Drug intelligence / Profile preview

bortezomib + pirarubicin + dexamethasone

Development stage
Phase 4
Lead developer
Takeda
Modality
Small Molecules
Administration
Intravenous, Subcutaneous, Oral
01

Overview

This is a combination regimen consisting of three drugs—bortezomib, pirarubicin, and dexamethasone—used primarily in the treatment of hematologic malignancies such as multiple myeloma. - **Bortezomib** is a small molecule proteasome inhibitor that disrupts the 26S proteasome, leading to apoptosis in cancer cells by preventing degradation of pro-apoptotic factors. - **Pirarubicin** is an anthracycline antibiotic structurally related to doxorubicin; it intercalates into DNA and inhibits topoisomerase II, resulting in DNA damage and cell death. - **Dexamethasone** is a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressant properties; it induces apoptosis in certain lymphoid malignancies. The combination leverages complementary mechanisms for enhanced antitumor activity. While combinations like bortezomib + doxorubicin (another anthracycline) + dexamethasone are well-studied and approved for multiple myeloma[1][2][10], regimens substituting pirarubicin for doxorubicin are less common but mechanistically similar due to the close relationship between these two anthracyclines.

02

Targets

TOP2A (DNA topoisomerase II)GR (Glucocorticoid receptor)PSMB5 (Proteasome subunit beta Type-5)

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