Darolutamide as a Second-Generation Androgen Receptor Inhibitor in the Treatment of Prostate Cancer

(E-pub Ahead of Print)

Author(s): Ali Abbasi, Ahmad Movahedpour, Ahmad Amiri, Mohamad Samare Najaf, Zohreh MostafaviPour*

Journal Name: Current Molecular Medicine

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Prostate cancer (PC) is known as the most frequent cancer among men in the world. Androgen Deprivation Therapy (ADT) is one of the initial treatment approaches in the PC therapy and various drugs can be used in routine Hormonal therapy for PC therapy. Nevertheless, PC cells can survive and continue their growth via different mechanisms which lead to their resistance to common treatments i.e., Enzalutamide. Darolutamide (ODM-201) is a second-generation androgen receptor (AR) inhibitor with a new chemical structure and has a high affinity to the AR. Darolutamide doesn’t cross the bloodbrain barrier, for this reason, reduces the possibility of seizures. Darolutamide also can inhibit the transcriptional activity of several AR mutant variants (F877L, F877L/T878A, and H875Y/T878A) which are Enzalutamide resistant. In this review we reviewed the results of different studies: in vitro, animal model and phase 1, 2 and 3 clinical trials (ARADES, ARAFOR and ARAMIS). We shall discuss worldwide phase 2 and 3 clinical trials (ARASENS and ODENZA) that are in progress, in order to demonstrate the advantages of Darolutamide consumption in different groups of patients. Darolutamide has shown high potential in inhibiting the growth of MR49F (Enzalutamide resistant PC cells) and VCaP (Castration-resistant PC cells) cell lines and transcriptional activities of AR. Fewer doses of Darolutamide is needed compared to Enzalutamide. The drug had significant anti-tumor activity and had no effect on serum testosterone levels in animal models. Darolutamide demonstrates its safety and efficacy in different studies and was well tolerated nearly in all of the patients.

Keywords: Prostate cancer, Darolutamide, ODM-201, hormonal therapy, Castrate-resistant prostate cancer, Androgen receptor inhibitor, second-generation androgen receptor inhibitor

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(E-pub Ahead of Print)
DOI: 10.2174/1566524020666200903120344
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