Table 4 List of developed inhibitors for pharmacological targeting of HOXA9 presented in this review
From: Role of HOXA9 in solid tumors: mechanistic insights and therapeutic potential
Targets | Inhibitors | Stage of development | PMID | References |
|---|---|---|---|---|
DOT1L inhibitors | EPZ004777 | Preclinical Stage | 21741596 | [109] |
SGC0946 | Preclinical Stage | 23250418 | [110] | |
EPZ-5676 | Phase I(NCT02141828) | 31790636 | [113] | |
SYC-522 | Preclinical Stage | 24858818 | [115] | |
LSD1 inhibitors | TCP | Phase I(NCT02273102) | 35914778; 32561840 | |
ORY-1001 | Phase I(NCT05546580) | 35914778; 29502954 | ||
GSK-2879552 | Phase I/II(NCT02929498) | 35914778; 29972300 | ||
INCB059872 | Phase I(NCT03132324) | 35914778 | [118] | |
IMG-7289 | Phase II(NCT04254978) | 35914778 | [118] | |
ORY-2001 | Phase II(NCT03867253) | 35914778 | [118] | |
SP2509 | Preclinical Stage | 24699304 | [122] | |
NCD38 | Preclinical Stage | 28210006 | [123] | |
JL1037 | Preclinical Stage | 28404874 | [124] | |
FY-56 | Preclinical Stage | 35051709 | [125] | |
Higenamine | Phase I(NCT01451229) | 33618250 | [126] | |
MS142 | Preclinical Stage | 30679800 | [127] | |
WDR5-MLL inhibitors | MM-101 | Preclinical Stage | 23210835 | [129] |
MM-102 | Preclinical Stage | 23210835 | [129] | |
MM-103 | Preclinical Stage | 23210835 | [129] | |
MM-589 | Preclinical Stage | 28603984 | [130] | |
MM-401 | Preclinical Stage | 28603984 | [130] | |
DDO-2084 | Preclinical Stage | 27598236 | [131] | |
OICR-9429 | Preclinical Stage | 34154613 | [132] | |
G9a inhibitors | DCG066 | Preclinical Stage | 27393948 | [134] |
BIX-01294 | Preclinical Stage | 34876693 | [135] | |
UNC0638 | Preclinical Stage | 29207160 | [136] | |
UNC0642 | Preclinical Stage | 30765842 | [137] | |
A-366 | Preclinical Stage | 34830365 | [139] | |
CM-272 | Preclinical Stage | 28548080 | [140] | |
Menin-MLL inhibitors | SNDX-5613 | Phase I/II(NCT05406817) | 35017466 | [144] |
KO-539 | Phase I/II(NCT04067336) | 36151141 | [145] | |
JNJ-75276617 | Phase I(NCT04811560) | – | – | |
BMF-219 | Phase I(NCT05153330) | – | – | |
M-1121 | Preclinical Stage | 34196551 | [146] | |
BET inhibitors | JQ-1 | Preclinical Stage | 35745584 | [148] |
I-BET151 | Preclinical Stage | 35745584 | [148] | |
AZD5153 | Phase I/II(NCT05253131) | 35399501 | [151] | |
BMS-986158 | Phase I(NCT03936465) | 36077617 | [152] | |
BI894999 | Phase I( NCT02516553) | 35444289 | [153] | |
GS-5829 | Phase I/II(NCT02983604) | 35816286 | [154] | |
GSK525762 | Phase II(NCT01943851) | 35681742 | [155] | |
ABBV-075 | Phase I(NCT02391480) | 36063752 | [156] | |
CPI-0610 | Phase I(NCT02157636) | 27890933 | [157] | |
INCB057643 | Phase I(NCT04279847) | 33396954 | [158] | |
OTX-015 | Phase I( NCT01713582) | 31632543 | [159] | |
PLX51107 | Phase I/II(NCT04910152) | 33504139 | [160] | |
INCB054329 | Phase I/II(NCT02431260) | 33148670 | [161] | |
FT-1101 | Phase I( NCT02543879) | 33574760 | [162] | |
CC-90010 | Phase I( NCT04047303) | 32240793 | [163] | |
ODM-207 | Phase I/II(NCT03035591) | 32989226 | [164] | |
CDK4/6 inhibitors | PD 0332991 | Phase I(NCT01701375) | 25744718 | [166] |
Abemaciclib | Phase II(NCT04169074) | 36174113 | [170] | |
Ribociclib | Phase II(NCT05163106) | 35972817 | [171] | |
Lerociclib | Phase II(NCT05085002) | 32130619 | [172] | |
Trilaciclib | Phase IV(NCT05071703) | 34887261 | [173] | |
Dinaciclib | Phase I(NCT03484520) | 34972202 | [174] | |
SHR6390 | Phase I( NCT05103826) | 33845905 | [175] |