Clinical data | |
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Trade names | Erleada, others |
Other names | ARN-509; JNJ-56021927; JNJ-927; A52 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a618018 |
License data | |
Pregnancy category |
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Routes of administration | By mouth[2] |
Drug class | Nonsteroidal antiandrogen |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | 100%[2] |
Protein binding | Apalutamide: 96%[2] NDMA: 95%[2] |
Metabolism | Liver (CYP2C8, CYP3A4)[2] |
Metabolites | • NDMA[2] |
Elimination half-life | Apalutamide: 3–4 days (at steady-state)[7][2] |
Excretion | Urine: 65%[2] Feces: 24%[2] |
Identifiers | |
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CAS Number | |
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ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.235.115 |
Chemical and physical data | |
Formula | C21H15F4N5O2S |
Molar mass | 477.44 g·mol−1 |
3D model (JSmol) | |
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Apalutamide, sold under the brand name Erleada among others, is a nonsteroidal antiandrogen (NSAA) medication used for the treatment of prostate cancer.[2][8][9] It is an androgen receptor inhibitor.[2] It is taken by mouth.[2][10]
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][11][12][10][13] Rarely, it can cause seizures.[2][10] The medication has a high potential for drug interactions.[2][10] Apalutamide is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like testosterone and dihydrotestosterone.[2][10][14] In doing so, it prevents the effects of these hormones in the prostate gland and elsewhere in the body.[2][10][14]
Apalutamide was first described in 2007, and was approved for the treatment of prostate cancer in February 2018.[8][9][10][15] It is the first medication to be approved specifically for the treatment of non-metastatic castration-resistant prostate cancer.[2][10][9]
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