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Enzalutamide

Pharmacological action Treatment Indications Clinical evaluation Side effects Biological activity In vivo studies
Enzalutamide
Enzalutamide structure
CAS No.
915087-33-1
Chemical Name:
Enzalutamide
Synonyms
101095;CS-355;MDV-3100;EnzalutaMide;brand name: Xtandi.;Enzalutamide, >=99%;MDV3100,Menzalutamide;Enzalutamide (Xtandi);ENZALUTAMIDE;MDV-3100;MDV3100 (EnzalutaMide)
CBNumber:
CB62500946
Molecular Formula:
C21H16F4N4O2S
Formula Weight:
464.4359528
MOL File:
915087-33-1.mol

Enzalutamide Properties

Density 
1.49
pka
13.88±0.46(Predicted)
FDA UNII
93T0T9GKNU
NCI Dictionary of Cancer Terms
enzalutamide
SAFETY
  • Risk and Safety Statements
HS Code  29339900

Enzalutamide price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 11596 MDV 3100 ≥98% 915087-33-1 5mg $75 2020-06-24 Buy
Cayman Chemical 11596 MDV 3100 ≥98% 915087-33-1 10mg $135 2020-06-24 Buy
Cayman Chemical 11596 MDV 3100 ≥98% 915087-33-1 25mg $263 2020-06-24 Buy
Cayman Chemical 11596 MDV 3100 ≥98% 915087-33-1 50mg $450 2020-06-24 Buy

Enzalutamide Chemical Properties,Uses,Production

Pharmacological action

Enzalutamide (XTANDI) is an oral androgen receptor antagonist, which is approved by the current clinical research and the US FDA (Food and Drug Administration), for the development of post-chemotherapy metastatic castration tolerance of prostate cancer Treatment (i.e. patients with prostate cancer after chemotherapy, cancer or cancer cells are still growing in such patients), can extend the survival of patients. The incidence of prostate cancer in the United States is very high, with an annual increase of nearly 240,000 patients (the highest among all cancers), nearly 30,000 deaths every year (second only to lung cancer, breast cancer, colorectal cancer),but its incidence is low in China.
Enzalutamide is an androgen receptor inhibitor, the target of action is different from the approved cabbitaxel in 2010 and the approved abbitolone in 2011, and can competitively inhibit androgen and receptor binding, and can inhibition of androgen receptor nuclear transport and the interaction of the receptor and DNA. Vitro studies have shown that enzalutamide can inhibit prostate cancer cell proliferation and induce death, and enzalutamide reduces tumor volume in mouse prostate cancer xenograft model experiment. The main metabolite of enzalutamide is N-demethylol enamine, which shows similar inhibitory activity with enzalutamide in vitro. The recommended adult dose for the drug is daily 160mg, rapidly absorbed after medication, plasma concentrations to reach the highest level in 0.5~3h, the average terminal half-life is 5.8d, the main metabolic enzymes are CYP2C8 and CYP3A4. The drug should be avoided with strong CYP2C8 inhibitors (such as gemfibrozil), if it is needed for co-administration, should reduce the dose of enzalutamide to 80mg, 1 day.

Treatment

In vitro, enzalutamide suppressed proliferation and induced apoptosis in human prostate cancer cell lines. The sensitivity of prostate cancer cells to T cell-mediated lysis via androgen receptor-dependent immunomodulation was enhanced by enzalutamide. Enzalutamide lacked androgen receptor agonist activity in CRPC cell models and induced tumour regression in CRPC xenograft models.

Indications

For the treatment of metastatic or recurrence of advanced male castration tolerance of prostate cancer.

Clinical evaluation

Enzalutamide is an oral androgen receptor inhibitor that reduces the risk of radiation-related disease progression and death.
Although anti-androgen therapy has been the preferred treatment option for patients with metastatic prostate cancer for more than 70 years, researchers have found that male hormone receptors play an important role in the development of prostate cancer throughout the course of disease with the in-depth exploration of disease at the molecular level. FDA-approved new generation of androgen receptor antagonists such as abiraterone and enzolatamide have shown that it is benefit for patients with advanced prostate cancer after chemotherapy with docetaxel.
Astellas in Japan and Johnson in the United States treat prostate cancer both through the target, according to statistics, similar to the treatment results, only a few differences, such as: abitron to be used simultaneously with steroid drugs , and enzalutamide is not required; abitron need to limit the diet, and enzalutamide does not need. Drugs in different countries is not the same as different the crowd, so there are price differences, but the effect is the same.
This information was compiled by the Editor of the Chemicalbook (2015-09-20).

