TABLE 2
FROM:
JAK2 inhibitor therapy in myeloproliferative disorders: rationale, preclinical studies and ongoing clinical trials
A Pardanani
BACK TO ARTICLETable 2. Clinical trials with JAK2 inhibitors
| Inhibitor | Company | Phase in development | Indication | Route | Primary target |
|---|---|---|---|---|---|
| JAK2-selective | |||||
| INCB018424 | Incyte | Phase I/II (open) | PMFa | Oral | JAK2 |
| XL019 | Exelixis | Phase I (open) | PMFa | Oral | JAK2 |
| TG101348 | TargeGen | Phase I/II (pending) | PMFa | Oral | JAK2 |
| Non-JAK2 selective | |||||
| MK-0457 (VX680) | Merck | Phase I (open) Phase II (open) | Relapsed/refractory hematological malignancies, including JAK2V617F-positive MPD CML or Ph+ ALL with T315I mutation | i.v. | Aurora kinases (A, B, C) |
| CEP-701 (Lestaurtinib) | Cephalon | Phase II (open) | PMFa | Oral | FLT3 |
| AT9283 | Astex Therapeutics | Phase I/II (open) | Acute leukemias, CML, high-risk MDS or PMF | i.v. | Aurora kinases |
Abbreviations: ALL, acute lymphoblastic leukemia; CML, chronic myelogenous leukemia; EGFR, epidermal growth factor receptor; i.v., intravenous; JAK2, Janus kinase-2; MDS, myelodysplastic syndrome; MPD, myeloproliferative disorder; Ph, Philadelphia chromosome; PMF, primary myelofibrosis.
a Relapsed/refractory PMF, if newly diagnosed, then must have intermediate or high-risk PMF (Mayo Clinic or Dupriez criteria),66, 67 or symptomatic splenomegaly 
10 cm below costal margin.
