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Title: Apalutamide  
Author: World Heritage Encyclopedia
Language: English
Subject: ODM-201, Antiandrogen, Enzalutamide, Bicalutamide, Hydroxyflutamide
Publisher: World Heritage Encyclopedia


Systematic (IUPAC) name
Clinical data
  • X
Routes of
CAS Registry Number
ATC code None
PubChem CID:
Chemical data
Formula C21H15F4N5O2S
Molecular mass 477.434713 g/mol

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.[1] It is similar to enzalutamide both structurally and pharmacologically,[2] acting as a selective competitive antagonist of the androgen receptor (AR), but shows some advantages, including greater potency and reduced central nervous system permeation.[1][3][4] 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.[1][3][5] The drug has been found to be effective and well-tolerated in clinical trials thus far,[2][4] with the most common side effects reported including fatigue, nausea, abdominal pain, and diarrhea.[6][3][5] Apalutamide is currently in phase III clinical trials for castration-resistant prostate cancer.[7]

Recently, the acquired F876L mutation of the AR identified in advanced prostate cancer cells was found to confer resistance to both enzalutamide and apalutamide.[8][9] 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.[10]

Apalutamide may be effective in a subset of prostate cancer patients with acquired resistance to abiraterone acetate.[2]

See also


  1. ^ a b c Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L, Aparicio A, Dorow S, Arora V, Shao G, Qian J, Zhao H, Yang G, Cao C, Sensintaffar J, Wasielewska T, Herbert MR, Bonnefous C, Darimont B, Scher HI, Smith-Jones P, Klang M, Smith ND, De Stanchina E, Wu N, Ouerfelli O, Rix PJ, Heyman RA, Jung ME, Sawyers CL, Hager JH (2012). "ARN-509: a novel antiandrogen for prostate cancer treatment". Cancer Res. 72 (6): 1494–503.  
  2. ^ a b c Patel JC, Maughan BL, Agarwal AM, Batten JA, Zhang TY, Agarwal N (2013). "Emerging molecularly targeted therapies in castration refractory prostate cancer". Prostate Cancer 2013: 981684.  
  3. ^ a b c Schweizer MT, Antonarakis ES (2012). "Abiraterone and other novel androgen-directed strategies for the treatment of prostate cancer: a new era of hormonal therapies is born". Ther Adv Urol 4 (4): 167–78.  
  4. ^ a b Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer J 19 (1): 43–9.  
  5. ^ a b Pinto Á (2014). "Beyond abiraterone: new hormonal therapies for metastatic castration-resistant prostate cancer". Cancer Biol. Ther. 15 (2): 149–55.  
  6. ^ Leibowitz-Amit R, Joshua AM (2012). "Targeting the androgen receptor in the management of castration-resistant prostate cancer: rationale, progress, and future directions". Curr Oncol 19 (Suppl 3): S22–31.  
  7. ^ Agarwal N, Di Lorenzo G, Sonpavde G, Bellmunt J (2014). "New agents for prostate cancer". Ann. Oncol. 25 (9): 1700–9.  
  8. ^ Joseph JD, Lu N, Qian J, Sensintaffar J, Shao G, Brigham D, Moon M, Maneval EC, Chen I, Darimont B, Hager JH (2013). "A clinically relevant androgen receptor mutation confers resistance to second-generation antiandrogens enzalutamide and ARN-509". Cancer Discov 3 (9): 1020–9.  
  9. ^ Nelson WG, Yegnasubramanian S (2013). "Resistance emerges to second-generation antiandrogens in prostate cancer". Cancer Discov 3 (9): 971–4.  
  10. ^ Moilanen AM, Riikonen R, Oksala R, Ravanti L, Aho E, Wohlfahrt G, Nykänen PS, Törmäkangas OP, Palvimo JJ, Kallio PJ (2015). "Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies". Sci Rep 5: 12007.  

External links

  • Apalutamide - AdisInsight

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