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N-Desmethylenzalutamide

January 01, 1970

N-Desmethylenzalutamide is a nonsteroidal antiandrogen (NSAA) and the major metabolite of enzalutamide, an NSAA which is used as a hormonal antineoplastic agent in the treatment of metastatic prostate cancer.[3][4][2] It has similar activity to that of enzalutamide and, with enzalutamide therapy, circulates at similar concentrations to those of enzalutamide at steady state.[3][4][2] N-Desmethylenzalutamide is formed from enzalutamide in the liver by the cytochrome P450 enzymes CYP2C8 and CYP3A4.[4] It has a longer terminal half-life than enzalutamide (7.8 days versus 5.8 days).[2]

N-Desmethylenzalutamide
Clinical data
Other namesDesmethylenzalutamide; Norenzalutamide
Drug classNonsteroidal antiandrogen
Pharmacokinetic data
Protein binding95%[1]
Elimination half-life7.8 days[2][1]
Identifiers
  • 4-[3-[4-Cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-fluorobenzamide
CAS Number
  • 1242137-16-1 Y
PubChem CID
  • 70678916
ChemSpider
  • 28533218
UNII
  • 567TX6UB9S
ChEBI
  • CHEBI:68538
Chemical and physical data
FormulaC20H14F4N4O2S
Molar mass450.41 g·mol−1
3D model (JSmol)
  • Interactive image
  • CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)N)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C
  • InChI=1S/C20H14F4N4O2S/c1-19(2)17(30)27(11-4-3-10(9-25)14(7-11)20(22,23)24)18(31)28(19)12-5-6-13(16(26)29)15(21)8-12/h3-8H,1-2H3,(H2,26,29)
  • Key:JSFOGZGIBIQRPU-UHFFFAOYSA-N

References edit

  1. ^ a b https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/203415s011lbl.pdf [bare URL PDF]
  2. ^ a b c d Benoist GE, Hendriks RJ, Mulders PF, Gerritsen WR, Somford DM, Schalken JA, van Oort IM, Burger DM, van Erp NP (2016). "Pharmacokinetic Aspects of the Two Novel Oral Drugs Used for Metastatic Castration-Resistant Prostate Cancer: Abiraterone Acetate and Enzalutamide". Clin Pharmacokinet. 55 (11): 1369–1380. doi:10.1007/s40262-016-0403-6. PMC 5069300. PMID 27106175.
  3. ^ a b Keating GM (2015). "Enzalutamide: a review of its use in chemotherapy-naïve metastatic castration-resistant prostate cancer". Drugs Aging. 32 (3): 243–9. doi:10.1007/s40266-015-0248-y. PMID 25711765. S2CID 29563345.
  4. ^ a b c El-Amm J, Patel N, Freeman A, Aragon-Ching JB (2013). "Metastatic castration-resistant prostate cancer: critical review of enzalutamide". Clin Med Insights Oncol. 7: 235–45. doi:10.4137/CMO.S11670. PMC 3813614. PMID 24179414.


 

This antineoplastic or immunomodulatory drug article is a stub. You can help Wikipedia by expanding it.

January 01, 1970
desmethylenzalutamide, nonsteroidal, antiandrogen, nsaa, major, metabolite, enzalutamide, nsaa, which, used, hormonal, antineoplastic, agent, treatment, metastatic, prostate, cancer, similar, activity, that, enzalutamide, with, enzalutamide, therapy, circulate. N Desmethylenzalutamide is a nonsteroidal antiandrogen NSAA and the major metabolite of enzalutamide an NSAA which is used as a hormonal antineoplastic agent in the treatment of metastatic prostate cancer 3 4 2 It has similar activity to that of enzalutamide and with enzalutamide therapy circulates at similar concentrations to those of enzalutamide at steady state 3 4 2 N Desmethylenzalutamide is formed from enzalutamide in the liver by the cytochrome P450 enzymes CYP2C8 and CYP3A4 4 It has a longer terminal half life than enzalutamide 7 8 days versus 5 8 days 2 N DesmethylenzalutamideClinical dataOther namesDesmethylenzalutamide NorenzalutamideDrug classNonsteroidal antiandrogenPharmacokinetic dataProtein binding95 1 Elimination half life7 8 days 2 1 IdentifiersIUPAC name 4 3 4 Cyano 3 trifluoromethyl phenyl 5 5 dimethyl 4 oxo 2 sulfanylideneimidazolidin 1 yl 2 fluorobenzamideCAS Number1242137 16 1 YPubChem CID70678916ChemSpider28533218UNII567TX6UB9SChEBICHEBI 68538Chemical and physical dataFormulaC 20H 14F 4N 4O 2SMolar mass450 41 g mol 13D model JSmol Interactive imageSMILES CC1 C O N C S N1C2 CC C C C2 C O N F C3 CC C C C3 C N C F F F CInChI InChI 1S C20H14F4N4O2S c1 19 2 17 30 27 11 4 3 10 9 25 14 7 11 20 22 23 24 18 31 28 19 12 5 6 13 16 26 29 15 21 8 12 h3 8H 1 2H3 H2 26 29 Key JSFOGZGIBIQRPU UHFFFAOYSA NReferences edit a b https www accessdata fda gov drugsatfda docs label 2017 203415s011lbl pdf bare URL PDF a b c d Benoist GE Hendriks RJ Mulders PF Gerritsen WR Somford DM Schalken JA van Oort IM Burger DM van Erp NP 2016 Pharmacokinetic Aspects of the Two Novel Oral Drugs Used for Metastatic Castration Resistant Prostate Cancer Abiraterone Acetate and Enzalutamide Clin Pharmacokinet 55 11 1369 1380 doi 10 1007 s40262 016 0403 6 PMC 5069300 PMID 27106175 a b Keating GM 2015 Enzalutamide a review of its use in chemotherapy naive metastatic castration resistant prostate cancer Drugs Aging 32 3 243 9 doi 10 1007 s40266 015 0248 y PMID 25711765 S2CID 29563345 a b c El Amm J Patel N Freeman A Aragon Ching JB 2013 Metastatic castration resistant prostate cancer critical review of enzalutamide Clin Med Insights Oncol 7 235 45 doi 10 4137 CMO S11670 PMC 3813614 PMID 24179414 nbsp This antineoplastic or immunomodulatory drug article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title N Desmethylenzalutamide amp oldid 1094323834, wikipedia, wiki, book, books, library,

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