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Nilutamide | CAS No: 63612-50-0 | GMP-certified suppliers
A medication that supports treatment of metastatic prostate cancer by combining with surgical castration to inhibit androgen-driven tumor growth in advanced disease stages.
Therapeutic categories
Primary indications
- For use in combination with surgical castration for the treatment of metastatic prostate cancer involving distant lymph nodes, bone, or visceral organs (Stage D2)
Product Snapshot
- Nilutamide is an oral small molecule formulated as tablets
- It is primarily indicated for use in combination therapy for metastatic prostate cancer involving distant lymph nodes, bone, or visceral organs
- Nilutamide is approved in the US and Canada and also has investigational status
Clinical Overview
Pharmacologically, nilutamide functions as a pure androgen receptor antagonist. It exhibits selective affinity for androgen receptors without appreciable binding to progestogen, estrogen, or glucocorticoid receptors. By competitively inhibiting androgen binding, nilutamide blocks the stimulatory effects of androgens of adrenal and testicular origin on normal and malignant prostatic tissue. This receptor blockade results in growth arrest or transient tumor regression via suppression of androgen-dependent DNA and protein synthesis. Its binding affinity to the androgen receptor is somewhat lower than that of bicalutamide but comparable to that of hydroxuflutamide.
From an absorption, distribution, metabolism, and excretion (ADME) standpoint, nilutamide is a substrate and inhibitor of cytochrome P-450 enzymes CYP2C19, CYP2C8, and CYP2C9, implicating potential drug-drug interaction considerations. The compound is mainly eliminated via renal excretion.
Safety and toxicity evaluations have identified challenges including hepatotoxicity and visual disturbances, which need to be monitored during treatment. Due to its pharmacological profile, nilutamide is not used as monotherapy since antiandrogen monotherapy has not demonstrated equivalent efficacy to castration alone.
Among currently approved androgen receptor antagonists, nilutamide is utilized in specific oncology treatment regimens targeting androgen-dependent prostate carcinomas. Its role remains primarily adjunctive, complementing surgical castration in metastatic cases.
When sourcing nilutamide active pharmaceutical ingredient (API), attention to regulatory compliance, impurity profiles, and robust quality control in manufacturing is imperative to ensure clinical safety and efficacy. Vendor qualification should confirm adherence to good manufacturing practices and validated analytical methods for assay and impurity characterization.
Identification & chemistry
| Generic name | Nilutamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 63612-50-0 |
| UNII | 51G6I8B902 |
| DrugBank ID | DB00665 |
Pharmacology
| Summary | Nilutamide is a nonsteroidal antiandrogen that competitively inhibits androgen receptors, blocking androgen-driven stimulation of prostatic tissue growth. It is primarily used in combination with surgical castration to treat metastatic prostate cancer by inhibiting androgen-dependent DNA and protein synthesis. Its mechanism targets androgen receptors without significant activity at other steroid hormone receptors. |
|---|---|
| Mechanism of action | Nilutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin that stimulate the growth of normal and malignant prostatic tissue. This blockade of androgen receptors may result in growth arrest or transient tumor regression through inhibition of androgen-dependent DNA and protein synthesis. |
| Pharmacodynamics | Nilutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin that stimulate the growth of normal and malignant prostatic tissue. Prostate cancer is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen monotherapy has not consistently been shown to be equivalent to castration. The relative binding affinity of nilutamide at the androgen receptor is less than that of bicalutamide, but similar to that of hydroxuflutamide. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Androgen receptor | Humans | antagonist |
ADME / PK
| Absorption | Rapidly and completely absorbed, yielding high and persistent plasma concentrations. |
|---|---|
| Half-life | 38.0-59.1 hours |
| Metabolism | The results of a human metabolism study using 14C-radiolabelled tablets show that nilutamide is extensively metabolized and less than 2% of the drug is excreted unchanged in urine after 5 days. |
| Route of elimination | Nilutamide is extensively metabolized andless than 2% of the drug is excreted unchanged in urine after 5 days. Fecal elimination is negligible, ranging from 1.4% to 7% of the dose after 4 to 5 days. |
Formulation & handling
- Nilutamide is a small molecule suitable for oral tablet formulations with low water solubility, requiring appropriate excipients to enhance bioavailability. Administration should be separated from meals and alcohol consumption avoided to minimize interaction risks. Handle the solid form with standard precautions; stability is consistent with phenylhydantoin-class compounds.
