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]
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]
^"Apalutamide (Erleada) Use During Pregnancy". Drugs.com. 20 July 2020. Retrieved 28 September 2020.
^ abcdefghijklmnopqrs"Erleada- apalutamide tablet, film coated". DailyMed. 27 October 2020. Retrieved 8 November 2020.
^"PRODUCT MONOGRAPH INCLUDING PATIENT MEDICATION INFORMATION" (PDF). hres.ca. Janssen Inc. 6 July 2021. Archived (PDF) from the original on 3 November 2022. Retrieved 3 November 2022.
^"Regulatory Decision Summary for Erleada". Drug and Health Products Portal. 2 August 2023. Retrieved 2 April 2024.
^"Drug and medical device highlights 2018: Helping you maintain and improve your health". Health Canada. 14 October 2020. Retrieved 17 April 2024.
^Cite error: The named reference Erleada EPAR was invoked but never defined (see the help page).
^Cite error: The named reference RathkopfMorris2013 was invoked but never defined (see the help page).
^ abcdefghiAl-Salama ZT (April 2018). "Apalutamide: First Global Approval". Drugs. 78 (6): 699–705. doi:10.1007/s40265-018-0900-z. PMID 29626324. S2CID 4653827.
^Chong JT, Oh WK, Liaw BC (2018). "Profile of apalutamide in the treatment of metastatic castration-resistant prostate cancer: evidence to date". OncoTargets Ther. 11: 2141–2147. doi:10.2147/OTT.S147168. PMC 5905496. PMID 29695920.
^ abDellis AE, Papatsoris AG (June 2018). "Apalutamide: The established and emerging roles in the treatment of advanced prostate cancer". Expert Opin Investig Drugs. 27 (6): 553–559. doi:10.1080/13543784.2018.1484107. PMID 29856649. S2CID 46925616.
^ abcClegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, et al. (March 2012). "ARN-509: a novel antiandrogen for prostate cancer treatment". Cancer Research. 72 (6): 1494–503. doi:10.1158/0008-5472.CAN-11-3948. PMC 3306502. PMID 22266222.
^ ab"FDA approves new treatment for a certain type of prostate cancer using novel clinical trial endpoint". Food and Drug Administration. 24 March 2020.
^ abc"FDA Approves Apalutamide for Nonmetastatic Prostate Cancer".
^Cite error: The named reference pmid22852027 was invoked but never defined (see the help page).
^Cite error: The named reference pmid23355790 was invoked but never defined (see the help page).
^Cite error: The named reference WO2007126765 was invoked but never defined (see the help page).
Apalutamide, sold under the brand name Erleada among others, is a nonsteroidal antiandrogen (NSAA) medication which is used in the treatment of prostate...
impairment is unknown. Two 2020 meta-analyses reported that enzalutamide and apalutamide seemed to be more effective than darolutamide in improving metastasis-free...
Structurally distinct from enzalutamide, apalutamide, and other NSAAs. Relative to enzalutamide and apalutamide, shows greater efficacy as an AR antagonist...
(also known as complete or maximal androgen blockade). Enzalutamide, apalutamide, and abiraterone acetate are specifically approved for use in combination...
nilutamide, and bicalutamide as well as to newer second-generation NSAAs like apalutamide and proxalutamide. Enzalutamide was discovered by Charles Sawyers and...
potent inhibition of the AR relative to the other NSAAs enzalutamide and apalutamide, although they also possess much shorter and comparatively less favorable...
pure antiandrogens such as flutamide, bicalutamide, enzalutamide, and apalutamide. Cole, H. H. (1975). "Studies on Reproduction with Emphasis on Gonadotropins...
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