A Phase I Study of Pelabresib (CPI-0610), a Small-Molecule Inhibitor of BET Proteins, in Patients with Relapsed or Refractory Lymphoma.
Kristie A BlumJeffrey G SupkoMichael B MarisIan W FlinnAndre H GoyAnas YounesSuresh BobbaAdrian M SenderowiczSergey EfuniRonda RippleyGozde ColakPatrick TrojerJeremy S AbramsonPublished in: Cancer research communications (2022)
BET proteins inhibition can potentially modify the pathogenic pathways which contribute to many diseases including malignancies. Pelabresib (CPI-0610), a potent and selective small molecule BET proteins inhibitor, has a MTD of 225 mg once daily for 14 days with a 7-day break, clear pharmacokinetic/pharmacodynamic relationship, and manageable clinical safety profile. These findings are part of the foundation for the ongoing pivotal study of pelabresib in patients with myelofibrosis.