Drug intelligence / Profile preview

bortezomib + thalidomide + prednisolone

Development stage
Phase 3
Lead developer
Takeda
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous (bortezomib), Oral (thalidomide), Oral (prednisolone)
01

Overview

Bortezomib + thalidomide + prednisolone is a combination regimen used primarily for the treatment of multiple myeloma, especially in patients who are not candidates for high-dose chemotherapy and stem cell transplantation.[7] - **Bortezomib** is a small molecule proteasome inhibitor that disrupts protein degradation in cancer cells, leading to cell cycle arrest and apoptosis. - **Thalidomide** acts as an immunomodulatory agent with anti-angiogenic effects; it inhibits tumor necrosis factor-alpha (TNF-α) and modulates the immune response. - **Prednisolone** is a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressive properties; it induces apoptosis in certain hematologic malignancies.[5][7] This regimen is typically used as part of first-line therapy for transplant-ineligible patients with multiple myeloma, with evidence supporting enhanced progression-free and overall survival when combined compared to two-drug regimens.[7] Most clinical studies of combination therapies also use melphalan with these agents (VMP or VMPT), but the combination of bortezomib, thalidomide, and prednisolone alone is pharmacologically rational and used when alkylators are contraindicated or not chosen.[5][7]

02

Targets

26S proteasomeCRBN (Cereblon)GR (Glucocorticoid receptor)TNFA (Tumor necrosis factor alpha (soluble))

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