恩杂鲁胺(ENZALUTAMIDE)
4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluoro-N-methylbenzamide
CAS: 915087-33-1
Molecular Formula: C21H16F4N4O2S
恩杂鲁胺(ENZALUTAMIDE) - Names and Identifiers
恩杂鲁胺(ENZALUTAMIDE) - Physico-chemical Properties
| Molecular Formula | C21H16F4N4O2S |
| Molar Mass | 464.44 |
| Density | 1.49 |
| Melting Point | 198 - 200°C |
| Solubility | Soluble in DMSO (>25 mg/ml) |
| Appearance | solid |
| Color | White to off-white |
| pKa | 13.88±0.46(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Refractive Index | 1.629 |
| Physical and Chemical Properties | White or off-white non-hygroscopic crystalline solid, melting point of 195-196 ℃, soluble in DMSO and acetonitrile, slightly soluble in absolute ethanol, insoluble in water. |
| Use | Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM. |
| In vitro study | Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM. In competitive experiments with the addition of 16β-[18F] fluoro-5α-dht (18-FDHT), Enzalutamide was found to have a higher affinity for AR than bicalutamide. While Enzalutamide had no effect on LNCaP/AR(AR-overexpressing) prostate cells. In parental LNCaP cells, Enzalutamide inhibits the production of prostate-specific antigen (PSA) and transmembrane serine protease 2(TMPRSS2) and their binding to the synthetic androgen r1881. Enzalutamide inhibited the translational activity of mutant AR protein (W741C, Trp at position 741 mutated to Cys). MDV310 also blocks the recruitment of coactivators by nuclear translocation and coordination receptor complexes. |
| In vivo study | Treatment of castrated male mice bearing LNCaP/AR xenograft tumors with Enzalutamide, 10mg of MDV310 per kg of mouse body weight, induced significant tumor regression. |
恩杂鲁胺(ENZALUTAMIDE) - Risk and Safety
| HS Code | 29339900 |
恩杂鲁胺(ENZALUTAMIDE) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.153 ml | 10.766 ml | 21.531 ml |
| 5 mM | 0.431 ml | 2.153 ml | 4.306 ml |
| 10 mM | 0.215 ml | 1.077 ml | 2.153 ml |
| 5 mM | 0.043 ml | 0.215 ml | 0.431 ml |
Last Update：2024-01-02 23:10:35
恩杂鲁胺(ENZALUTAMIDE) - Reference Information
| pharmacological action | enzalutamide (XTANDI, enzalutamide) is an oral androgen receptor antagonist, at present, it is approved by clinical research and FDA (Food and Drug Administration) for the treatment of metastatic castration-resistant prostate cancer that has progressed after chemotherapy (I. E, such patients whose tumor or cancer cells are still growing) may prolong the survival of the patients. prostate cancer is high in the United States Incidence Rate, with nearly 240,000 new cases per year (the highest of all cancers) and nearly 30,000 deaths per year (second only to lung, breast, and colorectal cancers), china's Incidence Rate was low. enzalutamide is an androgen receptor inhibitor that targets different from cabazitaxel, which was approved in 2010, and abiraterone, which competitively inhibits androgen binding to the receptor, and can inhibit the nuclear transport of androgen receptor and the interaction between the receptor and DNA. In vitro experimental studies show that Enzalutamide can inhibit the proliferation of prostate cancer cells and induce their death, in the mouse prostate cancer xenograft model experiment, Enzalutamide can reduce the tumor volume, it shows similar inhibitory activity to enzalutamide in vitro. The recommended adult dose of the drug is 160mg per day, which is rapidly absorbed after taking the drug, and the plasma concentration reaches the highest level within 0.5~3H, The mean terminal half-life is 5.8d. The main metabolizing enzymes are CYP2C8 and CYP3A4. This drug should be avoided in combination with strong CYP2C8 inhibitors (eg, gemfibrozil, gemfibrozil) if co-administration is required, the dose of enzalutamide should be reduced to 80mg once daily. FIG. 1 shows the structural formula of enzalutamide. |
| indication | for the treatment of advanced castration-resistant prostate cancer in men with spread or recurrence. |
| clinical evaluation | Enzalutamide is an oral androgen receptor inhibitor, the risk of disease progression and death associated with radiotherapy can be reduced. Although antiandrogen therapy has been the standard treatment of choice for patients with metastatic prostate cancer for 70 years, the researchers found that androgen receptors play an important role in driving prostate cancer development throughout the course of the disease. FDA-approved next-generation androgen receptor antagonists such as abiraterone and enzalutamide have been shown to benefit patients with advanced prostate cancer after docetaxel chemotherapy. both enzalutamide in Japan and abiraterone in Johnson & Johnson in the United States are targeted for the treatment of prostate cancer. According to statistics, the treatment effect is similar, with only a few differences, such: abiraterone needs to be used concomitantly with steroids, whereas enzalutamide is not required; Abiraterone needs to be diet-restricted, whereas enzalutamide is not required. Different countries of the drug is to face the crowd is not the same, so there is a price difference, the effect is the same. |
| adverse reactions | The main side effects of enzalutamide (XTANDI) were hypertension and fatigue. The most common adverse reactions (≥ 5%) were asthenia/fatigue, back pain, Diarrhea, Arthralgia, hot flashes, peripheral edema, musculoskeletal pain, Head Pain, Upper Respiratory Infections, muscle weakness, dizziness, Sleep Initiation and Maintenance Disorders, lower respiratory tract infections, spinal cord compression and cauda equina syndrome, hematuria, paresthesia, Anxiety and hypertension. |
| Application | Enzalutamide can be applied to all stages of prostate cancer, such as patients with advanced stage before chemotherapy, patients can significantly delay the time of the start of chemotherapy. In addition to CRPC and mCRPC after chemotherapy, it can significantly improve the overall survival time and progression-free survival time. |
| biological activity | Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM. |
Last Update：2024-04-10 22:29:15
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