Drug intelligence / Profile preview

ARRY-520 + bortezomib + dexamethasone

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Subcutaneous, Oral
01

Overview

**ARRY-520 + bortezomib + dexamethasone** is an investigational combination regimen for relapsed or refractory multiple myeloma and plasma cell leukemia. **ARRY-520 (filanesib)** is a highly selective inhibitor of kinesin spindle protein (KSP/Eg5), leading to mitotic arrest and apoptosis in dividing cells. **Bortezomib** is a small molecule proteasome inhibitor, disrupting protein degradation and promoting cancer cell death. **Dexamethasone** is a corticosteroid with anti-inflammatory and antimyeloma activity. The combination leverages ARRY-520's cytostatic action, bortezomib's inhibition of proteasomal degradation, and dexamethasone's apoptotic and immunosuppressive effects. Developed and studied by Array BioPharma, the three-drug regimen has been investigated in phase 1 trials for relapsed/refractory multiple myeloma, showing manageable safety, hematologic toxicity (notably neutropenia and anemia), and initial efficacy with overall response rates up to 43% in small expansion cohorts[1][7].

Other names
filanesib + bortezomib + dexamethasone
02

Targets

KIF11 (Kinesin Spindle Protein)GR (Glucocorticoid receptor)PSMB5 (Proteasome subunit beta Type-5)

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