Safety and efficacy of fedratinib, a selective oral inhibitor of Janus kinase-2 (JAK2), in patients with myelofibrosis and low pretreatment platelet counts

Br J Haematol. 2022 Jul;198(2):317-327. doi: 10.1111/bjh.18207. Epub 2022 Apr 27.

Abstract

Fedratinib, an oral Janus kinase-2 (JAK2) inhibitor, is approved for patients with myelofibrosis (MF) and platelet counts ≥50 × 109 /l, based on outcomes from the phase 3, placebo-controlled JAKARTA trial in JAK-inhibitor-naïve MF, and the phase 2, single-arm JAKARTA2 trial in patients previously treated with ruxolitinib. We evaluated the efficacy and safety of fedratinib 400 mg/day in patients with baseline platelet counts 50 to <100 × 109 /l ("Low-Platelets" cohorts), including 14/96 patients (15%) in JAKARTA and 33/97 (34%) in JAKARTA2. At 24 weeks, spleen response rates were not significantly different between the Low-Platelets cohort and patients with baseline platelet counts ≥100 × 109 /l ("High-Platelets" cohort), in JAKARTA (36% vs. 49%, respectively; p = 0.37) or JAKARTA2 (36% vs. 28%; p = 0.41). Symptom response rates were also not statistically different between the Low- and High-Platelets cohorts. Fedratinib was generally well-tolerated in both platelet-count cohorts. New or worsening thrombocytopaenia was more frequent in the Low-Platelets (44%) versus the High-Platelets (9%) cohort, but no serious thrombocytopaenia events occurred. Thrombocytopaenia was typically managed with dose modifications; only 3/48 Low-Platelets patients discontinued fedratinib due to thrombocytopaenia. These data indicate that fedratinib 400 mg/day is safe and effective in patients with MF and low pretreatment platelet counts, and no initial fedratinib dose adjustment is required for these patients.

Keywords: JAK; fedratinib; myelofibrosis; platelets; thrombocytopaenia.

Publication types

  • Clinical Trial, Phase III
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Double-Blind Method
  • Humans
  • Janus Kinase 1
  • Janus Kinase 2
  • Nitriles / therapeutic use
  • Platelet Count
  • Primary Myelofibrosis* / diagnosis
  • Primary Myelofibrosis* / drug therapy
  • Protein Kinase Inhibitors / adverse effects
  • Pyrrolidines
  • Sulfonamides
  • Thrombocytopenia* / chemically induced
  • Thrombocytopenia* / drug therapy

Substances

  • Nitriles
  • Protein Kinase Inhibitors
  • Pyrrolidines
  • Sulfonamides
  • fedratinib
  • JAK2 protein, human
  • Janus Kinase 1
  • Janus Kinase 2