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Enzalutamide | CAS No: 915087-33-1 | GMP-certified suppliers
A medication that supports treatment of castration-resistant and castration-sensitive prostate cancers, including high-risk recurrence and certain HRR‑mutated metastatic cases, for streamlined API sourcing.
Therapeutic categories
Primary indications
- Enzalutamide is indicated for the treatment of castration-resistant prostate cancer, metastatic castration-sensitive prostate cancer (mCSPC), and non-metastatic castration-sensitive prostate cancer (nmCSPC) with biochemical recurrence at high risk for metastasis (high-risk BCR)
- It is also used in combination with [talazoparib] for the treatment of adult patients with HRR gene-mutated mCRPC
Product Snapshot
- Oral small‑molecule formulation supplied mainly as capsules and film‑coated tablets
- Used for castration‑resistant and castration‑sensitive prostate cancer, including metastatic and high‑risk biochemical‑recurrence settings, and in combination with talazoparib for HRR‑mutated mCRPC
- Approved in the US, Canada, and EU
Clinical Overview
Enzalutamide exhibits high affinity for the androgen receptor and lacks partial agonist activity. Its pharmacodynamic effect is based on competitive inhibition of androgen binding, blockade of androgen receptor nuclear translocation, and prevention of receptor interaction with chromosomal DNA. This disrupts transcription of androgen‑regulated oncogenic pathways. Binding affinity is reported to be five to eight times greater than that of bicalutamide and only modestly lower than that of dihydrotestosterone. In vitro and clinical data demonstrate suppression of tumor cell proliferation, induction of apoptosis, reductions in prostate‑specific antigen levels, and improved survival outcomes in castration‑resistant disease.
Absorption is oral, with high protein binding and extensive hepatic metabolism. The compound is both a substrate and a modulator of multiple CYP450 enzymes, including CYP2C8 and CYP3A families, which contributes to drug–drug interaction potential. Induction of CYP2C19, CYP2C9, and CYP3A pathways and inhibition of CYP2C8 are noted. It also interacts with P‑glycoprotein. Elimination involves both hepatic metabolism and renal excretion of metabolites.
Safety considerations include risks of fatigue, seizures, hypertension, falls, and potential hepatic laboratory abnormalities. Resistance may emerge due to androgen receptor mutations or splice variants. Use requires attention to co‑medications influenced by CYP induction or inhibition.
Enzalutamide is marketed globally, with Xtandi being a widely recognized brand. For API procurement, suppliers should demonstrate rigorous control of polymorphic form, impurity profile, and stability characteristics, along with full traceability to GMP‑compliant production and validated analytical methods.
Identification & chemistry
| Generic name | Enzalutamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 915087-33-1 |
| UNII | 93T0T9GKNU |
| DrugBank ID | DB08899 |
Pharmacology
| Summary | Enzalutamide is a second‑generation androgen receptor inhibitor that blocks androgen binding, receptor nuclear translocation, and downstream transcriptional signaling. By targeting multiple steps in the androgen signaling pathway with high receptor affinity, it suppresses AR‑driven proliferation in prostate cancer cells, including certain resistance‑associated receptor alterations. Its pharmacologic effect is characterized by reduced AR activity and inhibition of androgen‑dependent tumor growth. |
|---|---|
| Mechanism of action | Enzalutamide is a competitive androgen receptor (AR) inhibitor that has a threefold inhibition on the androgen signaling pathway without significant AR agonist activity.It inhibits androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with chromosomal DNA to upregulate oncogenes.Enzalutamide binds to the AR with 5 to 8-fold greater affinity than first-generation antiandrogens such as bicalutamide and only 2-3 fold reduced affinity than the natural ligand dihydrotestosterone.Molecular docking showed that enzalutamide binds to the ligand binding domain of the AR distinctive from that of bicalutamide. |
| Pharmacodynamics | Enzalutamide is a second-generation antiandrogen that blocks the activity of androgen and androgen receptor (AR) in prostate cancer. AR activity and prostate cancer progression are closely related due to the normal physiology of prostate cells, providing the rationale for androgen deprivation therapy (ADT).However, resistance will eventually arise after the commencement of ADT in 2-3 years due to the accumulation of mutations, including constitutively active mutation, AR overexpression, and changes in AR splicing variants.Enzalutamide was therefore designed to exploit these mutations.In vitro experiments in human prostate cancer cell line VCaP showed that enzalutamide can suppress cell growth and induce apoptosis while other antiandrogens like bicalutamide did not. Clinical trials on prostate cancer patients indicated that enzalutamide can lead to a decrease in serum PSA for at least 12 weeks, although this response can be short-lived and thus resulting in enzalutamide resistance.Patients receiving enzalutamide also had a 37% decreased in the risk of death compared to placebo. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Androgen receptor | Humans | inhibitor |
ADME / PK
| Absorption | The median Tmax is 1 hour (0.5 to 3 hours) following a single 160 mg dose of capsules and 2 hours (0.5 to 6 hours) following a single 160 mg dose of tablets.Enzalutamide achieves steady-state by Day 28 and its AUC accumulates approximately 8.3-fold relative to a single dose. At steady-state, the mean (%CV) maximum concentration (Cmax) for enzalutamide and N-desmethyl enzalutamide is 16.6 µg/mL (23%) and 12.7 µg/mL (30%), respectively, and the mean (%CV) minimum concentrations (Cmin) are 11.4 µg/mL (26%) and 13.0 µg/mL (30%), respectively. |
|---|---|
| Half-life | The mean terminal half-life (t1/2) for enzalutamide in patients after a single oral dose is 5.8 days (range 2.8 to 10.2 days). Following a single 160 mg oral dose of enzalutamide in healthy volunteers, the mean terminal t1/2 for N-desmethyl enzalutamide is approximately 7.8 to 8.6 days. |
| Protein binding | Enzalutamide is 97% to 98% bound to plasma proteins, primarily albumin. N-desmethyl enzalutamide is 95% bound to plasma proteins. |
| Metabolism | Enzalutamide is metabolized by CYP2C8 and CYP3A4. CYP2C8 is primarily responsible for the formation of the active metabolite (N-desmethyl enzalutamide). Carboxylesterase 1 metabolizes N-desmethyl enzalutamide and enzalutamide to the inactive carboxylic acid metabolite. |
| Route of elimination | Enzalutamide is primarily eliminated by hepatic metabolism. 71% of the dose is recovered in urine (including only trace amounts of enzalutamide and N-desmethyl enzalutamide), and 14% is recovered in feces (0.4% of the dose as unchanged enzalutamide and 1% as N-desmethyl enzalutamide). |
| Volume of distribution | The mean (%CV) volume of distribution after a single oral dose is 110 L (29%). |
| Clearance | The mean apparent clearance (CL/F) of enzalutamide after a single dose is 0.56 L/h (0.33 to 1.02 L/h). |
Formulation & handling
- Oral small‑molecule API with very low aqueous solubility, typically requiring solubilizing excipients or lipid-filled capsule systems to enhance dissolution.
