A Phase I/II Study of the Investigational Drug Alisertib in Combination With Abiraterone and Prednisone for Patients With Metastatic Castration-Resistant Prostate Cancer Progressing on Abiraterone

Oncologist. 2016 Nov;21(11):1296-1297e. doi: 10.1634/theoncologist.2016-0297. Epub 2016 Oct 24.

Abstract

Lessons learned: Patients with metastatic castration-resistant prostate cancer did not tolerate the combination of alisertib with abiraterone and prednisone.There was no clear signal indicating that adding alisertib might be beneficial for those patients progressing on abiraterone.

Background: We hypothesized that Aurora A kinase (AK) contributes to castrate resistance in prostate cancer (PCa) and that inhibiting AK with alisertib can resensitize PCa cells to androgen receptor (AR) inhibitor abiraterone.

Methods: This was a phase I/II trial to determine the safety and efficacy of alisertib when given in combination with abiraterone plus prednisone (AP). Metastatic castration-resistant prostate cancer (mCRPC) patients were treated with dose escalation (alisertib at 30, 40, and 50 mg orally b.i.d., days 1-7 every 21 days) per standard 3+3 design.

Results: Nine of 43 planned subjects were enrolled. The maximum tolerated dose (MTD) was not reached, and the dose-limiting toxicities (DLTs) included neutropenic fever (1 of 9), neutropenia (1 of 9), fatigue with memory impairment (1 of 9), and diarrhea/mucositis (1 of 9). No prostate-specific antigen (PSA) decrease or circulating tumor cell (CTC) changes were observed during the study. Pharmacodynamically, adding alisertib did not affect total testosterone or dehydroepiandrosterone (DHEA) levels. There was some change in neuroendocrine markers after therapy. Mean duration on study was 2.5 months. The trial was terminated early.

Conclusion: A tolerable dose of alisertib in combination with AP in mCRPC was not established in this study. There was no clear signal indicating that alisertib might be beneficial for patients with mCRPC progressing on abiraterone.

作者总结

经验

• 转移性去势抵抗性前列腺癌患者不能耐受alisertib与阿比特龙和泼尼松的联合方案。

• 在接受阿比特龙治疗后发生进展的患者中, 尚无明确迹象表明联合alisertib治疗可带来临床获益。

摘要

背景. 假设Aurora A激酶(AK)可促成前列腺癌(PCa)发生去势抵抗, 而使用alisertib抑制AK可使PCa细胞对雄激素受体(AR)抑制剂阿比特龙治疗恢复敏感。

方法. 本项I/II期临床试验旨在确定alisertib联合阿比特龙和泼尼松(AP)治疗的安全性和有效性。研究为标准3+3设计, 转移性去势抵抗性前列腺癌(mCRPC)患者接受剂量递增治疗: alisertib 30、40和50 mg口服, 每日2次, 第1∼7天, 21天为一周期。

结果. 计划招募43例患者, 研究共纳入9例。本研究未达到最大耐受剂量(MTD), 剂量限制毒性(DLT)包括中性粒细胞减少性发热(1/9例)、中性粒细胞减少(1/9例)、疲乏伴记忆受损(1/9例), 以及腹泻/黏膜炎(1/9例)。研究期间未观察到前列腺特异性抗原(PSA)水平下降及循环肿瘤细胞(CTC)数量改变。从药效学上来说, 联合alisertib没有影响总睾酮或脱氢表雄酮(DHEA)水平。治疗后神经内分泌标记物有所变化。治疗平均时间为2.5个月。研究提早终止。

结论. 本研究未确立alisertib联合AP在mCRPC患者中的耐受剂量。没有明确的征象提示alisertib治疗可为阿比特龙治疗后发生进展的mCRPC患者带来临床获益。The Oncologist 2016;21:1296–1297e

Trial registration: ClinicalTrials.gov NCT01848067.

Publication types

  • Clinical Trial, Phase I
  • Clinical Trial, Phase II
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Aged, 80 and over
  • Androstenes / administration & dosage
  • Androstenes / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Aurora Kinase A / antagonists & inhibitors*
  • Azepines / administration & dosage*
  • Azepines / adverse effects
  • Humans
  • Male
  • Maximum Tolerated Dose
  • Middle Aged
  • Neoplasm Metastasis
  • Prednisone / administration & dosage
  • Prednisone / adverse effects
  • Prostatic Neoplasms, Castration-Resistant / drug therapy*
  • Pyrimidines / administration & dosage*
  • Pyrimidines / adverse effects
  • Testosterone / blood

Substances

  • Androstenes
  • Azepines
  • MLN 8237
  • Pyrimidines
  • Testosterone
  • Aurora Kinase A
  • abiraterone
  • Prednisone

Associated data

  • ClinicalTrials.gov/NCT01848067