User:Mr. Ibrahem/Apalutamide

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Mr. Ibrahem/Apalutamide
Clinical data
Trade namesErleada, others
Other namesARN-509; JNJ-56021927; JNJ-927; A52
AHFS/Drugs.comMonograph
MedlinePlusa618018
License data
Pregnancy
category
Routes of
administration		By mouth[2]
Drug classNonsteroidal antiandrogen[3]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only[2]
  • EU: Rx-only[4]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability100%[2]
Protein bindingApalutamide: 96%[2]
NDMA: 95%[2]
MetabolismLiver (CYP2C8, CYP3A4)[2]
Metabolites• NDMATooltip N-Desmethylapalutamide[2]
Elimination half-lifeApalutamide: 3–4 days (at steady-state)[5][2]
ExcretionUrine: 65%[2]
Feces: 24%[2]
Identifiers
  • 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
Chemical and physical data
FormulaC21H15F4N5O2S
Molar mass477.44 g·mol−1
3D model (JSmol)
  • CNC(=O)C1=C(C=C(C=C1)N2C(=S)N(C(=O)C23CCC3)C4=CN=C(C(=C4)C(F)(F)F)C#N)F
  • InChI=1S/C21H15F4N5O2S/c1-27-17(31)13-4-3-11(8-15(13)22)30-19(33)29(18(32)20(30)5-2-6-20)12-7-14(21(23,24)25)16(9-26)28-10-12/h3-4,7-8,10H,2,5-6H2,1H3,(H,27,31)
  • Key:HJBWBFZLDZWPHF-UHFFFAOYSA-N

Apalutamide, sold under the brand name Erleada among others, is a medication used to treat prostate cancer.[2] Specifically it is used in metastatic castration-sensitive prostate cancer and non-metastatic castration-resistant prostate cancer (NM-CRPC).[2] It is taken by mouth.[2]

Common side effects include tiredness, joint pain, rash, falls, high blood pressure, hot flashes, diarrhea, and bone fractures.[2] Other side effects may include stroke and seizures.[2] Use by males whose partners are pregnant may harm the baby.[2] It is a nonsteroidal antiandrogen (NSAA) and works by blocking androgens including testosterone.[4][3] As prostate cancer require androgens, blocking them slows its growth.[4]

Apalutamide was described in 2007.[6] It approved for medical use in the United States in 2018 and Europe in 2019.[2][4] In the United Kingdom 4 weeks costs the NHS about £2,700 as of 2021.[7] This amount in the United States is about 12,500 USD.[8]

References[edit]

  1. ^ a b "Apalutamide (Erleada) Use During Pregnancy". Drugs.com. 20 July 2020. Archived from the original on 29 November 2020. Retrieved 28 September 2020.
  2. ^ a b c d e f g h i j k l m n o p q r s "Erleada- apalutamide tablet, film coated". DailyMed. 27 October 2020. Archived from the original on 9 November 2020. Retrieved 8 November 2020.
  3. ^ a b "Apalutamide Monograph for Professionals". Drugs.com. Retrieved 14 January 2022.
  4. ^ a b c d "Erleada". Archived from the original on 28 December 2020. Retrieved 14 January 2022.
  5. ^ Rathkopf DE, Morris MJ, Fox JJ, Danila DC, Slovin SF, Hager JH, et al. (October 2013). "Phase I study of ARN-509, a novel antiandrogen, in the treatment of castration-resistant prostate cancer". Journal of Clinical Oncology. 31 (28): 3525–30. doi:10.1200/JCO.2013.50.1684. PMC 3782148. PMID 24002508.
  6. ^ "Espacenet - Original document". Archived from the original on 4 November 2021. Retrieved 25 August 2021.
  7. ^ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 990. ISBN 978-0857114105.
  8. ^ "Erleada Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 15 January 2021. Retrieved 14 January 2022.
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