Darolutamide (Nubeqa)

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]^[2]^[3]^[4]
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, Medscape UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

Prostate cancer

Patient drug information

History of changes in FDA indication

2019-07-30: Initial approval for non-metastatic castration-resistant prostate cancer. (Based on ARAMIS)
2022-08-05: Approved in combination with docetaxel for adult patients with metastatic hormone-sensitive prostate cancer (mHSPC). (Based on ARASENS)

History of changes in EMA indication

2020-03-27: Initial authorization as Nubeqa. Nubeqa is indicated for the treatment of adult men with non metastatic castration resistant prostate cancer (nmCRPC) who are at risk of developing metastatic disease. (Based on ARAMIS)
2023-03-20: Additional indication for metastatic hormone sensitive prostate cancer (mHSPC) in combination with docetaxel and androgen deprivation therapy. (Based on ARASENS)

History of changes in Health Canada indication

2020-02-20: Notice of compliance for the treatment of patients with non-metastatic castration resistant prostate cancer (nmCRPC).
2022-09-29: New indication (details unknown)

History of changes in PMDA indications

2020-01-23: Newly indicated for the treatment of non-metastatic, castration-resistant prostate cancer.

Also known as

Code name: BAY-1841788, ODM-201
Brand name: Nubeqa

References

↑ ^1.0 ^1.1 Darolutamide (Nubeqa) package insert
↑ Darolutamide (Nubeqa) package insert (locally hosted backup)
↑ Nubeqa manufacturer's website
↑ 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
↑ Darolutamide (Nubeqa) patient drug information (Chemocare)
↑ Darolutamide (Nubeqa) patient drug information (UpToDate)

[insert-1] 1.0 ^1.1 Darolutamide (Nubeqa) package insert

[2] Darolutamide (Nubeqa) package insert (locally hosted backup)

[3] Nubeqa manufacturer's website

[4] 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

[5] Darolutamide (Nubeqa) patient drug information (Chemocare)

[6] Darolutamide (Nubeqa) patient drug information (UpToDate)

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