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@ARTICLE{Jrvelinen:274561,
      author       = {H. A. Järveläinen and C. Schmithals and M. von Harten and
                      B. Kakoschky and T. J. Vogl and S. Harris and C. Henson and
                      G. Bullen-Clerkson and A. Piiper$^*$},
      title        = {{A}ssessment of the {P}harmacokinetics, {D}isposition, and
                      {D}uration of {A}ction of the {T}umour-{T}argeting {P}eptide
                      {CEND}-1.},
      journal      = {International journal of molecular sciences},
      volume       = {24},
      number       = {6},
      issn         = {1422-0067},
      address      = {Basel},
      publisher    = {Molecular Diversity Preservation International},
      reportid     = {DKFZ-2023-00638},
      pages        = {5700},
      year         = {2023},
      abstract     = {CEND-1 (iRGD) is a bifunctional cyclic peptide that can
                      modulate the solid tumour microenvironment, enhancing the
                      delivery and therapeutic index of co-administered
                      anti-cancer agents. This study explored CEND-1's
                      pharmacokinetic (PK) properties pre-clinically and
                      clinically, and assessed CEND-1 distribution, tumour
                      selectivity and duration of action in pre-clinical tumour
                      models. Its PK properties were assessed after intravenous
                      infusion of CEND-1 at various doses in animals (mice, rats,
                      dogs and monkeys) and patients with metastatic pancreatic
                      cancer. To assess tissue disposition, [3H]-CEND-1
                      radioligand was administered intravenously to mice bearing
                      orthotopic 4T1 mammary carcinoma, followed by tissue
                      measurement using quantitative whole-body autoradiography or
                      quantitative radioactivity analysis. The duration of the
                      tumour-penetrating effect of CEND-1 was evaluated by
                      assessing tumour accumulation of Evans blue and
                      gadolinium-based contrast agents in hepatocellular carcinoma
                      (HCC) mouse models. The plasma half-life was approximately
                      25 min in mice and 2 h in patients following intravenous
                      administration of CEND-1. [3H]-CEND-1 localised to the
                      tumour and several healthy tissues shortly after
                      administration but was cleared from most healthy tissues by
                      3 h. Despite the rapid systemic clearance, tumours retained
                      significant [3H]-CEND-1 several hours post-administration.
                      In mice with HCC, the tumour penetration activity remained
                      elevated for at least 24 h after the injection of a single
                      dose of CEND-1. These results indicate a favourable in vivo
                      PK profile of CEND-1 and a specific and sustained tumour
                      homing and tumour penetrability. Taken together, these data
                      suggest that even single injections of CEND-1 may elicit
                      long-lasting tumour PK improvements for co-administered
                      anti-cancer agents.},
      keywords     = {CEND-1 (Other) / LSTA1 (Other) / certepetide (Other) / iRGD
                      peptide (Other) / pharmacokinetics (Other) / quantitative
                      radioactivity analysis (QRA) (Other) / quantitative
                      whole-body autoradiography (QWBA) (Other)},
      cin          = {FM01},
      ddc          = {540},
      cid          = {I:(DE-He78)FM01-20160331},
      pnm          = {899 - ohne Topic (POF4-899)},
      pid          = {G:(DE-HGF)POF4-899},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:36982773},
      doi          = {10.3390/ijms24065700},
      url          = {https://inrepo02.dkfz.de/record/274561},
}