Damid

Darolutamide is an androgen receptor (AR) inhibitor. It works in three ways: it competes with androgens for binding to the receptor, it blocks the receptor from moving into the cell nucleus, and it stops AR-mediated transcription.

Darolutamide has a major metabolite called keto-darolutamide, and in vitro this metabolite showed similar activity to Darolutamide itself. In vitro, Darolutamide also acted as a progesterone receptor (PR) antagonist, though only at approximately 1% of its activity against AR.

In laboratory studies, Darolutamide reduced the growth of prostate cancer cells in vitro. It also reduced tumor volume in mouse xenograft models of prostate cancer.

Darolutamide has not been shown to be safe or effective in females. Going by how the medicine works, it can harm an unborn baby and can cause loss of pregnancy. No animal studies on embryo and fetal development were done with Darolutamide, and there are no human data on its use in pregnant females.

There is no known specific antidote for Darolutamide overdose. The highest dose studied in clinical use was 900 mg twice daily, which makes a total daily dose of 1800 mg, and no dose limiting toxicities were seen at this dose.

Considering that absorption of Darolutamide is saturable and there is no evidence of acute toxicity, taking more than the recommended dose is not expected to cause systemic toxicity in patients with intact hepatic and renal function.

If a patient with severe renal impairment or moderate hepatic impairment takes more than the recommended dose and toxicity is suspected, interrupt Darolutamide treatment and give general supportive measures until the clinical toxicity has diminished or resolved. If toxicity is not suspected, Darolutamide treatment can continue with the next dose as scheduled.

Store Darolutamide at a temperature not above 25°C. Keep it away from light and from wet places. Keep it out of reach of children.