Drug intelligence / Profile preview

palbociclib + bortezomib + dexamethasone

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Combination regimen of palbociclib, bortezomib, and dexamethasone studied in relapsed/refractory multiple myeloma. Palbociclib is a selective small-molecule inhibitor of cyclin-dependent kinase 4 and 6 (CDK4/6), which causes cell cycle arrest in the G1 phase. Bortezomib is a small-molecule proteasome inhibitor that disrupts protein degradation, inducing apoptosis in cancer cells. Dexamethasone is a synthetic glucocorticoid with antitumor and anti-inflammatory properties that enhances the efficacy of antineoplastic regimens by promoting apoptosis. The combination is investigated to exploit cell cycle arrest (palbociclib), proteasome inhibition (bortezomib), and glucocorticoid-induced apoptosis (dexamethasone) in a synergistic fashion for multiple myeloma. In a phase 1/2 study, this sequential combination demonstrated manageable safety and antitumor activity in relapsed/refractory multiple myeloma[1][3][10].

Brand names
IbranceVelcadeDecadron
Other names
Palbociclib/Bortezomib/Dexamethasone triplet
02

Targets

26S proteasomeGR (Glucocorticoid receptor)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)

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