The functions and effects of Relugolix

Relugolix is a non-peptide small molecule potent gonadotropin-releasing hormone (GnRH) receptor antagonist that works through competitive inhibition and competes with natural GnRH to bind to the GnRH receptor in the anterior pituitary gland. Oral administration of regagliccan produce sustained and effective inhibitory effects on the hypothalamic-pituitary-gonadal axis. After initiation of treatment with Repagliflozin, luteinizing hormone (LH) and follicle-stimulating hormone (FSH) concentrations decrease rapidly, resulting in lower testosterone levels.

Contrary to what may occur with GnRH agonists, no initial increase in luteinizing hormone, follicle-stimulating hormone, and testosterone levels was observed upon initiating repagliflozin treatment. The effects of regaglic treatment on pituitary hormone levels are reversible, and luteinizing hormone and follicle-stimulating hormone levels return to physiological concentrations after cessation of regaglic. Testosterone levels may also return to baseline or normal levels after stopping treatment. Approximately 56% of patients achieved castrate-level testosterone concentrations (<50 ng/dL) on day 4 of treatment, and 97% maintained this level through 48 weeks of treatment. Repagolic needs to be taken orally once daily to maintain desired testosterone concentrations.

The original drug of Regogliflox has not yet been launched in the country, so it is not covered by medical insurance. There are European and Japanese versions of the original drug Rleglik available overseas. The ingredients of the two are basically the same. The price of the European version of 120mg*30 tablets per box may be around RMB 4,000, and the price of the Japanese version of 40mg*100 tablets per box may be around RMB 4,000 (the price may fluctuate due to exchange rates). Currently, there are no generic versions of Repagliflox produced and put on the market.