Abstract
Background: Prostate cancer is considered the second most diagnosed cancer, and one of the most common causes of death from cancer in men. Apalutamide is an effective, safe, and well-tolerated agent used for the treatment of men with non-metastatic Castration-Resistant Prostate Cancer (nmCRPC) and metastatic Hormone-Naive Prostate Cancer (mHNPC). Androgen receptor signaling is a leading factor that drives these prostate tumors. USFDA has approved apalutamide on 14 February 2018 as an agent that targets androgen receptor signaling through inhibition causing significant improvement in metastasis-free survival in patients with prostate cancer.
Objective: In this review, various aspects related to apalutamide have been summarized which involve the mechanism of action, chemistry, synthesis, pharmacokinetics, pharmacodynamics, adverse reactions, and safety parameters.
Methods: The literature was thoroughly searched in the relevant databases to identify studies published in this field during recent years. Special attention has been given to apalutamide clinical trials phases and its promising future as one of the first-line agents for the treatment of patients with advanced prostate cancer.
Results: Ongoing trials are progressing for apalutamide monotherapy and also for its combinations in other disease settings. The expected results of such trials will shape the future scenario of prostate cancer therapy.
Conclusion: This review article has highlighted different aspects of Apalutamide like its mechanism of action, adverse effects, pharmacokinetics, pharmacodynamics, clinical trials among others. The contents of this article should make an excellent read for prospective researchers in this field.
Keywords: Prostate cancer, nmCRPC, mHNPC, androgen receptor inhibitor, apalutamide, monotherapy.
Graphical Abstract
[http://dx.doi.org/10.3322/caac.21492] [PMID: 30207593]
[http://dx.doi.org/10.1080/14656566.2020.1770726] [PMID: 32543237]
[http://dx.doi.org/10.1200/EDBK_200319] [PMID: 30231323]
[http://dx.doi.org/10.1002/(SICI)1097-0142(19960101)77:1<138:AID-CNCR23>3.0.CO;2-5] [PMID: 8630920]
[http://dx.doi.org/10.7314/APJCP.2015.16.13.5137] [PMID: 26225642]
[http://dx.doi.org/10.1016/S0959-8049(01)00267-2] [PMID: 11602373]
[http://dx.doi.org/10.1016/j.ejca.2016.04.022] [PMID: 27267143]
[http://dx.doi.org/10.1007/BF02893851] [PMID: 16388315]
[http://dx.doi.org/10.1002/ijc.10188] [PMID: 11857418]
[http://dx.doi.org/10.1126/science.1117679] [PMID: 16254181]
[http://dx.doi.org/10.1093/jnci/89.5.385] [PMID: 9060961]
[http://dx.doi.org/10.1056/NEJMoa1715546] [PMID: 29420164]
[http://dx.doi.org/10.1111/ajco.12266] [PMID: 25227727]
[http://dx.doi.org/10.1007/s11427-015-4876-6] [PMID: 26025283]
[http://dx.doi.org/10.1186/1476-4598-5-17] [PMID: 16700911]
[http://dx.doi.org/10.2353/ajpath.2010.090521] [PMID: 19948822]
[http://dx.doi.org/10.4161/cc.8.24.10316]
[http://dx.doi.org/10.1002/pros.21065] [PMID: 19830782]
[http://dx.doi.org/10.2165/00003088-200443130-00003] [PMID: 15509184]
[http://dx.doi.org/10.1016/j.urolonc.2014.12.017] [PMID: 25797385]
[http://dx.doi.org/10.1177/106002809002400612] [PMID: 2193461]
[http://dx.doi.org/10.2165/00002512-199303010-00002] [PMID: 8453188]
[http://dx.doi.org/10.1158/0008-5472.CAN-11-3948] [PMID: 22266222]
[http://dx.doi.org/10.1097/CAD.0000000000000592] [PMID: 29381490]
[http://dx.doi.org/10.1080/14737140.2018.1503954] [PMID: 30101644]
[http://dx.doi.org/10.1177/1756287212452196] [PMID: 22852027]
[http://dx.doi.org/10.1097/PPO.0b013e318282635a] [PMID: 23337756]
[http://dx.doi.org/10.1200/JCO.2013.50.1684] [PMID: 24002508]
[http://dx.doi.org/10.1016/j.bmcl.2017.04.071] [PMID: 28478926]
[http://dx.doi.org/10.1016/S1470-2045(18)30456-X] [PMID: 30213449]
[http://dx.doi.org/10.1093/annonc/mdz397] [PMID: 31560066]
[http://dx.doi.org/10.1016/S1470-2045(19)30620-5] [PMID: 31578173]
[http://dx.doi.org/10.1093/annonc/mdv542] [PMID: 26578735]
[http://dx.doi.org/10.1007/s00280-018-3632-6] [PMID: 29974203]