Drug intelligence / Profile preview

ibrutinib + carfilzomib + dexamethasone

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

Overview

**Ibrutinib + carfilzomib + dexamethasone** is a combination regimen studied for the treatment of relapsed/refractory multiple myeloma. \n- **Ibrutinib** is a first-in-class, oral small molecule inhibitor of Bruton's tyrosine kinase (BTK), blocking B-cell receptor signaling, impairing MM cell survival and proliferation[1][3][6][8]. \n- **Carfilzomib** is a second-generation proteasome inhibitor (PI), irreversibly inhibiting the chymotrypsin-like activity of the 20S proteasome (mainly via β5 and immunoproteasome LMP7 subunits), resulting in accumulation of proteins and induction of apoptosis in MM cells[2][3][7]. \n- **Dexamethasone** is a synthetic glucocorticoid, reducing inflammation and augmenting the antitumor response when used in MM treatment[1][3][6][8]. \nPreclinical and clinical data suggest synergistic activity between ibrutinib and carfilzomib, possibly by targeting distinct but complementary mechanisms of MM pathogenesis. The regimen has demonstrated efficacy (ORR ~67–72%) and manageable safety in phase 1/2 trials for relapsed/refractory multiple myeloma, including in high-risk (e.g., del17p, t(4;14)) and bortezomib-refractory subgroups[1][2][3][4][6]. The combination is not marketed as a single product, and dosing schedules are individualized in trials.

Other names
ibrutinib + carfilzomib + dexamethasone
02

Targets

GR (Glucocorticoid receptor)PSMB9 (Immunoproteasome subunit beta type-1i)PSMB5 (Proteasome subunit beta Type-5)BTK (Bruton tyrosine kinase)

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