• #LGM Pharma is a Enzalutamide CAS# 915087-33-1 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, delivery, purity, and more.
  • #Questions? Call our customer API support number 1-(800)-881-8210.
  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 915087-33-1
  • AHFC code: 10:00
  • Synonyms: MDV3100
  • ATC Code: L02BB03
  • Chemical Formula: C21H16F4N4O2S
  • Molecular Weight: 464.436
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB08899
  • 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
  • InChl:
  • PubChem:
  • IUPAC: 4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl}-2-fluoro-N-methylbenzamide

Additional Details

Indication:
Enzalutamide is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel.
Pharmacodynamics:
Resitance to enzalutamide therapy has been observed. This may occurred due to an upregulation of NF-_B2/p52.
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.
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.
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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