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<p>One of the most significant challenges in developing new treatments for primary and metastatic brain tumors is the requirement for crossing the blood-brain barrier (BBB). By examining the brain penetration and spatial distribution of drug candidates in animal models, we can gain valuable insights into their potential for clinical success. In this study, we used multimodal imaging alongside complementary analytical methods to assess the brain distribution of two clinically advanced poly(ADP-ribose) polymerase (PARP) inhibitors—niraparib and olaparib—across three preclinical models: healthy brain (nonhuman primates (NHPs)), primary brain tumors (mouse glioblastoma), and metastatic brain tumors (mouse breast cancer metastasis). The results suggest that niraparib has a superior ability (relative to olaparib) to penetrate the BBB, distribute widely throughout the brain, and accumulate in brain tumor lesions. These findings support further studies of niraparib as a potential treatment for tumors in the human brain.</p>

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Assessment of brain penetration and tumor accumulation of niraparib and olaparib: insights from multimodal imaging in preclinical models

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年9月29日

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  • M. Reid Groseclose,
  • Jeremy A. Barry,
  • Tina Skedzielewski,
  • Yongle Pang,
  • Yinghe Li,
  • Gerald McDermott,
  • Jennifer Deutsch,
  • Chakravarthi Balabhadrapatruni,
  • William Benson,
  • David Lim,
  • Hoang Tran,
  • Elisabeth Minthorn,
  • Casey Kmett,
  • Theresa Roethke,
  • Shannon Berry,
  • Elaina McCormick,
  • William Feeney,
  • M. A. Ringenberg,
  • Sean Maguire,
  • Geeta Sharma,
  • Amine Aziez,
  • Elaine M. Paul,
  • Kunal Taskar,
  • Keyur Gada,
  • Hasan Alsaid

摘要

One of the most significant challenges in developing new treatments for primary and metastatic brain tumors is the requirement for crossing the blood-brain barrier (BBB). By examining the brain penetration and spatial distribution of drug candidates in animal models, we can gain valuable insights into their potential for clinical success. In this study, we used multimodal imaging alongside complementary analytical methods to assess the brain distribution of two clinically advanced poly(ADP-ribose) polymerase (PARP) inhibitors—niraparib and olaparib—across three preclinical models: healthy brain (nonhuman primates (NHPs)), primary brain tumors (mouse glioblastoma), and metastatic brain tumors (mouse breast cancer metastasis). The results suggest that niraparib has a superior ability (relative to olaparib) to penetrate the BBB, distribute widely throughout the brain, and accumulate in brain tumor lesions. These findings support further studies of niraparib as a potential treatment for tumors in the human brain.