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thalidomide + prednisone + bortezomib
- Development stage
- Phase 3
- Lead developer
- Bristol Myers Squibb
- Modality
- Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral, Intravenous, Subcutaneous
01
Overview
This is a combination regimen consisting of thalidomide, prednisone, and bortezomib. Thalidomide is an immunomodulatory agent with anti-angiogenic and anti-neoplastic properties; it inhibits tumor necrosis factor-alpha (TNF-α), modulates immune response, and impairs blood vessel formation in tumors. Prednisone is a synthetic glucocorticoid corticosteroid that exerts anti-inflammatory and immunosuppressive effects by binding to the glucocorticoid receptor. Bortezomib is a small molecule proteasome inhibitor that disrupts the 26S proteasome, leading to accumulation of proteins within cells and subsequent apoptosis, particularly in malignant plasma cells. This combination has been studied primarily for the treatment of multiple myeloma in patients who are not eligible for autologous stem cell transplantation[1][2][3].
02
Targets
CRBN (Cereblon)GR (Glucocorticoid receptor)PSMB5 (Proteasome subunit beta Type-5)TNFA (Tumor necrosis factor alpha (soluble))
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