Oteseconazole, a novel

tetrazole A tetrazole is a chemical synthesis, synthetic organic heterocyclic compound, consisting of a 5-member ring of four nitrogen atoms and one carbon atom. The name tetrazole also refers to the parent compound - a whitish crystalline powder with the f ...

containing

orally bioavailable In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. Ho ...

and selective inhibitor of fungal lanosterol 14α-demethylase (CYP51), has shown promising efficacy in the treatment of recurrent

vulvovaginal candidiasis Vaginal yeast infection, also known as candidal vulvovaginitis and vaginal thrush, is excessive growth of yeast in the vagina that results in irritation. The most common symptom is vaginal itching, which may be severe. Other symptoms include burn ...

(RVVC). Marketed under the brand name Vivjoa, this medication was developed by Mycovia Pharmaceuticals and received approval for medicinal use from

United States Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respo ...

(US FDA) in April 2022.

Society and culture

Names

Oteseconazole is the international nonproprietary name (INN).

Mechanism of action

Oteseconazole targets cytochrome P450 enzymes 51 (CYP51), which a play crucial role in maintaining the integrity and growth of fungal

cell membranes The cell membrane (also known as the plasma membrane or cytoplasmic membrane, and historically referred to as the plasmalemma) is a biological membrane that separates and protects the interior of a cell from the outside environment (the extra ...

. Through inhibition of these enzymes, oteseconazole prevents the synthesis of

ergosterol Ergosterol (ergosta-5,7,22-trien-3β-ol) is a mycosterol found in cell membranes of fungi and protozoa, serving many of the same functions that cholesterol serves in animal cells. Because many fungi and protozoa cannot survive without ergostero ...

, a key component of fungal cell membranes development. This disruption in ergosterol production leads to fungal membranes permeability, ultimately causing cell death. Oteseconazole exhibits selective inhibition of fungal CYP51 and has shown remarkable potency against ''Candida'' species during

in vitro ''In vitro'' (meaning ''in glass'', or ''in the glass'') Research, studies are performed with Cell (biology), cells or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in ...

pharmacological studies. This targeted action of oteseconazole makes it a highly effective choice for treating RVVC. Additionally, oteseconazole was found to possess superior activity against certain fungi, such as ''

Candida glabrata ''Nakaseomyces glabratus'' is a species of haploid yeast of the genus ''Nakaseomyces'', previously known as ''Candida glabrata''. Despite the fact that no sexual life cycle has been documented for this species, ''N. glabratus'' strains of both ma ...

'' compared to commonly used

antifungals An antifungal medication, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as ...

Adverse effect and interaction

Oteseconazole has exhibited an outstanding tolerability profile and a low occurrence of adverse effects in clinical trials. In a phase 3 study, the incidence of treatment-emergent adverse events (TEAEs) was comparable between the oteseconazole and

fluconazole Fluconazole is an antifungal medication used for a number of fungal infections. These include candidiasis, blastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, dermatophytosis, and tinea versicolor. It is also used to pr ...

placebo A placebo ( ) can be roughly defined as a sham medical treatment. Common placebos include inert tablets (like sugar pills), inert injections (like saline), sham surgery, and other procedures. Placebos are used in randomized clinical trials ...

groups, with the majority of TEAEs being of mild or moderate severity. No serious adverse events related to the drug, as well as no adverse effects on liver function or QT intervals, were reported. However, as with any medication, there is a potential risk of adverse effects. Therefore, it is crucial to consult with a healthcare provider prior to initiating oteseconazole or any other medication. There is currently limited information available on oteseconazole interactions with other medications. The prescribing information for oteseconazole indicates that it is a moderate inhibitor of the

CYP3A4 Cytochrome P450 3A4 (abbreviated CYP3A4) () is an important enzyme in the body, mainly found in the liver and in the intestine, which in humans is encoded by ''CYP3A4'' gene. It organic redox reaction, oxidizes small foreign organic molecules ( ...

enzyme, suggesting that it may potentially increase the exposure of co-administered medications that are primarily metabolized by CYP3A4. Therefore, patients who are taking medications metabolized by CYP3A4 should be closely monitored for any signs of toxicity or adverse effects when using oteseconazole. It is crucial to have a discussion with a healthcare provider about the use of any medications or supplements to ensure safe and effective usage.

References

External links

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