Albert Einstein College of Medicine, Departments of Oncology and Urology, Montefiore Einstein Center for Cancer Care, Montefiore Medical Center, New York, NY, USA.
Departments of Radiation Oncology & Urology, University of California San Francisco (UCSF) Helen Diller Family Comprehensive Cancer Center (HDFCC), San Francisco, CA, USA.
Invest New Drugs. 2021 Apr;39(2):499-508. doi: 10.1007/s10637-020-00993-4. Epub 2020 Sep 13.
Background Androgen deprivation therapy (ADT) is a standard treatment for high-risk biochemically-recurrent, non-metastatic prostate cancer (BRPC) but is not curative and associated with toxicity. Racemetyrosine (SM-88) is an amino-acid analogue used with methoxsalen, phenytoin, and sirolimus (MPS) to enhance SM-88 activity. Method A phase 1b/2, open-label trial in BRPC and rising PSA. Patients were given daily SM-88 (230 mg BID), methoxsalen (10 mg), phenytoin (50 mg), and sirolimus (0.5 mg)). Outcome measures included changes in PSA, circulating tumor cells (CTCs) and imaging. Results 34 subjects were screened, 23 treated and 21 remained on study for ≥12 weeks. The median PSA was 6.4 ng/ml (range 1.7-80.1); doubling-time 6.2 months (range 1.4-36.6) and baseline testosterone 319.1 ng/ml (range 2.5-913.7). Median duration of therapy was 6.5 months (2.6-14.0). CTCs (median 48.5 cells/4 ml (range 15-268) at baseline) decreased a median of 65.3% in 18 of 19 patients. For patients who achieved an absolute CTC nadir count of <10 cells/4 ml (n = 10), disease control was 100% i.e. no metastases or PSA progression, while on trial (p = 0.005). PSA fell by ≥50% in 4.3% (1 subject). No patients developed metastatic disease while on treatment (metastases free survival =100%). There were no treatment-related adverse events (AEs) and quality of life was unchanged from baseline on the EORTC QLQ-C30 and QLQ-PR25. Testosterone levels rose slightly on SM-88 and were unrelated to efficacy or toxicity. Conclusions Use of SM-88 was associated with disease control while maintaining QOL. SM-88 may delay the need for ADT and the associated hormonal side effects. Larger trials are planned.Trial registration number, date of registration - NCT02796898, June 13, 2016.
雄激素剥夺疗法(ADT)是治疗高风险生化复发性非转移性前列腺癌(BRPC)的标准治疗方法,但并非治愈性治疗,且与毒性相关。Racemetyrosine(SM-88)是一种氨基酸类似物,与甲氧基补骨脂素、苯妥英和西罗莫司(MPS)联合使用以增强 SM-88 的活性。
BRPC 和 PSA 升高患者的 1b/2 期、开放标签试验。患者每日给予 SM-88(230mg 每日 2 次)、甲氧基补骨脂素(10mg)、苯妥英(50mg)和西罗莫司(0.5mg)。观察指标包括 PSA、循环肿瘤细胞(CTC)和影像学的变化。
34 例患者进行了筛选,23 例接受治疗,21 例至少接受治疗 12 周。中位 PSA 为 6.4ng/ml(范围 1.7-80.1);倍增时间 6.2 个月(范围 1.4-36.6),基线睾酮为 319.1ng/ml(范围 2.5-913.7)。中位治疗时间为 6.5 个月(2.6-14.0)。CTC(基线时中位数 48.5 个细胞/4ml(范围 15-268))在 19 例患者中有 18 例下降了中位数 65.3%。对于在试验期间达到绝对 CTC 最低计数<10 个细胞/4ml(n=10)的患者,疾病控制率为 100%,即无转移或 PSA 进展(p=0.005)。PSA 下降≥50%的患者占 4.3%(1 例)。在治疗期间没有患者发生转移性疾病(无转移生存=100%)。治疗期间无治疗相关不良事件(AE),EORTC QLQ-C30 和 QLQ-PR25 量表的生活质量与基线相比无变化。SM-88 治疗后睾酮水平略有升高,但与疗效或毒性无关。
SM-88 的使用与疾病控制相关,同时保持生活质量。SM-88 可能延迟 ADT 的需求和相关的激素副作用。计划进行更大规模的试验。试验注册号,注册日期-NCT02796898,2016 年 6 月 13 日。