- High lipophilicity (LogP ~4) supports lipid-based formulations but may necessitate attention to precipitation control in the GI environment.
- Stable as a solid oral product and not food‑sensitive for absorption, enabling flexible administration without specific meal‑time constraints.
Regulatory status
| Lifecycle | The API remains partially protected in the United States through 2033 due to a later‑expiring patent, while earlier patents expire between 2026 and 2027. With products already marketed in the US, Canada, and the EU, the asset is in a mature commercial phase, with additional U.S. exclusivity potentially delaying full generic entry. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Enzalutamide is supplied primarily by a single originator product, with branded formulations available across the US, Canada, and EU, indicating well‑established global distribution. Several key US patents expire between 2026 and 2027, while a later-expiring patent extends to 2033. The staggered expiry profile suggests that although some earlier protections will lapse soon, full generic entry may depend on the remaining later patent. |
|---|
Safety
| Toxicity | In an embryo-fetal developmental toxicity study in mice, enzalutamide caused developmental toxicity when administered at oral doses of 10 or 30 mg/kg/day throughout the period of organogenesis (gestational days 6-15). Findings included embryo-fetal lethality (increased post-implantation loss and resorptions) and decreased anogenital distance at ≥ 10 mg/kg/day, and cleft palate and absent palatine bone at 30 mg/kg/day. Doses of 30 mg/kg/day caused maternal toxicity. The doses tested in mice (1, 10, and 30 mg/kg/day) resulted in systemic exposures (AUC) of approximately 0.04, 0.4, and 1.1 times, respectively, the exposures in patients. Enzalutamide did not cause developmental toxicity in rabbits when administered throughout the period of organogenesis (gestational days 6-18) at dose levels up to 10 mg/kg/day (approximately 0.4 times the exposures in patients based on AUC). In a pharmacokinetic study in pregnant rats with a single oral 30 mg/kg enzalutamide administration on gestation day 14, enzalutamide and/or its metabolites were present in the fetus at a Cmax that was approximately 0.3 times the concentration found in maternal plasma and occurred 4 hours after administration. Based on animal studies, XTANDI may impair fertility in males of reproductive potential. Advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 3 months after the last dose of XTANDI. The most common adverse reactions (≥ 5%) are asthenia/fatigue, back pain, diarrhea, arthralgia, hot flush, peripheral edema, musculoskeletal pain, headache, upper respiratory infection, muscular weakness, dizziness, insomnia, lower respiratory infection, spinal cord compression and cauda equina syndrome, hematuria, paresthesia, anxiety, and hypertension. |
|---|
- Developmental toxicity observed in mice at ≥10 mg/kg/day included embryo‑fetal lethality, reduced anogenital distance, and craniofacial malformations
- Maternal toxicity occurred at 30 mg/kg/day
- Fetal exposure in rats reached roughly one‑third of maternal plasma concentrations
Good Manufacturing Practices
Active pharmaceutical ingredients are made in GMP-certified manufacturing facilities. GMP stands for Good Manufacturing Practices and is the main standard in the pharmaceutical industry. cGMP or Current GMP means that the company complies with the most recent requirements/version of GMP. The WHO has its own guideline for GMP, the World Health Organization or WHO GMP. The authority that has audited the company can also be from a country like China (Chinese GMP) or from the EU (EU GMP), every authority has different GMP requirements.
Enzalutamide 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.
Enzalutamide (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.
Enzalutamide API manufacturers & distributors
Compare qualified Enzalutamide API suppliers worldwide. We currently have 14 companies offering Enzalutamide 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, GMP, USDMF | 229 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Hunan Huateng Pharmaceuti... | Producer | China | China | CoA, GMP, ISO9001, MSDS | 7 products |
| Laurus Labs | Producer | India | India | CoA, USDMF | 50 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF | 64 products |
| Shandong Boyuan | Producer | China | China | BSE/TSE, CoA, MSDS, USDMF | 55 products |
| Shilpa Medicare Ltd | Producer | India | India | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF, WC | 54 products |
| Shivalik Rasayan Ltd. | Producer | India | India | CoA, GMP, USDMF, WC, WHO-GMP | 13 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, Other | 764 products |
| Tianjin Pharmacn Medical ... | Producer | China | China | BSE/TSE, CoA, MSDS, USDMF | 66 products |
When sending a request, specify which Enzalutamide 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 Enzalutamide 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.
Frequently asked questions about Enzalutamide API
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Technical
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Regulatory
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