Drug intelligence / Profile preview

palbociclib + CPX-351

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Oral, Intravenous
01

Overview

This combination therapy involves palbociclib, a small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), and CPX-351, a liposomal encapsulation of cytarabine and daunorubicin in a fixed 5:1 molar ratio. Palbociclib is used to induce G1 cell cycle arrest in acute myeloid leukemia (AML) cells, theoretically synchronizing them to increase their sensitivity to the S-phase specific cytotoxic effects of CPX-351. This approach is being investigated in Phase I/II trials led by Dr. Sudipto Mukherjee for patients with newly diagnosed or relapsed/refractory AML, particularly those with secondary AML or therapy-related AML. The liposomal delivery of CPX-351 allows for prolonged exposure and preferential uptake by bone marrow leukemia cells, while palbociclib acts as a cell cycle modulator to enhance the efficacy of the chemotherapy backbone.

Brand names
IbranceVyxeos
Other names
palbociclibCPX-351CPX351CPX 351liposomal cytarabine and daunorubicindaunorubicin and cytarabine liposome
02

Targets

DNACDK6 (Cyclin-dependent kinase 6)DNA polymerase familyCDK4 (Cyclin-dependent kinase 4)TOP2A (DNA topoisomerase II)

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