Drug intelligence / Profile preview

bortezomib + melphalan + prednisolone

Development stage
Unknown
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

**bortezomib + melphalan + prednisolone** is a combination chemotherapy regimen used primarily for the treatment of multiple myeloma in patients who are not eligible for high-dose chemotherapy with autologous stem cell transplantation. - **Bortezomib** is a small molecule proteasome inhibitor that disrupts the 26S proteasome function, impairing protein degradation and leading to apoptosis in cancer cells. - **Melphalan** is an alkylating agent that crosslinks DNA and inhibits DNA and RNA synthesis, contributing to cytotoxicity, especially in dividing cells. - **Prednisolone** (often prednisone in the US) is a synthetic glucocorticoid with anti-inflammatory and antitumor properties, promoting apoptosis and suppressing the immune microenvironment in myeloma. The regimen (often known by the acronyms MPB or VMP) is typically administered in cycles involving oral melphalan and prednisolone for the first four days, and bortezomib by subcutaneous or intravenous injection on specified days per cycle. Multiple phase III clinical trials (VISTA, GIMEMA MM-03-05, GEM2005MAS65) have established its efficacy and tolerability, and the regimen remains a standard of care globally for transplant-ineligible newly diagnosed multiple myeloma[2][3][4][5].

Other names
bortezomib melphalan prednisoloneMPBVMPbortezomib/melphalan/prednisone
02

Targets

GR (Glucocorticoid receptor)DNAPSMB5 (Proteasome subunit beta Type-5)PSMB6 (Proteasome 20S subunit beta 6)PSMB9 (Immunoproteasome subunit beta type-1i)

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