TABLE 2.
JAK inhibitors in clinical development for MF
| Drug | Target | Off-targets | Phase | Current status |
|---|---|---|---|---|
Momelotinib (CYT387)
|
JAK1, JAK2 | TYK2 | 3 | Recruiting |
Pacritinib (SB1518)
|
JAK2 | FLT3 | 3 | PERSIST-2 recruiting |
NS-018
|
JAK2 | Src family | 1/2 | Recruiting |
Fedratinib (SAR302503)
|
JAK2 | FLT3, RET | 3 | Drug development terminated due to adverse neurologic sequelae, including Wernicke’s encephalopathy |
AZD1480
|
JAK1, JAK2 | 1 | Study terminated following observed low-grade neurological toxicity | |
Lestaurtinib (CEP701)
|
JAK2 | FLT3, TrkA | 2 | Phased out of development in MF due to unacceptable GI toxicity and narrow therapeutic window |
BMS-911543
|
JAK2 | 1/2 | No longer in clinical development for MF due to high rate of drug discontinuation rate and questionable efficacy | |
Gandotinib (LY2784544)
|
JAK2 | 2 | No longer in clinical development for MF; high rate of renal insufficiency, tumor lysis | |
INCB039110
|
JAK1 | 2 | No longer in clinical development for MF |