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. Author manuscript; available in PMC: 2017 Jan 1.
Published in final edited form as: Cancer J. 2016 Jan-Feb;22(1):40–50. doi: 10.1097/PPO.0000000000000165

Table 6. Newer TKIs & non-TKIs under study for CML.

Agent Mode of action Activity in the presence
of mutations/
Preliminary data		 Phase of
development		 References
Omacetaxine
mepesuccinate
(Synribo)		 Semisynthetic formulation of homoharringtonine. The
mechanism of action includes inhibition of protein synthesis
leading to cell death.		 Not known/
CML-CP 18% MCR.		 Phase 3 71-74
MK 0457 Aurora kinase inhibitor T315I/
Minimal response in
clinical trials		 Phase 2 75
PHA-739358
(Danusertib)		 Pan aurora kinase inhibitor and third generation TKI T315I Phase 2 45
ABL001 Allosteric inhibitor of BCR-ABL prevents emergence of
resistant disease when administered in combination with
nilotinib		 Yes Phase 1 48
DCC-2036
(Rebastinib)		 TIE2, VEGFR1, BCR-ABL kinase inhibitor T315I Phase 1 46,47
AT9283 Aurora kinase inhibitor Yes Phase 1 76
BP5-087 STAT3 SH2 domain inhibitor combines with bcr-abl1
inhibition to overcome kinase-independent resistance in
chronic myeloid leukemia		 Yes Pre-clinical 77,78
ON012380 Non-ATP competitive inhibitor of BCR-ABL Unknown Pre-clinical 79
SGX70393 Azapyridine-based inhibitor of native and T315I-mutant
BCR-ABL kinase		 T315I Pre-clinical 80
TG101223 Small molecule BCR-ABL inhibitor T315I Pre-clinical 81
GNF-2/ GNF-5 Allosteric inhibitors of BCR-ABL T315I Pre-clinical 82
ESKM Human IgG1 T-cell receptor mimic monoclonal antibody
used alone or in combination with TKIs		 T315I Pre-clinical 83
U0126 MEK1/2 inhibitor reverses imatinib resistance through down-
regulating activation of Lyn/ERK signaling pathway in
imatinib-resistant K562R leukemia cells		 Yes Pre-clinical 84
KW-2449 Dual BCR-ABL Aurora kinase inhibitor Yes Pre-clinical 85,86