Product Name

Enzalutamide

Name: Enzalutamide
SKU: 915087-33-1

CAS Number

915087-33-1

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Product Name:

Enzalutamide

CAS Number:

915087-33-1

Indication:

Enzalutamide is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel.

Mode of Action:

Enzalutamide is a competitive androgen receptor inhibitor that effects multiple stages of the signalling pathway. It is able to inhibit androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with DNA. As a result, proliferation of prostate cancer cells decreases which ultimately leads to apoptosis and decreased tumour volume.

Pharmacodynamics:

Resitance to enzalutamide therapy has been observed. This may occurred due to an upregulation of NF-_B2/p52.

Metabolism:

Enzalutamide is hepatically metabolized, primarily by CYP2C8 and CYP3A4. The enzyme that converts enzalutamide to its active metabolite, N-desmethyl enzalutamide, is CYP2C8. The activity of N-desmethyl-enzalutamide is similar to that of the parent compound.

Toxicity:

The most common adverse reactions (³ 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.

IUPAC:

4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5, 5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl}-2-fluoro-N-methylbenzamide

ATC:

L02BB03

DrugBank:

DB08899

Formula:

C₂₁H₁₆F₄N₄O₂S

Molecular Mass:

464.436

Synonyms:

MDV3100

SMILES:

CNC(=O)C1=C(F)C=C(C=C1)N1C(=S)N(C(=O)C1(C)C)C1=CC=C(C#N)C(=C1)C(F)(F)F

AHFS Code:

10:00

General Reference:

Nadiminty N, Tummala R, Liu C, Yang J, Lou W, Evans CP, Gao AC: NF-kappaB2/p52 induces resistance to Enzalutamide in Prostate Cancer: Role of androgen receptor and its variants. Mol Cancer Ther. 2013 May 22. Pubmed

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Enzalutamide

915087-33-1

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