Drug intelligence / Profile preview

filanesib + carfilzomib

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

**Filanesib + carfilzomib** is an investigational combination regimen for relapsed or refractory multiple myeloma. Filanesib (ARRY-520) is a small molecule inhibitor of kinesin spindle protein (KSP), essential for mitotic spindle formation and, thus, cell division. Its activity leads to cell cycle arrest and apoptosis, in part by causing rapid depletion of the antiapoptotic protein Mcl-1, critical for the survival of myeloma cells[1][3][5]. Carfilzomib is a second-generation small molecule proteasome inhibitor that irreversibly binds to the chymotrypsin-like activity of the 20S proteasome core, leading to accumulation of unfolded proteins, apoptosis, and cell death[2][4]. In combination, these agents have demonstrated manageable safety and encouraging clinical efficacy in phase 1 studies for patients with relapsed/refractory multiple myeloma, including those refractory to other proteasome inhibitors[1][3][5].

Other names
filanesib plus carfilzomibARRY-520 plus carfilzomibARRY520 plus carfilzomibARRY 520 plus carfilzomib
02

Targets

KIF11 (Kinesin Spindle Protein)PSMB1 (26S Proteasome (β1-Subunit))PSMB5 (Proteasome subunit beta Type-5)PSMB10 (Proteasome subunit beta type-10)PSMB2 (Proteasome subunit beta type-2)PSMB9 (Immunoproteasome subunit beta type-1i)

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