Drug intelligence / Profile preview

bortezomib + pirarubicin + dexamethasone

Development stage
Preclinical
Lead developer
Millennium Pharmaceuticals
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

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

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