Emerging targets and selected AML targeted agents
| Targets . | Emerging targeted agents . |
|---|---|
| Tyrosine and signaling kinases | Midostaurin, sorafenib, crenolanib, quizartinib, gilteritinib, and pacritinib (FLT3) |
| BGB324 (AXL) | |
| BKM120, BYL719, and TGR-1202 (PI3K) | |
| Trametinib (RAS) | |
| GSK2141795 (AKT) | |
| Cell cycle regulators | Alisertib and AZD1152 (aurora kinases) |
| Rigosertib (PLK1) | |
| MK-1775 (WEE1) | |
| Palbociclib, LEE011, and FLX-925 (CDK4/6) | |
| DNA methylation | AG120, IDH305, AG881, and FT-2102 (IDH1) |
| AG221 and AG881 (IDH2) | |
| Histone methylation | EPZ-5676 (MLL) |
| GSK2879552 (LSD1) | |
| BETs/epigenetic “readers” | OTX-015, CPI-0610, TEN-010, GSK525762, and INCB054329 |
| WNT pathway | PRI-724 |
| TP53 | ONC201 |
| Apoptosis regulators | Venetoclax (BCL2) |
| Birinapant (IAP) | |
| DS3032b, RO5503781, AMG232, and HDM201 (MDM2) |
| Targets . | Emerging targeted agents . |
|---|---|
| Tyrosine and signaling kinases | Midostaurin, sorafenib, crenolanib, quizartinib, gilteritinib, and pacritinib (FLT3) |
| BGB324 (AXL) | |
| BKM120, BYL719, and TGR-1202 (PI3K) | |
| Trametinib (RAS) | |
| GSK2141795 (AKT) | |
| Cell cycle regulators | Alisertib and AZD1152 (aurora kinases) |
| Rigosertib (PLK1) | |
| MK-1775 (WEE1) | |
| Palbociclib, LEE011, and FLX-925 (CDK4/6) | |
| DNA methylation | AG120, IDH305, AG881, and FT-2102 (IDH1) |
| AG221 and AG881 (IDH2) | |
| Histone methylation | EPZ-5676 (MLL) |
| GSK2879552 (LSD1) | |
| BETs/epigenetic “readers” | OTX-015, CPI-0610, TEN-010, GSK525762, and INCB054329 |
| WNT pathway | PRI-724 |
| TP53 | ONC201 |
| Apoptosis regulators | Venetoclax (BCL2) |
| Birinapant (IAP) | |
| DS3032b, RO5503781, AMG232, and HDM201 (MDM2) |
Selected agents are provided as examples; this is not an exhaustive list. Monoclonal antibodies and immunotherapies are outside the scope of this review.
BET, bromodomain and extraterminal domain family.