Drug intelligence / Profile preview

bortezomib

Development stage
Approved
Lead developer
Millennium Pharmaceuticals
Modality
Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Subcutaneous, Intravenous
01

Overview

Bortezomib is a first-in-class small molecule proteasome inhibitor developed for cancer therapy. It reversibly inhibits the 26S proteasome by targeting the threonine residue of its 20S catalytic core, leading to disruption of protein degradation pathways essential for cell cycle progression and survival in malignant cells. This results in apoptosis and inhibition of tumor growth. Bortezomib is primarily indicated for multiple myeloma (including newly diagnosed and relapsed/refractory cases) and mantle cell lymphoma (MCL), including patients unsuitable for stem cell transplantation. It can be used as monotherapy or in combination with other agents such as dexamethasone or prednisone[1][2][3][6]. The drug was originally developed by Millennium Pharmaceuticals and is marketed under the brand name Velcade; it has been approved since 2003 in major markets including the US, China, and Europe[1][2][6]. Administration routes include intravenous injection and subcutaneous injection[1][2].

Brand names
Velcade万珂万科
Other names
硼替佐米
02

Targets

PSMB5 (Proteasome subunit beta Type-5)

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