E4206: AMG 706 and Octreotide in Patients with Low-Grade Neuroendocrine Tumors

Oncologist. 2018 Sep;23(9):1006-e104. doi: 10.1634/theoncologist.2018-0294. Epub 2018 May 31.

Abstract

Lessons learned: Rate of progression-free survival at a particular point in time, i.e., a landmark analysis, is a difficult endpoint for a heterogenous malignancy such as neuroendocrine cancer.Landmark analyses can also be complicated by evolution in the standard of care during the conduct of a clinical trial.Improvements in biomarker development would be useful in developing future clinical trials in NET to better tailor individualized therapies and assess for possible efficacy endpoints.

Background: Neuroendocrine tumors (NETs) are rare malignancies of the gastrointestinal (GI) tract that are highly vascularized and overexpress vascular-endothelial growth factor (VEGF). Sunitinib has demonstrated efficacy in the pancreatic subset of NET. This study explored the activity of another oral VEGF inhibitor, AMG 706 or motesanib, a multikinase inhibitor that targets receptor tyrosine kinases, including VEGFR1, VEGFR2, VEGFR3, KIT, RET, and PDGFR (IC50s = 2, 3, 6, 8, 59, and 84 nM, respectively).

Methods: This was a single-arm, first-line, phase II study run through the Eastern Cooperative Oncology Group. Patients with low-grade NET (as defined by central confirmation of Ki-67 of 0%-2%) were administered a flat dose of 125 mg per day orally combined with octreotide long acting-repeatable (LAR) for patients who had been on a stable dose. The primary objective was to determine the 4-month progression-free survival (PFS).

Results: Forty-four patients were evaluated per protocol. The 4-month PFS was 78.5%. The partial response rate was 13.6% (6/44), stable disease was 54.5% (24/44), 9.1% (4/44) had progressive disease, and 10/44 were not evaluable for response. Common toxicities included fatigue, hypertension, nausea, and headache, and most were grade 1-2. Median PFS was 8.7 months, and overall survival was 27.5 months.

Conclusion: Motesanib (AMG 706) demonstrated a 4-month PFS that met the per-protocol definition of efficacy. Fatigue and hypertension were the most common toxicities, and few grade 3-4 toxicities were encountered. The progression-free survival of 8.7 months in all NETs merits further study.

经验获取

• 在特定时间点的无进展生存率,如landmark分析,是神经内分泌癌等异质性恶性肿瘤的一个困难终点。

• Landmark分析也可因临床试验过程中医疗标准的演变而变得复杂。

• 生物标志物开发的改善将有助于未来在临床试验中更好地为NET制定个体化治疗,评估可能的疗效终点。

摘要

背景。 神经内分泌肿瘤 (NET) 是一种罕见的胃肠道 (GI) 恶性肿瘤,具有高度血管化和血管内皮生长因子 (VEGF) 过度表达的特点。舒尼替尼已证实在NET胰腺亚型中有效。本研究探讨了另一种口服VEGF抑制剂的活性,即 AMG 706或motesanib,是一种靶向受体酪氨酸激酶的多重激酶抑制剂,包括VEGFR1、VEGFR2、VEGFR3、KIT、RET和PDGFR(相应地,IC50=2、3、6、8、59和84nM)。

方法. 这是一项通过美国东部肿瘤协作组进行的单臂、一线、II期研究。对于低级别NET患者(定义为通过中心实验室确认的0%‐2%的Ki‐67),给予每天口服固定剂量125 mg,对于已经服用稳定剂量的患者,则联合长效缓释 (LAR) 奥曲肽。主要目标是确定4个月无进展生存期(PFS)。

结果。 按试验方案评估44例患者。4个月PFS为78.5%。部分缓解率为13.6%(6/44),疾病稳定率为54.5% (24/44),疾病进展率为9.1%(4/44),10/44不可评价。常见毒性包括疲劳、高血压、恶心和头痛,多数为1‐2级。PFS中位数为8.7个月,总生存期为27.5个月。

结论。 Motesanib(AMG 706)的4个月PFS符合方案界定的有效性。疲劳和高血压是最常见的毒性反应,很少出现3‐4级毒性。所有 NET 中8.7个月的无进展生存期值得进一步研究。

Trial registration: ClinicalTrials.gov NCT00427349.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Agents, Hormonal / pharmacology
  • Antineoplastic Agents, Hormonal / therapeutic use*
  • Humans
  • Indoles / pharmacology
  • Indoles / therapeutic use*
  • Middle Aged
  • Neuroendocrine Tumors / drug therapy*
  • Neuroendocrine Tumors / pathology
  • Niacinamide / administration & dosage*
  • Niacinamide / pharmacology
  • Niacinamide / therapeutic use
  • Octreotide / pharmacology
  • Octreotide / therapeutic use*
  • Treatment Outcome

Substances

  • Antineoplastic Agents, Hormonal
  • Indoles
  • Niacinamide
  • Octreotide
  • motesanib diphosphate

Associated data

  • ClinicalTrials.gov/NCT00427349