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- Apalutamide abstract "Apalutamide (INN) (developmental code name ARN-509, also JNJ-56021927) is a non-steroidal antiandrogen that is under development for the treatment of prostate cancer. It is similar to enzalutamide both structurally and pharmacologically, acting as a selective competitive antagonist of the androgen receptor (AR), but shows some advantages, including greater potency and reduced central nervous system permeation. Apalutamide binds weakly to the GABAA receptor similarly to enzalutamide, but due to its relatively lower central concentrations, may have a lower risk of seizures in comparison. The drug has been found to be effective and well-tolerated in clinical trials thus far, with the most common side effects reported including fatigue, nausea, abdominal pain, and diarrhea. Apalutamide is currently in phase III clinical trials for castration-resistant prostate cancer.Recently, the acquired F876L mutation of the AR identified in advanced prostate cancer cells was found to confer resistance to both enzalutamide and apalutamide. A newer antiandrogen, ODM-201, is not affected by this mutation, nor has it been found to be affected by any other tested/well-known AR mutations.Apalutamide may be effective in a subset of prostate cancer patients with acquired resistance to abiraterone acetate.".
- Apalutamide atcPrefix "None".
- Apalutamide casNumber "956104-40-8".
- Apalutamide iupacName "4-[7-[6-Cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-N-methylbenzamide".
- Apalutamide pubchem "24872560".
- Apalutamide thumbnail Apalutamide.svg?width=300.
- Apalutamide wikiPageExternalLink 800032695.
- Apalutamide wikiPageID "47734223".
- Apalutamide wikiPageLength "7759".
- Apalutamide wikiPageOutDegree "33".
- Apalutamide wikiPageRevisionID "698910564".
- Apalutamide wikiPageWikiLink Abdominal_pain.
- Apalutamide wikiPageWikiLink Abiraterone_acetate.
- Apalutamide wikiPageWikiLink Androgen_receptor.
- Apalutamide wikiPageWikiLink Antiandrogen.
- Apalutamide wikiPageWikiLink Castration.
- Apalutamide wikiPageWikiLink Category:Antiandrogens.
- Apalutamide wikiPageWikiLink Category:Benzamides.
- Apalutamide wikiPageWikiLink Category:Experimental_cancer_drugs.
- Apalutamide wikiPageWikiLink Category:GABAA_receptor_negative_allosteric_modulators.
- Apalutamide wikiPageWikiLink Category:Organofluorides.
- Apalutamide wikiPageWikiLink Category:Pyridines.
- Apalutamide wikiPageWikiLink Category:Spiro_compounds.
- Apalutamide wikiPageWikiLink Central_nervous_system.
- Apalutamide wikiPageWikiLink Clinical_trial.
- Apalutamide wikiPageWikiLink Competitive_antagonist.
- Apalutamide wikiPageWikiLink Diarrhea.
- Apalutamide wikiPageWikiLink EPI-001.
- Apalutamide wikiPageWikiLink Enzalutamide.
- Apalutamide wikiPageWikiLink Epileptic_seizure.
- Apalutamide wikiPageWikiLink Fatigue_(medical).
- Apalutamide wikiPageWikiLink GABAA_receptor.
- Apalutamide wikiPageWikiLink Galeterone.
- Apalutamide wikiPageWikiLink International_nonproprietary_name.
- Apalutamide wikiPageWikiLink Mouth.
- Apalutamide wikiPageWikiLink Nausea.
- Apalutamide wikiPageWikiLink Nonsteroidal.
- Apalutamide wikiPageWikiLink ODM-201.
- Apalutamide wikiPageWikiLink Orteronel.
- Apalutamide wikiPageWikiLink Phases_of_clinical_research.
- Apalutamide wikiPageWikiLink Potency_(pharmacology).
- Apalutamide wikiPageWikiLink Prostate_cancer.
- Apalutamide wikiPageWikiLink Side_effect.
- Apalutamide wikiPageWikiLink VT-464.
- Apalutamide wikiPageWikiLinkText "Apalutamide".
- Apalutamide wikiPageWikiLinkText "apalutamide".
- Apalutamide atcPrefix "None".
- Apalutamide c "21".
- Apalutamide casNumber "956104".
- Apalutamide chemspiderid "28424131".
- Apalutamide f "4".
- Apalutamide h "15".
- Apalutamide inchi "InChI=1S/C21H15F4N5O2S/c1-27-1713-4-3-1130-192912-7-141628-10-12/h3-4,7-8,10H,2,5-6H2,1H3,".
- Apalutamide inchikey "HJBWBFZLDZWPHF-UHFFFAOYSA-N".
- Apalutamide iupacName "4".
- Apalutamide molecularWeight "477.434713".
- Apalutamide n "5".
- Apalutamide o "2".
- Apalutamide pregnancyCategory "X".
- Apalutamide pubchem "24872560".
- Apalutamide routesOfAdministration Mouth.
- Apalutamide s "1".
- Apalutamide smiles "CNCC1=CF".
- Apalutamide wikiPageUsesTemplate Template:Androgenics.
- Apalutamide wikiPageUsesTemplate Template:Antiandrogens.
- Apalutamide wikiPageUsesTemplate Template:Drug-stub.
- Apalutamide wikiPageUsesTemplate Template:Drugbox.
- Apalutamide wikiPageUsesTemplate Template:GABAergics.
- Apalutamide wikiPageUsesTemplate Template:Reflist.
- Apalutamide subject Category:Antiandrogens.
- Apalutamide subject Category:Benzamides.
- Apalutamide subject Category:Experimental_cancer_drugs.
- Apalutamide subject Category:GABAA_receptor_negative_allosteric_modulators.
- Apalutamide subject Category:Organofluorides.
- Apalutamide subject Category:Pyridines.
- Apalutamide subject Category:Spiro_compounds.
- Apalutamide hypernym Antiandrogen.
- Apalutamide type ChemicalSubstance.
- Apalutamide type Drug.
- Apalutamide type ChemicalObject.
- Apalutamide type Thing.
- Apalutamide type Q8386.
- Apalutamide comment "Apalutamide (INN) (developmental code name ARN-509, also JNJ-56021927) is a non-steroidal antiandrogen that is under development for the treatment of prostate cancer. It is similar to enzalutamide both structurally and pharmacologically, acting as a selective competitive antagonist of the androgen receptor (AR), but shows some advantages, including greater potency and reduced central nervous system permeation.".
- Apalutamide label "Apalutamide".
- Apalutamide sameAs Q21098975.
- Apalutamide sameAs Q21098975.
- Apalutamide wasDerivedFrom Apalutamide?oldid=698910564.
- Apalutamide depiction Apalutamide.svg.
- Apalutamide isPrimaryTopicOf Apalutamide.