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Prostate Cancer and Darolutamide

Views:44     Author:Site Editor     Publish Time: 2020-12-23      Origin:Site

Disease background

Prostate cancer results from uncontrollable growth of cancer cells in the prostate gland. The prostate gland is located below the bladder and in front of the rectum, and is only found in males. Almost all prostate cancers (more than 95% of primary prostate cancers) develop from the gland cells and are known as adenocarcinomas (National Cancer Institute, 2017). Other types of prostate cancers (eg sarcomas, small cell carcinomas, neuroendocrine tumors, and transitional cell carcinomas) do exist, but are rare (American Cancer Society, 2016).


On a global scale, prostate cancer is the second most common cancer in men, and the fourth most common cancer overall. It is also the fifth leading cause of death from cancer among men. In 2012, the World Health Organization (WHO) estimated that 1.1 million men were diagnosed with prostate cancer globally, with almost 70% of cases occurring in more developed regions. Widespread use of prostate-specific antigen (PSA) testing followed by biopsy has contributed to higher incidence rates of diagnosed prostate cancer in more developed regions such as North America, Western Europe, and Northern Europe, but rates remain low in Eastern and South- Central Asian populations (GLOBOCAN, 2012).


There are often no symptoms associated with the development of prostate cancer, which is why PSA screenings are recommended. However, there are some instances when prostate cancer can cause symptoms. Some possible symptoms include:


•frequent urination with urgency, especially at night

•difficulty starting/stopping urination

•weak flow of urine

•difficulty in having an erection

•painful ejaculation; decrease in amount of fluid ejaculated

•painful or burning urination; blood in the urine or semen

•pain in the lower back, hips, pelvis, or thighs.


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Introduction of Darolutamide

Darolutamide was approved by FDA on Jul 30, 2019, and approved by the EMA on March 27, 2020, the trade name is Nubeqa. The drug was research by Orinon, the on Jun 2014, Bayer got the global development and commercial right in the world. Its molecular conformation is different from Enzalutamide and Apalutamide, and its unique chemical structure enables this drug to inhibit the growth of cancer cells by blocking the function of androgen receptors by blocking nuclear ectopic.


Nubeqa is Non-steroidal androgen receptor inhibitors, For the treatment of non-metastatic castration-resistant prostate cancer.


Nubeqa is oral tablet, 300mg of Darolutamide per tablet. 


Basic information of Darolutamide

Research code: ODM-201

Mechanism of action: Androgen receptor antagonists

Research status: approved

Structure: 


Prostate cancer and Darolutamide 2


Molecular weight: 398.85

Molecular structure: C19H19ClN6O2

CAS : 1297538-32-9


Glocal approval

Prostate cancer and Darolutamide 3


Prostate cancer and Darolutamide 4


Prostate Cancer and Darolutamide manufacturer


Route of systhetis


Prostate cancer and Darolutamide 6


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Related intermediates


79069-13-9

N-Boc-L-alaninol

1297537-37-1

2-Chloro-4-(1H-Pyrazol-5-Yl)Benzonitrile

1297537-41-7

(S)-4-(1-(2-aminopropyl)-1H-pyrazol-3-yl)-2-chlorobenzonitrile

1297537-45-1

5-ACETYL-1H-PYRAZOLE-3-CARBOXYLIC ACID


Therapeutic category competitors


Prostate cancer and Darolutamide 9

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