Side effects

The main side effects of enxtran (XTANDI) are hypertension and fatigue. The most common adverse reactions (≥ 5%) are weakness/fatigue, back pain, diarrhea, joint pain, hot flashes, peripheral blood edema, musculoskeletal pain, headache, upper respiratory tract infection, muscle weakness, dizziness, insomnia, lower respiratory tract infection, spinal cord compression syndrome and cauda equina syndrome, hematuria, paresthesia, anxiety and hypertension.

Biological activity

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM.
Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in vitro studies. In competitive experiments with 16β-[18F] fluoro-5α-DHT (18-FDHT), enzalutamide was found to have higher affinity for bilirubin than Bicalutamide when administered to AR. While enzalutamide had no effect on LNCaP/AR (AR-overexpression) of prostate cells. In parental LNCaP cells, Enzalutamide inhibits the production of prostate specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), and inhibits their binding to the synthetic and rogen R1881. Enzalutamide inhibits the translation activity of the mutant AR protein (W741C, Trp at position 741 mutanting to Cys). MDV310 also blocked the nuclear translocation and coordination receptor complexes that recruit coactivators.

In vivo studies

Enzalutamide treatment of castrated male mice carrying LNCa/AR xenografts, mice treated with 10 mg MDV310 per kilogram of body weight, can induce significant tumor regression.

Description

In August 2012, the US FDA approved enzalutamide for the treatment of metastatic castration-resistant prostate cancer (mCRPC) in patients who have previously been treated with docetaxel. Synthesis of enzalutamide was achieved by a triply convergent route that employed a Strecker condensation, followed by isothiocyanate condensation and hydrolysis to form the thiohydantoin moiety. In LNCaP/AR cells with high expression of AR, enzalutamide demonstrated potent inhibition of 16b-[18F]-5α-dihydrotestosterone binding (IC50=21 nM compared with bicalutamide IC50=160 nM), and inhibited AR translocation to the nucleus more potently than bicalutamide.The primary metabolite is the result of CYP2C8-mediated N-demethylation; enzalutamide is primarily eliminated by hepatic metabolism.

Chemical Properties

White Solid

Originator

University of California (United States)

Uses

MDV3100, known as Enzalutamide, is a second-generation androgen receptor (AR) signaling inhibitor. It is able to inhibit binding of androgens to the AR, AR nuclear translocation, and the association of the AR with DNA.

Uses

MDV 3100 is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. MDV 3100 has also been shown to induce tumor cell apoptosis, and has no agonist activity. MDV 3100 is a candidate for the treatment of castration-resistant prostate cancer.

Definition

ChEBI: A benzamide obtained by formal condensation of the carboxy group of 4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluorobenzoic acid with methylamine. Used for the treatment of of metastatic castration-resistant p ostate cancer.

brand name

Xtandi

Enzalutamide Preparation Products And Raw materials

Raw materials

Preparation Products


Enzalutamide Suppliers

Global( 277)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58
Jurong Coupling Biotechnology Co., Ltd.
13656108824
coupling278191416@hotmail.com CHINA 184 58
Capot Chemical Co.,Ltd.
+86-571-85586718
+86-571-85864795 sales@capotchem.com China 19929 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21821 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
Hangzhou FandaChem Co.,Ltd.
0086 158 5814 5714 (Mobile
+86-571-56059825 fandachem@gmail.com CHINA 3248 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24723 60
Shandonghaohong biotechnology Co.,ltd.
0635-6175299 13961496334
0635-6175299 sale@inyelchem.com CHINA 44 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30045 58

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View Lastest Price from Enzalutamide manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-10-22 Enzalutamide MDV 3100
915087-33-1
US $95.00 / KG 10g 99% 20tons Hebei shuoxi biotechnology co. LTD
2019-08-26 Enzalutamide/MDV 3100
915087-33-1
US $0.00-0.00 / KG 1g 99% 50kg/month Beijing Yibai Biotechnology Co., Ltd
2018-07-26 4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N
915087-33-1
US $10.00 / KG 1KG 98% 200KG career henan chemical co

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