Targeted therapy

• NTRK inhibitors
  9 November 2019

  TRK inhibitors
  Examples
  larotrectinib / Vitrakvi
  entrectinib / Rozlytrek
  See also
  NTRKs NTRKs-rearranged tumors

• anti-MET targeted therapy
  4 May 2017

  See also
  MET
  targeted therapy

• CDK inhibitors
  14 December 2016

  CDK4/6 inhibitor
  |WKP|
  Examples
  abemaciclib is a CDK inhibitor selective for CDK4 and CDK6 .
  See also
  CDKs
  CDK4
  CDK6

• ROS1 inhibitors
  1 November 2016

  ROS1 inhibition; ROS1 Kinase Inhibitors
  ROS1 is a pivotal transmembrane receptor protein tyrosine kinase which regulates several cellular processes like apoptosis, survival, differentiation, proliferation, cell migration, and transformation.
  There is increasing evidence supporting that ROS1 plays an important role in different malignancies including glioblastoma, colorectal cancer, gastric adenocarcinoma, inflammatory myofibroblastic tumor, ovarian cancer, angiosarcoma, and non small cell (...)

• CTLA-4 blockade
  15 June 2016

  Targeted therapy
  anti-CTLA4s / CTLA-4 blockade ipilimumab tremelimumab
  CTLA4 blockade : Antagonists to increase immune activity
  There is increasing interest in the possible therapeutic benefits of blocking CTLA4 (using antagonistic antibodies against CTLA such as ipilimumab (FDA approved for melanoma in 2011) as a means of inhibiting immune system tolerance to tumours and thereby providing a potentially useful immunotherapy strategy for patients with cancer.
  Another (not yet approved) (...)

• WEE1 inhibitors
  10 June 2016

  WP
  Examples
  MK-1775
  Target
  WEE1 is a nuclear kinase belonging to the Ser/Thr family of protein kinases in the fission yeast Schizosaccharomyces pombe (S. pombe). It has a molecular mass of 96 kDa and it is a key regulator of cell cycle progression. It influences cell size by inhibiting the entry into mitosis, through inhibiting Cdk1. It has homologues in many other organisms, including mammals.
  The mitosis promoting factor MPF also regulates DNA-damage induced apoptosis. Negative (...)

• CCR2 inhibitors
  10 June 2016

  Examples
  CCX140-B
  CCX872
  Chemokine receptor CCR2 mediates monocyte mobilization from the bone marrow (BM) and subsequent migration into target tissues.
  CCR2 is highly expressed by inflammatory monocytes, dendritic cells, plasmacytoid dendritic cells and NK cells in all tissues.
  Results demonstrate the central role CCR2 plays in mediating leukocyte mobilization from the BM, and suggest a role for CCR2 inhibition in managing monocytes/macrophages-mediated chronic inflammatory (...)

• targeted immunotherapy
  10 June 2016

  Types
  CTLA-4 inhibitors
  PD-L1 inhibitors (immune checkpoint blockade )
  See also
  targeted therapy
  References
  http://www.nature.com/bjc/journal/v108/n8/full/bjc2013117a.html

• FAK inhibitors
  10 June 2016

  Definition : Small molecule FAK inhibitors decrease tumour growth and metastasis in several preclinical models and have initial clinical activity in patients with limited adverse events.
  The focal adhesion kinase (FAK) is a cytoplasmic protein tyrosine kinase that is overexpressed and activated in several advanced-stage solid cancers. FAK promotes tumour progression and metastasis through effects on cancer cells, as well as stromal cells of the tumour microenvironment. The (...)

• ERK inhibitors
  10 June 2016

  Members
  SCH772984
  VTX11e
  See also
  RAS-ERK pathway inhibitors RAF inhibitors MEK inhibitors ERK inhibitors
  References
  http://www.nature.com/nrd/journal/v13/n12/fig_tab/nrd4281_T1.html

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