5
views
0
recommends
+1 Recommend
0 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: not found

      P-glycoprotein and breast cancer resistance protein restrict the brain penetration of the CDK4/6 inhibitor palbociclib.

      Read this article at

      ScienceOpenPublisherPubMed
      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          Palbociclib is a cyclin dependent kinase (CDK) 4/6 inhibitor with nanomolar potency and was recently approved for treatment of breast cancer. The drug may also be useful in glioblastoma (GBM) and diffuse intrinsic pontine gliomas (DIPG), which often have an activated CDK4/6-retinoblastoma signaling pathway. However, GBM and DIPG spread widely into the surrounding brain, which calls for a CDK4/6 inhibitor with sufficient blood-brain barrier penetration.

          Related collections

          Author and article information

          Journal
          Invest New Drugs
          Investigational new drugs
          1573-0646
          0167-6997
          Oct 2015
          : 33
          : 5
          Affiliations
          [1 ] Department of Bio-Pharmacology/ Mouse Cancer Clinic, The Netherlands Cancer Institute, AKL room C1.005, Plesmanlaan 121, 1066 CX, Amsterdam, The Netherlands.
          [2 ] Department of Neurosurgery, Qilu Hospital, Shandong University, Wenhua Xi Road 107, 250012, Jinan, People's Republic China.
          [3 ] Department of Pharmacy and Pharmacology, The Netherlands Cancer Institute /Slotervaart Hospital, Louwesweg 6, 1066 EC, Amsterdam, The Netherlands.
          [4 ] Division of Drug Toxicology, Faculty of Pharmacy, Division of Biomedical Analysis, Faculty of Science, Utrecht University, Sorbonnelaan 16, 3584 CA, Utrecht, The Netherlands.
          [5 ] Department of Bio-Pharmacology/ Mouse Cancer Clinic, The Netherlands Cancer Institute, AKL room C1.005, Plesmanlaan 121, 1066 CX, Amsterdam, The Netherlands. o.v.tellingen@nki.nl.
          Article
          10.1007/s10637-015-0266-y
          10.1007/s10637-015-0266-y
          26123925
          66818568-2512-4773-bf89-c93687d9631c

          ABC transporters, CDK4/6, Glioma, Palbociclib, Pharmacokinetics

          Comments

          Comment on this article