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Terconazole | CAS No: 67915-31-5 | GMP-certified suppliers
A medication that treats vulvovaginal candidiasis by providing localized antifungal therapy to effectively manage yeast infections of the vulva and vagina.
Therapeutic categories
Primary indications
- For the treatment of candidiasis (a yeast-like fungal infection) of the vulva and vagina
Product Snapshot
- Terconazole is formulated as a vaginal cream, insert, and suppository
- It is indicated for the treatment of vulvovaginal candidiasis
- Terconazole is approved for use in the US and Canadian markets
Clinical Overview
Pharmacologically, terconazole functions as a triazole antifungal agent that targets fungal cell membrane synthesis. It exerts its activity by inhibiting the fungal cytochrome P450 enzyme 14-alpha-demethylase (lanosterol 14-alpha-demethylase). This enzyme is essential for converting lanosterol to ergosterol, a critical component of the fungal cell membrane. Inhibition of this enzyme leads to ergosterol depletion, which compromises membrane integrity and disrupts membrane-associated processes, thereby inhibiting fungal growth and replication.
Terconazole’s mechanism of action involves disruption of fungal cell membrane permeability due to the decrease in ergosterol content. The accumulation of methylated sterols alters membrane structure and function, resulting in antifungal effects selective to susceptible fungal species. This mode of action aligns with the broader class effects of triazole antifungal agents.
Key pharmacokinetic data of terconazole are limited due to its localized intravaginal use; systemic absorption is typically minimal, reducing systemic exposure and associated risks. This localized delivery contributes to a favorable safety profile and tolerability. Safety considerations include possible local irritation or hypersensitivity reactions. Systemic toxicity is uncommon, but the potential for drug interactions mediated by cytochrome P450 enzymes should be evaluated in clinical contexts.
Terconazole is categorized as an azole antifungal agent within gynecological anti-infective therapies and has widespread approval for clinical use. It is commonly employed in managing vaginal candidiasis where topical antifungal treatment is appropriate.
From an API sourcing and quality perspective, terconazole requires stringent control of stereochemistry due to its two stereocenters, resulting in four possible stereoisomers. Consistency in stereochemical purity is critical to ensure desired pharmacological effects and safety. Suppliers should provide APIs conforming to relevant pharmacopeial standards, with adequate documentation of manufacturing controls, impurity profiles, and stability data to support regulatory submissions and clinical use.
Identification & chemistry
| Generic name | Terconazole |
|---|---|
| Molecule type | Small molecule |
| CAS | 67915-31-5 |
| UNII | 0KJ2VE664U |
| DrugBank ID | DB00251 |
Pharmacology
| Summary | Terconazole is a triazole antifungal agent that targets fungal cytochrome P450 14-alpha-demethylase (CYP51), inhibiting ergosterol synthesis. This disruption in ergosterol production compromises fungal cell membrane integrity and function, leading to inhibited fungal growth. It is primarily indicated for the treatment of vulvovaginal candidiasis. |
|---|---|
| Mechanism of action | Terconazole may exert its antifungal activity by disrupting normal fungal cell membrane permeability. Terconazole and other triazole antifungal agents inhibit cytochrome P450 14-alpha-demethylase in susceptible fungi, which leads to the accumulation of lanosterol and other methylated sterols and a decrease in ergosterol concentration. Depletion of ergosterol in the membrane disrupts the structure and function of the fungal cell leading to a decrease or inhibition of fungal growth. |
| Pharmacodynamics | Terconazole is a triazole antifungal agent available for intravaginal use. It is structurally related to imidazole-derivative antifungal agents, although terconazole and other triazoles have 3 nitrogens in the azole ring. By inhibiting the 14-alpha-demethylase (lanosterol 14-alpha-demethylase), Terconazole inhibits ergosterol synthesis. Depletion of ergosterol in fungal membrane disrupts the structure and many functions of fungal membrane leading to inhibition of fungal growth. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Cytochrome P450 51 | Yeast | antagonist |
ADME / PK
| Absorption | Following intravaginal administration of terconazole in humans, absorption ranged from 5-8% in three hysterectomized subjects and 12-16% in two non-hysterectomized subjects with tubal ligations |
|---|---|
| Half-life | 6.9 hours (range 4.0-11.3) |
| Protein binding | 94.9% |
| Metabolism | Systemically absorbed drug appears to be rapidly and extensively metabolized. Terconazole primarily undergoes oxidatative N- and O-dealkylation, dioxolane ring cleavage, and conjugation. |
| Route of elimination | Following oral (30 mg) administration of 14C-labelled terconazole, excretion of radioactivity was both by renal (32-56%) and fecal (47-52%) routes. |
Formulation & handling
- Terconazole is a small molecule antifungal formulated exclusively for vaginal administration via creams, inserts, or suppositories.
