Drug intelligence / Profile preview

PRT2527

Development stage
Phase 1
Lead developer
Prelude Therapeutics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

PRT2527 is a potent and highly selective small molecule inhibitor of cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the RNA polymerase II elongation factor positive transcription elongation factor b (P-TEFb). By inhibiting CDK9, PRT2527 disrupts transcriptional regulation critical for cancer cell survival, leading to antineoplastic effects. It is being developed primarily for hematologic malignancies such as relapsed/refractory lymphoid cancers—including diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), peripheral T-cell lymphoma (PTCL), chronic lymphocytic leukemia (CLL), Richter syndrome—as well as advanced solid tumors and acute myeloid leukemia. The drug has shown preliminary clinical activity both as monotherapy and in combination with zanubrutinib, with an acceptable safety profile in early-phase trials[1][2][3][5][6][8][10].

02

Targets

CDK9 (Cyclin-dependent kinase 9)

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