An Update on Triptorelin: Current Thinking on Androgen Deprivation Therapy for Prostate Cancer

Merseburger, Axel S.; Hupe, Marie C.

doi:10.1007/s12325-016-0351-4

Cited by 46 publications

(37 citation statements)

References 73 publications

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“…The main objective of any ADT is to rapidly suppress testosterone to castrate levels as elevated testosterone levels are associated with an increased risk of progression of prostate cancer [ 16 ]. Importantly, serum testosterone levels as low as 0.25 ng/mL indicate a good prognosis in patients with prostate cancer receiving ADT [ 17 ].…”

Section: Discussionmentioning

confidence: 99%

Efficacy and safety of degarelix in patients with prostate cancer: Results from a phase III study in China

Sun

Xie

et al. 2020

Asian Journal of Urology

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Objective To establish non-inferiority of gonadotropin-releasing hormone degarelix compared with goserelin in suppressing and maintaining castrate testosterone levels from Day 28 to Day 364 in Chinese patients with prostate cancer. Methods This is an open-label, multi-centre study in which men aged ≥18 years were randomised in a 1:1 ratio to once-a-month subcutaneous injection of either degarelix (240/80 mg) or goserelin (3.6 mg) for 12 months. The primary endpoint was difference in 1-year cumulative probability of suppressing testosterone to ≤0.5 ng/mL. Non-inferiority was to be established if the lower 95% confidence interval (CI) limit for difference in cumulative probability between the treatment arms was greater than −10%. Secondary endpoints included cumulative probability of prostate-specific-antigen-progression-free-survival (PSA-PFS). Safety was also assessed. Results Baseline demographics and disease characteristics were similar between degarelix ( n =142) and goserelin ( n =141) treatment arms. The difference in cumulative probability of maintaining castrate levels from Day 28–364 was 3.6% (95% CI:−1.5%, 8.7%), demonstrating non-inferiority of degarelix. The cumulative probability of PSA-PFS at Day 364 was higher for degarelix (82.3%, 95% CI: 74.7%, 87.7%) versus goserelin (71.7%, 95% CI: 63.2%, 78.5%, p =0.038). Adverse events (AEs) were similar between treatment arms, except for more injection site reactions with degarelix versus goserelin. Four (2.8%) and nine (6.4%) patients discontinued due to AEs in degarelix and goserelin groups, respectively. Conclusion Degarelix was non-inferior to goserelin in achieving and maintaining testosterone suppression at castrate levels during 1-year treatment. PSA-PFS was significantly higher with degarelix, suggesting improved disease control. Both treatments were well tolerated.

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Section: Discussionmentioning

confidence: 99%

Efficacy and safety of degarelix in patients with prostate cancer: Results from a phase III study in China

Sun

Xie

et al. 2020

Asian Journal of Urology

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“…In humans, the half-life of GnRH-I is only 2-5 minutes before cleavage by serum proteases; GnRH agonists, including triptorelin, can extend its half-life and increase binding to receptors [14]. In the treatment of prostate cancer, triptorelin is a first-line hormone therapy and can be efficacious and safe for patients with advanced prostate cancer [15].…”

Section: Discussionmentioning

confidence: 99%

Inhibitory Effect of GnRH and Its Analog on Tongue Cancer Cells Might Be Related to Downregulation of GnRHR mRNA

Li¹,

Wei²,

Yu-huan³

et al. 2020

CRC

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Aim: We investigated the expression of type-I gonadotropin-releasing hormone receptor (GnRHR-I) in human tongue cancer SCC-25 cells and the effects of gonadotropin-releasing hormone (GnRH)-I and its analog triptorelin on SCC-25 cells and the related mechanisms of action. Methods: We used RT-PCR, realtime PCR (qPCR) and western blotting to detect the expression of GnRHR-I mRNA and protein in SCC-25 cells, We also used a Cell Counting Kit-8 (CCK-8) assay to calculate cell viability, after treatment with GnRH-I or triptorelin. Results: Results of agarose gel electrophoresis and DNA sequencing showed that the GnRHR-I mRNA of SCC-25 cells were amplified correctly. Western blotting showed that the protein samples of SCC-25 cells had a specific reaction at approximately 60 kDa. GnRH or triptorelin inhibited the proliferation of SCC-25 cells in a dose-dependent manner. GnRH-I and triptorelin at the same concentrations did not significantly differ in inhibiting the proliferation of SCC-25 cells (10 µg/ml: P=0.44,20 µg/ml: P=0.57, 40µg/ml: P=0.28,80 µg/ml: P=0.051). Results of qPCR showed that triptorelin treatment led to stronger inhibition of GnRHR-I mRNA expression in SCC-25 cells than did GnRH-I treatment. (P<0.05). Triptorelin also decreased GnRHR mRNA expression time-dependently. Conclusion: The SCC-25 cell line expresses GnRHR protein and mRNA. The inhibitory effect of GnRH-I and triptorelin on tongue cancer cells might be related to the downregulation of GnRHR-I mRNA.

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“…Clinical trials have shown a reduction in serum testosterone levels below the castration level [45,46].…”

Section: Lhrh Agonistsmentioning

confidence: 99%

“…Overstimulation of LH release desensitizes and down regulates pituitary receptors for LHRH. Goserelin and triptorelin were accepted in the early 2000s [46,50]. LHRH agonists have shown similar effectiveness to surgical castration procedures in survival context.…”

Section: Abiraterone Acetatementioning

confidence: 99%

Previous, Current, and Future Pharmacotherapy and Diagnosis of Prostate Cancer—A Comprehensive Review

et al. 2019

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Prostate cancer (PCa) is one of the most common cancers in men that usually develops slowly. Since diagnostic methods improved in the last decade and are highly precise, more cancers are diagnosed at an early stage. Active surveillance or watchful waiting are appealing approaches for men diagnosed with low-risk prostate cancer, and they are an antidote to the overtreatment problem and unnecessary biopsies. However, treatment depends on individual circumstances of a patient. Older hormonal therapies based on first generation antiandrogens and steroids were widely used in metastatic castration-resistant prostate cancer (mCRPC) patients prior to the implementation of docetaxel. Nowadays, accordingly to randomized clinical trials, abiraterone, enzalutamide, apalutamide. and docetaxel became first line agents administrated in the treatment of mCRPC. Furthermore, radium-223 is an optional therapy for bone-only metastasis patients. Sipuleucel-T demonstrated an overall survival benefit. However, other novel immunotherapeutics showed limitations in monotherapy. Possible combinations of new vaccines or immune checkpoint blockers with enzalutamide, abiraterone, radium-223, or docetaxel are the subject of ongoing rivalry regarding optimal therapy of prostate cancer.

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An Update on Triptorelin: Current Thinking on Androgen Deprivation Therapy for Prostate Cancer

Cited by 46 publications

References 73 publications

Efficacy and safety of degarelix in patients with prostate cancer: Results from a phase III study in China

Efficacy and safety of degarelix in patients with prostate cancer: Results from a phase III study in China

Inhibitory Effect of GnRH and Its Analog on Tongue Cancer Cells Might Be Related to Downregulation of GnRHR mRNA

Previous, Current, and Future Pharmacotherapy and Diagnosis of Prostate Cancer—A Comprehensive Review

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