Drug intelligence / Profile preview

thalidomide + prednisone + bortezomib

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules, Irreversible 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

GR (Glucocorticoid receptor)CRBN (Cereblon)PSMB5 (Proteasome subunit beta Type-5)

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