Regulatory status
| Lifecycle | The API’s primary patents have expired, allowing for generic competition in both Canada and the US. Consequently, the product is in a mature market phase with multiple authorized generic and branded alternatives available. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Nilutamide is primarily manufactured and packaged by a single originator company, with branded products available in North American markets, specifically the US and Canada. The brand variants include multiple dosage forms, indicating established market presence. Patent expiry status is not provided, so the timeline for generic competition cannot be determined from the available data. |
|---|
Safety
| Toxicity | Symptoms of overdose include dizziness, general discomfort, headache, nausea, and vomiting. |
|---|
- Overexposure may cause central nervous system effects including dizziness and headache
- Ingestion at high doses can induce gastrointestinal disturbances such as nausea and vomiting
- Handling requires appropriate protective measures to minimize risk of systemic toxicity
Nilutamide is a type of Anti-androgens
Anti-androgens are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various androgen-dependent conditions. These medications work by blocking or inhibiting the activity of androgens, which are male sex hormones like testosterone. Anti-androgens are primarily employed in the management of conditions such as prostate cancer, hirsutism, androgenetic alopecia, and certain types of acne.
There are different types of anti-androgens, including steroidal and non-steroidal variants. Steroidal anti-androgens, such as cyproterone acetate, possess a similar chemical structure to testosterone and competitively bind to androgen receptors, thereby preventing the binding of testosterone. On the other hand, non-steroidal anti-androgens, like bicalutamide and flutamide, act by blocking the androgen receptors directly.
These APIs are typically synthesized through complex chemical processes in pharmaceutical manufacturing facilities, ensuring high purity and quality. Anti-androgens may be formulated into various dosage forms, such as tablets, capsules, or injections, for easy administration and absorption in the body.
The effectiveness of anti-androgens in mitigating androgen-related disorders has made them a crucial component in medical practice. Patients who require androgen suppression therapy can benefit from these medications, as they help reduce the effects of androgens on target tissues and cells.
Overall, anti-androgens play a crucial role in the treatment of androgen-dependent conditions, and their pharmaceutical APIs are engineered to provide optimal therapeutic outcomes. These pharmaceutical ingredients are a result of extensive research and development, ensuring their efficacy, safety, and compliance with regulatory standards.
Nilutamide (Anti-androgens), classified under Hormonal Agents
Hormonal agents are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the medical field. These substances play a crucial role in regulating and modulating hormonal functions within the body. Hormonal agents are designed to mimic or manipulate the effects of naturally occurring hormones, allowing healthcare professionals to treat various endocrine disorders and hormonal imbalances.
Hormonal agents are commonly employed in the treatment of conditions such as hypothyroidism, hyperthyroidism, diabetes, and hormonal cancers. These APIs work by interacting with specific hormone receptors, either by stimulating or inhibiting their activity, to restore the balance of hormones in the body. They can be administered orally, intravenously, or through other routes depending on the specific medication and patient needs.
Pharmaceutical companies employ rigorous manufacturing processes and quality control measures to ensure the purity, potency, and safety of hormonal agent APIs. These APIs are synthesized using chemical or biotechnological methods, often starting from natural hormone sources or through recombinant DNA technology. Stringent regulatory guidelines are in place to guarantee the efficacy and safety of hormonal agent APIs, ensuring that patients receive high-quality medications.
As the demand for hormone-related therapies continues to grow, ongoing research and development efforts focus on enhancing the effectiveness and reducing the side effects of hormonal agent APIs. This includes the exploration of novel delivery systems, advanced formulations, and targeted drug delivery methods. By continuously advancing our understanding and capabilities in hormonal agents, the medical community can improve patient outcomes and quality of life for individuals with hormonal disorders.
Nilutamide API manufacturers & distributors
Compare qualified Nilutamide API suppliers worldwide. We currently have 7 companies offering Nilutamide 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 |
|---|---|---|---|---|---|
| Biophore India | Producer | India | India | CEP, CoA, GMP, USDMF | 46 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Kekule Pharma | Producer | India | India | CoA, USDMF | 2 products |
| Kromozome | Distributor | India | India | CoA, GMP | 17 products |
| Sanofi | Producer | France | France | CoA, GMP | 93 products |
| Sionc Pharma | Producer | India | India | CoA, WC | 10 products |
| Triquim | Producer | Argentina | Argentina | CoA, GMP, ISO9001 | 16 products |
When sending a request, specify which Nilutamide 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.).
Use the list above to find high-quality Nilutamide API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
