Effectiveness, pharmacokinetics, and safety of triptorelin acetate microspheres in patients with locally advanced and metastatic prostate cancer.
Wu. Guolan G; Zhou. Feng F; Wang. Haiping H; Liu. Kan K; Yu. Dexin D; Fan. Lianlian L; Han. Yangyun Y; Ai. Xiaohong X; Cao. Youhan Y; Wang. Xiaolin X; Wang. Sheng S; He. Chaohong C; Wu. Jitao J; Wu. Ji J; Wang. Youlei Y; Wang. Yanqing Y; Jin. Baiye B; Shentu. Jianzhong J
Key Findings
- 97.6% of patients reached testosterone <0.5 ng/mL by day 28 and stayed there through day 84
- 95.1% achieved even lower testosterone <0.2 ng/mL
- Monthly injections provided steady drug release with AUC values of 134.42 h·ng/mL (days 0‑28) and 154.72 h·ng/mL (days 56‑84)
- Most common side effects were mild liver enzyme increases, hot flashes, and occasional injection‑site pain
Practical Outcomes
- A single 3.75 mg triptorelin injection each month can be used to achieve strong, sustained testosterone suppression, which may be useful for medical hormone control. Expect mild liver‑related lab changes and hot flashes; monitor labs and symptoms. This regimen is designed for cancer patients and should only be used under medical supervision, not as a DIY anti‑aging shortcut.
Summary
A month‑long injectable form of triptorelin (3.75 mg) reliably lowered testosterone to castration levels in almost all prostate‑cancer patients, staying low for at least three months, and was generally well tolerated, though some people had mild liver enzyme rises, hot flashes, or injection‑site pain.
Abstract
A newly generic microspheres, sustained-release formulation of triptorelin acetate 3.75 mg has been developed. To evaluate the efficacy, pharmacokinetics, and safety of triptorelin 1-month formulation in Chinese patients with prostate cancer. An open-label, multicenter clinical trial with one arm testing a 1-month sustained-release triptorelin formulation in prostate cancer patients. Patients with prostate cancer received three consecutive 28-day injections of triptorelin acetate. The primary endpoint was the proportion of successful patients over the total number of evaluable patients. Treatment success was defined as testosterone suppression below the clinical castration level (i.e., <0.5 ng/mL) at day 28 and maintenance of clinical castration until study completion (day 84). The frequency of patients with testosterone concentrations <0.2 ng/mL was also studied. The study included 125 patients. All 125 patients received at least one dose of the study drug and 122 completed the study. The successful patient proportion among the evaluable patients was 97.6% (122/125; 95% CI, 92.7-99.2). 95.1% (116/122) achieved testosterone concentrations <0.2 ng/mL. The pharmacokinetic profile of triptorelin during the first 3 months of treatment, evaluated in a subset of the study population (<i>n</i> = 11), showed sustained release of triptorelin from the formulation. Values for AUC<sub>0-τ</sub> calculated from day 0 to 28, and day 56 to 84 were 134.42 (28.76), and 154.72 (21.86) h*ng/mL, respectively. The most common treatment-related adverse events were increased alanine aminotransferase (18.4%), increased aspartate aminotransferase (16.0%), and hot flashes (9.6%). Prolonged QT interval on electrocardiogram, erectile dysfunction, and decreased libido each occurred in ⩽4% of the patients. The frequently reported local adverse reaction was pain at the injection site, experienced by 2.4% (3/125) of the patients. 3.75-mg Triptorelin acetate microspheres for injection were effective in achieving and maintaining testosterone suppression and were well tolerated in patients with prostate cancer. chictr.org.cn (ChiCTR2000033188).
Study Information
pubmed
2024
2024-12-23T00:00:00.000Z
10.1177/17588359241307818
29