- The compound exhibits low aqueous solubility and high lipophilicity (LogP 5.37), indicating a need for formulation strategies to enhance local bioavailability.
- As a solid, Terconazole requires appropriate handling to maintain stability, with no noted peptide or biologic sensitivity concerns.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's primary patents have expired in both the US and Canada, with generic versions widely available, indicating a mature market phase in these regions. Ongoing competition focuses on formulation differentiation and cost optimization. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Terconazole's manufacturing landscape includes multiple originator companies such as Ortho McNeil Janssen Pharmaceuticals and Taro Pharmaceuticals USA, indicating a diverse supply base. Branded products are primarily present in the US and Canadian markets, with names like Terazol 3 and Taro-terconazole reflecting established market presence. The data suggests the existence of generic competition, consistent with the expiration or near-expiration of relevant patents. |
|---|
Safety
| Toxicity | The oral LD<sub>50</sub> values were found to be 1741 and 849 mg/kg for the male and female in rat. |
|---|
- 1
- Handle with appropriate personal protective equipment to avoid ingestion or inhalation exposure
- 2
Terconazole is a type of Antimycotics
Antimycotics, a subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs), are essential in the treatment of various fungal infections. These powerful medications target and eliminate harmful fungi that can cause infections in humans.
Antimycotics are classified into two main types: systemic and topical. Systemic antimycotics are administered orally or intravenously and work by circulating throughout the body, treating systemic fungal infections that affect internal organs or spread throughout the bloodstream. On the other hand, topical antimycotics are applied externally to treat localized fungal infections such as athlete's foot or yeast infections.
The efficacy of antimycotics lies in their ability to disrupt fungal cell membranes, inhibit the synthesis of fungal DNA or proteins, or interfere with essential metabolic processes specific to fungi. This targeted action minimizes damage to human cells, making these medications relatively safe for patients.
Commonly prescribed antimycotics include azoles, polyenes, allylamines, and echinocandins. Azoles inhibit the synthesis of ergosterol, a vital component of fungal cell membranes, while polyenes bind to ergosterol, resulting in the formation of pores that lead to cell death. Allylamines disrupt the synthesis of ergosterol and inhibit the activity of squalene epoxidase, an enzyme involved in ergosterol production. Echinocandins target the synthesis of β-(1,3)-D-glucan, an essential component of the fungal cell wall.
Antimycotics play a crucial role in the management of fungal infections, offering relief to patients and aiding in their recovery. As with any medication, it is important to follow healthcare professionals' guidance regarding dosage, duration of treatment, and potential side effects to ensure optimal therapeutic outcomes.
Terconazole (Antimycotics), classified under Antifungals
Antifungals are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) designed to combat fungal infections. These medications are developed to target and eliminate fungi, including yeasts and molds, which can cause a range of diseases in humans and animals.
Antifungals work by interfering with specific components or processes essential for fungal growth and reproduction. They may inhibit the synthesis of fungal cell walls or disrupt the production of ergosterol, a crucial component of fungal cell membranes. By targeting these key mechanisms, antifungal APIs effectively hinder the growth and spread of fungal infections.
The diversity within the antifungal category is reflected in the various classes of antifungal APIs available. Azoles, polyenes, echinocandins, and allylamines are common classes of antifungals. Each class exhibits unique mechanisms of action and targets specific types of fungi. This diversity enables healthcare professionals to tailor treatment plans to the specific fungal infection, optimizing therapeutic outcomes.
Antifungal APIs find application in various pharmaceutical formulations, including oral medications, topical creams, ointments, and intravenous solutions. They are crucial for the treatment of common fungal infections like athlete's foot, ringworm, vaginal yeast infections, and oral thrush. Additionally, antifungals play a crucial role in managing serious systemic fungal infections that can pose significant health risks, especially in immunocompromised individuals.
Overall, antifungal APIs are indispensable tools in the fight against fungal infections, offering effective treatment options and improving the quality of life for patients suffering from these conditions. With ongoing research and development, the antifungal category continues to evolve, providing innovative solutions to combat the ever-changing landscape of fungal pathogens.
Terconazole API manufacturers & distributors
Compare qualified Terconazole API suppliers worldwide. We currently have 4 companies offering Terconazole API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Albemarle | Producer | United States | United States | CoA, USDMF | 17 products |
| Derivados Quimicos | Producer | Spain | Spain | CoA, GMP, USDMF | 18 products |
| Janssen Pharma | Producer | Belgium | Unknown | CoA, USDMF | 63 products |
| Quimica Sintetica | Producer | Spain | Unknown | CoA, GMP, USDMF | 51 products |
When sending a request, specify which Terconazole API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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