Drug intelligence / Profile preview

evofosfamide + dexamethasone + bortezomib

Development stage
Unknown
Lead developer
Molecular Templates
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Peptides
Administration
Intravenous, Subcutaneous, Oral
01

Overview

Evofosfamide (formerly known as TH-302) is a hypoxia-activated prodrug of the DNA alkylator bromo-isophosphoramide mustard. It is selectively activated under hypoxic conditions commonly found in the bone marrow microenvironment of multiple myeloma. Evofosfamide has been investigated in combination with dexamethasone and bortezomib for the treatment of relapsed/refractory multiple myeloma. Dexamethasone is a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressant properties, while bortezomib is a proteasome inhibitor that disrupts protein degradation pathways, leading to apoptosis in cancer cells. The combination aims to exploit synergistic effects by targeting both hypoxic tumor cells and proteasome-dependent survival mechanisms[1][2][5][6].

Brand names
Velcade
Other names
evofosfamide + dexamethasone + bortezomibTH-302 + dexamethasone + bortezomib
02

Targets

GR (Glucocorticoid receptor)DNAPSMB5 (Proteasome subunit beta Type-5)

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