Drug intelligence / Profile preview

samarium-153 lexidronam pentasodium + bortezomib

Development stage
Unknown
Lead developer
CISBIO
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

This is a **combination therapy** of samarium-153 lexidronam pentasodium (a bone-seeking radiopharmaceutical, also known as Quadramet) and bortezomib (a proteasome inhibitor). **Samarium-153 lexidronam pentasodium** is a radiopharmaceutical that binds selectively to bone, especially areas of increased bone turnover such as bone metastases, where it delivers localized beta-radiation for cytotoxic effect. **Bortezomib** is a reversible inhibitor of the 26S proteasome, leading to disruption of cell signaling and induction of apoptosis, particularly in myeloma cells. The combination has been investigated in phase I studies for relapsed/refractory multiple myeloma, motivated by evidence that bortezomib can sensitize tumor cells to radiation, potentially increasing the cytotoxicity of samarium-153 lexidronam pentasodium[1][2][6]. Primary indication studied: multiple myeloma (relapsed/refractory).

Brand names
Quadramet (for samarium sm-153 lexidronam pentasodium)Velcade (for bortezomib)
Other names
153Sm-EDTMP + bortezomibsamarium Sm 153 lexidronam pentasodium + bortezomibQuadramet + bortezomib
02

Targets

PSMB5 (Proteasome subunit beta Type-5)

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