antifungal pipeline. (Houšť J., et al., 2020)

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

At Protheragen, we offer complete antifungal drug development services, focusing on diseases of the eye. Our capabilities include the entire scope of drug development activity from target selection to preclinical study, enabling the formulation of safe and effective antifungal drugs.

Identification of New Targets

The initial stage of antifungal drug development involves identifying novel targets that are unique to fungi and not present in human cells. This is crucial for minimizing toxicity while maximizing efficacy. Recent advancements in genomics and proteomics have enabled researchers at Protheragen to identify and validate new targets more efficiently.

Optional Targets

Ergosterol Biosynthesis	Cell Wall Synthesis	Nucleic Acid Synthesis
Mitochondrial Function	Siderophore Transport	Dihydroorotate Dehydrogenase
Glyoxylate Cycle	Calcineurin Pathway	Heat Shock Protein 90 (Hsp90)
Trehalose Pathway	Sphingolipid Synthesis	High-Osmolarity Glycerol (HOG) Pathway
Protein Kinase C (PKC) Pathway

Types of Antifungal Drugs

Protheragen excels in multiple types of antifungal drug development, each tailored to the specific needs of ophthalmic therapeutics.

• Polyene-Based Antifungal Development
• Azole-Based Antifungal Development

• Echinocandin-Based Antifungal Development
• Novel Antifungal Peptide Development

Preclinical Development

Preclinical development involves extensive in vitro and in vivo testing to evaluate the efficacy, safety, and pharmacokinetics of new antifungal compounds. This stage is critical for understanding the mechanism of action, identifying potential toxicities, and optimizing the drug's formulation.

Solutions for Ophthalmic Diseases

• Fungal Keratitis
• Endophthalmitis
• Cryptococcal Endophthalmitis
• Scleritis
• Conjunctival Sporotrichosis

• Postoperative Fungal Infections
• Orbital Aspergillosis
• Mycotic Ulcer
• Invasive Pansinusitis with Ocular Involvement

Protheragen actively seeks to progress the domain of antifungal drug development through novel research and integrated services. We are assured that our specialization in novel target identification, new compound discovery, and stringent preclinical assessments guarantees our leadership in this defining aspect of ophthalmic disease therapeutics development. If you are interested in our services, please feel free to contact us.

References

• Mota Fernandes, Caroline, et al. "The future of antifungal drug therapy: novel compounds and targets." Antimicrobial agents and chemotherapy 65.2 (2021): 10-1128.
• Houšť, Jiří, Jaroslav Spížek, and Vladimír Havlíček. "Antifungal drugs." Metabolites 10.3 (2020): 106.