Genes recurrently altered, with targeted therapy approved or in clinical trials
| Name of altered gene . | No. of altered samples . | Potential therapeutic treatment . | Reference . |
|---|---|---|---|
| ABL1 | 3 | Dasatinib, Nilotinib, Ponatinib, AS703569, AT9283, Bafetinib, Bosutinib, Imatinib, XL228, Saracatinib | |
| ATM | 5 | Niraparib, Olaparib, BMN673, Rucaparib, Veliparib | 35 |
| BIRC3 (cIAP2) | 5 | AEG40826, TL 32711, AT-406, GDC0917, LCL161 | 36 |
| BRCA2# | 3 | Rucaparib, Olaparib, BMN673, E7449, Niraparib, Veliparib, | 37 |
| CD274 (PDL1) | 4 | MDX-1105, MPDL3280A, MDX-1105, RG7446 | 38 |
| CDK4 | 2 | PD0332991, Alvocidib, Palbociclib, LY2835219, BAY1000394, and others | 39 |
| JAK2 | 3 | Ruxolitinib, AZD1480, LY2784544, AT9283, SAR30250, INCB280503, TG101348, XL019, ITF2357, INCB018424 | 40 |
| PIM2 | 2 | SGI-1776 | 41,42 |
| UBE2A* | 6* | DKCI-73, Seliciclib (Roscovitine), CR8, P276-00, Dinaciclib (SCH727965), Alvocidib (Flavopiridol), SNS-032, BAY1000394 | 39,43 |
| WEE1 | 2 | MK-1775 | 44 |
| XPO1 | 5 | Selinexor (KPT-330) |
| Name of altered gene . | No. of altered samples . | Potential therapeutic treatment . | Reference . |
|---|---|---|---|
| ABL1 | 3 | Dasatinib, Nilotinib, Ponatinib, AS703569, AT9283, Bafetinib, Bosutinib, Imatinib, XL228, Saracatinib | |
| ATM | 5 | Niraparib, Olaparib, BMN673, Rucaparib, Veliparib | 35 |
| BIRC3 (cIAP2) | 5 | AEG40826, TL 32711, AT-406, GDC0917, LCL161 | 36 |
| BRCA2# | 3 | Rucaparib, Olaparib, BMN673, E7449, Niraparib, Veliparib, | 37 |
| CD274 (PDL1) | 4 | MDX-1105, MPDL3280A, MDX-1105, RG7446 | 38 |
| CDK4 | 2 | PD0332991, Alvocidib, Palbociclib, LY2835219, BAY1000394, and others | 39 |
| JAK2 | 3 | Ruxolitinib, AZD1480, LY2784544, AT9283, SAR30250, INCB280503, TG101348, XL019, ITF2357, INCB018424 | 40 |
| PIM2 | 2 | SGI-1776 | 41,42 |
| UBE2A* | 6* | DKCI-73, Seliciclib (Roscovitine), CR8, P276-00, Dinaciclib (SCH727965), Alvocidib (Flavopiridol), SNS-032, BAY1000394 | 39,43 |
| WEE1 | 2 | MK-1775 | 44 |
| XPO1 | 5 | Selinexor (KPT-330) |
Mutations in the BRCA2 gene render cells sensitive to poly(ADP-ribose) polymerase (PARP) inhibition; therefore, PARP inhibitors are listed.
UBE2A is amplified in 3 cases and there are splice-site alterations in 3 cases (1 case also has a nonsynonymous mutation). UBE2A is phosphorylated and activated by CDK9, for which inhibitors are available (note that SNS-032 and CDKI-73 are selective CDK9 inhibitors, whereas others inhibit multiple cyclin-dependent kinases).