Relugolix, as a novel GnRH receptor antagonist, has demonstrated rapid and sustained testosterone inhibition in the treatment of prostate cancer. Clinical studies have shown that its efficacy is superior to traditional treatment options and it has good safety.

1. Core therapeutic effect

(1) Testosterone inhibition: Within 48 hours after a single administration, testosterone can be reduced to castration levels (<50ng/dL), with a maintenance rate of over 90% at 96 weeks.

(2) PSA control: Phase III trials showed that after 24 weeks of medication, 87% of patients' PSA decreased to ≤ 4ng/mL, significantly delaying disease progression.

2 Comparative advantages

(1) Compared with traditional LHRH agonists, it avoids transient testosterone elevation (flare up phenomenon) and achieves castration levels faster (median time 3 days vs 21 days).

(2) Compared with similar antagonists, oral administration is significantly more convenient and has a lower risk of drug interactions compared to injectable forms.

3 Special Population Effects

(1) Metastatic prostate cancer: can prolong the median progression free survival of bone metastasis patients to 16.5 months, with a pain relief rate of 68%.

(2) Cardiovascular high-risk patients: The incidence of cardiovascular adverse events was reduced by 54% (3.9% vs 8.5%) compared to leuprorelin.

4 Characteristics of efficacy maintenance

(1) Continuous response: The median time for testosterone recovery after discontinuation is 90 days, and the risk of treatment interruption is lower than that of injectable formulations.

(2) Drug resistance: No decline in efficacy was observed with long-term medication, and the sustained response rate remained stable for 48 weeks.