Apalutamide
Chemical compound / From Wikipedia, the free encyclopedia
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Apalutamide, sold under the brand name Erleada among others, is a nonsteroidal antiandrogen (NSAA) medication which is used in the treatment of prostate cancer.[2][8][9][10][11] It is specifically indicated for use in conjunction with castration in the treatment of non-metastatic castration-resistant prostate cancer (NM-CRPC).[2][12][13] It is taken by mouth.[2][8]
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Trade names | Erleada, others |
Other names | ARN-509; JNJ-56021927; JNJ-927; A52 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a618018 |
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Routes of administration | By mouth[2] |
Drug class | Nonsteroidal antiandrogen |
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Bioavailability | 100%[2] |
Protein binding | Apalutamide: 96%[2] NDMA: 95%[2] |
Metabolism | Liver (CYP2C8, CYP3A4)[2] |
Metabolites | • NDMATooltip N-Desmethylapalutamide[2] |
Elimination half-life | Apalutamide: 3–4 days (at steady-state)[7][2] |
Excretion | Urine: 65%[2] Feces: 24%[2] |
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ECHA InfoCard | 100.235.115 |
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Formula | C21H15F4N5O2S |
Molar mass | 477.44 g·mol−1 |
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Side effects of apalutamide when added to castration include fatigue, nausea, abdominal pain, diarrhea, high blood pressure, rash, falls, bone fractures, and an underactive thyroid.[2][14][15][8][10] Rarely, it can cause seizures.[2][8] The medication has a high potential for drug interactions.[2][8] Apalutamide is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like testosterone and dihydrotestosterone.[2][8][11] In doing so, it prevents the effects of these hormones in the prostate gland and elsewhere in the body.[2][8][11]
Apalutamide was first described in 2007, and was approved for the treatment of prostate cancer in February 2018.[12][13][8][16] It was the first medication to be approved specifically for the treatment of NM-CRPC.[2][8][13]