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Table 1 Summary of available inhibitors which target self-renewal pathways involved in myeloid malignancies

From: Targeting self-renewal pathways in myeloid malignancies

Pathway Name of drug Mode of action Producer Stage of clinical / non-clinical development Trial number
Wnt/GSK3β[2632] Aspirin / NSAIDs Complex / chemoprevention Generic Over the counter medications; no ongoing clinical  
Vitamin A Reduce TCF-β-catenin Generic trials in haematological malignancies
Non-clinical
Vitamin D complex formation Leo Non-clinical
(EB1089) Binding of β-catenin by Pharmaceuticals  
WNT1 and WNT2 vitamin D receptor   Non-clinical
McAbs Monoclonal antibodies Generic  
XAV939    Non-clinical
ZTM000990, Inhibits tankyrase 1&2 Novartis Non-clinical
PKF118-310, PKF118-744, PKF222-815, CGP049090, PNU-74654 ICG-001 NSC668036 SB-216763 Inhibit TCF-β-catenin Multiple Institute for Chemical Genomics Non-clinical Non-clinical
NCI Non-clinical
  complex   
Inhibits β-catenin/CREB-binding protein transcription
Inhibits dishevelled PDZ domain
  Inhibits GSK-3 Sigma  
GSK-3IX,   Chemicals Non-clinical
  Inhibit GSK-3 EMD  
alsterpaullone   Biosciences  
Notch[32, 33] MK-0752 γ-secretase inhibitor Merck Phase 1: T acute lymphoblastic leukemia NCT00100152
GSI-I, GSI-IX, GSI- γ-secretase inhibitors Calbiochem Non-clinical
X, GSI-XII, GSI- Monoclonal antibody Generic Non-clinical
XXI
NOTCH3 McAb
Hh[34] Cyclopamine SMO antagonist Generic Non-clinical  
  LDE225 SMO antagonist Novartis Phase 1: CML – in combination with Nilotinib NCT1456676
LEQ506 SMO antagonist Novartis Solid tumours only (phase I & II)  
GDC-0449 SMO antagonist Genentech Phase 1b: Myeloma in first remission or first relapse post ASCT NCT01330173
BMS-833923 SMO antagonist Bristol-Myers Squibb Phase 1: CML - in combination with Dasatinib NCT01218477
Phase 1b: Myeloma - in combination with Lenalidomide with Dexamethasone or Bortezomib with Dexamethasone NCT00884546
  IPI926 SMO antagonist Infinity Phase 2: Myelofibrosis NCT01371617
PF-04449913 SMO antagonist Pfizer Phase 1: CML - in combination with Dasatinib or Bosutinib NCT00953758
GANT61 Direct GLI inhibition Generic Non-clinical  
FOXO/TGFβ[35] Rapamycin Inhibitor of mTOR Generic No current clinical trials in haematological malignancies
LY294002 PI3K inhibitor
LY364947 PI3K inhibitor Merck Non-clinical
Merck Non-clinical
C-MYB[36] C-MYB AS ODN Infusional C-MYB anti-sense oligodeoxy nucleotides University of Pennsylvannia Phase 1 - In Advanced Hematological Malignancies NCT00780052