Bicalutamide API Manufacturers & Suppliers
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Bicalutamide | CAS No: 90357-06-5 | GMP-certified suppliers
A medication that provides antiandrogen therapy in combination with LHRH agonists for treating advanced metastatic prostate cancer by inhibiting androgen receptor activity.
Therapeutic categories
Primary indications
- Bicalutamide is indicated in combination with a luteinizing hormone-releasing hormone (LHRH) agonist for the treatment of Stage D2 metastatic carcinoma of the prostate
Product Snapshot
- Bicalutamide is an oral small molecule formulated primarily as coated and film-coated tablets
- It is indicated for use in combination therapy for metastatic prostate carcinoma
- The product is approved for sale in regulated markets including the US and Canada
Clinical Overview
Pharmacologically, bicalutamide functions as a pure androgen receptor antagonist. It selectively binds to androgen receptors without significant affinity for other steroid hormone receptors such as progestogen, estrogen, or glucocorticoid receptors. By competitively inhibiting androgen binding, bicalutamide blocks the stimulatory effects of both testicular and adrenal androgens on prostatic tissue, thus impeding the growth of androgen-dependent prostate cancer cells. However, antiandrogen monotherapy has not consistently demonstrated efficacy equivalent to castration methods.
Bicalutamide belongs to the chemical class of trifluoromethylbenzenes, which are organofluorine compounds characterized by a benzene ring substituted with trifluoromethyl groups. It also falls under several pharmacological categories, including amides, amines, sulfur compounds, and cytochrome P450 enzyme inhibitors and substrates, particularly affecting CYP2C19, CYP2C9, CYP2D6, and CYP3A4 isoforms. This interaction profile necessitates consideration of potential drug-drug interactions during clinical use.
Key ADME characteristics include oral bioavailability and metabolism predominantly mediated through hepatic cytochrome P450 enzymes. Its role as both a substrate and inhibitor of multiple CYP450 enzymes underscores the need for careful evaluation of co-administered agents. Safety considerations include monitoring for hepatotoxicity, gastrointestinal disturbances, and potential effects on the cardiovascular system.
Bicalutamide is marketed under various brand names worldwide and remains a standard component of endocrine therapy in prostate cancer management. From an API sourcing perspective, ensuring pharmaceutical-grade purity, enantiomeric composition consistency, and compliance with relevant pharmacopeial standards is essential. Reliable supply chains with robust quality control are critical due to the compound’s narrow therapeutic window and complex metabolic profile.
Identification & chemistry
| Generic name | Bicalutamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 90357-06-5 |
| UNII | A0Z3NAU9DP |
| DrugBank ID | DB01128 |
Pharmacology
| Summary | Bicalutamide is a nonsteroidal anti-androgen that selectively binds to androgen receptors, inhibiting the effects of androgens from adrenal and testicular sources. This blockade reduces stimulation of both normal and malignant prostatic tissue growth. It is primarily utilized in combination therapy for androgen-dependent prostate cancer. |
|---|---|
| Mechanism of action | Bicalutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue. |
| Pharmacodynamics | Bicalutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Bicalutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Bicalutamide blocks the action of androgens of adrenal and testicular origin which 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. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Androgen receptor | Humans | antagonist |
ADME / PK
| Absorption | Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown. |
|---|---|
| Half-life | 5.9 days |
| Protein binding | 96% |
| Metabolism | Bicalutamide undergoes stereo specific metabolism. The S (inactive) isomer is metabolized primarily by glucuronidation. The R (active) isomer also undergoes glucuronidation but is predominantly oxidized to an inactive metabolite followed by glucuronidation. |
| Clearance | * Apparent oral cl=0.32 L/h [Normal Males] |
Formulation & handling
- Bicalutamide is a small molecule formulated exclusively for oral administration as film-coated or coated tablets.
- The API exhibits low water solubility and moderate lipophilicity (LogP 2.71), which may influence formulation strategies for dissolution enhancement.
- Food intake does not significantly impact absorption, allowing flexible dosing without strict dietary restrictions.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) entered the market in Canada and the US following patent expiry in 2022, leading to increased generic availability and established market presence in both countries. Ongoing competition is primarily from approved generics within these mature markets. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Bicalutamide's manufacturing and supply landscape involves multiple originator and generic manufacturers, indicating a diversified and competitive market. Branded products have a presence primarily in the US and Canadian markets, supported by a range of packagers. Patent expirations have facilitated the entry of numerous generic competitors, reflecting ongoing generic competition in key markets. |
|---|
Bicalutamide 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.
Bicalutamide (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.
Bicalutamide API manufacturers & distributors
Compare qualified Bicalutamide API suppliers worldwide. We currently have 18 companies offering Bicalutamide API, with manufacturing taking place in 7 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 |
|---|---|---|---|---|---|
| AXXO GmbH | Distributor | Germany | European Union | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| CF Pharma | Producer | Hungary | Hungary | CoA, GMP | 7 products |
| Cipla | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 164 products |
| Gedeon Richter | Producer | Hungary | Hungary | CoA, GMP | 48 products |
| Hetero Labs | Producer | India | India | CEP, CoA, FDA, GMP, JDMF, USDMF, WC | 90 products |
| Kekule Pharma | Producer | India | India | CEP, CoA, FDA, JDMF, WC | 2 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Mac Chem Products | Producer | India | India | CoA, USDMF | 25 products |
| MSN Labs. | Producer | India | India | CEP, CoA, FDA, GMP, USDMF | 119 products |
| Prochem Pharmtech Co., Lt... | Producer | Taiwan | Taiwan | BSE/TSE, CoA, MSDS, USDMF | 2 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shaanxi Dasheng Pharma | Producer | China | China | CEP, CoA, GMP | 3 products |
| Shilpa Medicare Ltd | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, GMP, ISO9001, MSDS, USDMF, WC | 54 products |
| Signa | Producer | Mexico | Mexico | CoA, USDMF | 42 products |
| Sumitomo Chemical | Producer | Japan | Japan | CoA, JDMF | 28 products |
| Sun Pharma | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 219 products |
| USV | Producer | India | India | CoA, FDA, GMP, JDMF, USDMF, WC | 35 products |
| Zhejiang Hisun Pharma | Producer | China | China | CEP, CoA, GMP, JDMF, USDMF | 69 products |
When sending a request, specify which Bicalutamide 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 Bicalutamide 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.
