Darolutamide (Nubeqa)

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General information

Class/mechanism: Antiandrogen; non-steroidal androgen receptor inhibitor, non-steroidal antiandrogen (NSAA) that competitively inhibits androgens by binding to androgen receptors and exhibiting antitumor activity by blocking testosterone-induced nuclear translocation of androgen receptors.[1]
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, MedscapeUpToDate (courtesy of Lexicomp), or the prescribing information.

Preliminary data

Prostate cancer

  1. ARAMIS: Fizazi K, Shore N, Tammela TL, Ulys A, Vjaters E, Polyakov S, Jievaltas M, Luz M, Alekseev B, Kuss I, Kappeler C, Snapir A, Sarapohja T, Smith MR; ARAMIS Investigators. Darolutamide in nonmetastatic, castration-resistant prostate cancer. N Engl J Med. 2019 Mar 28;380(13):1235-1246. Epub 2019 Feb 14. link to original article PubMed

Also known as

  • Code name: BAY-1841788

References

  1. Moilanen AM, Riikonen R, Oksala R, Ravanti L, Aho E, Wohlfahrt G, Nykänen PS, Törmäkangas OP, Palvimo JJ, Kallio PJ. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. link to original article PubMed