Drug intelligence / Profile preview

prednimustine

Development stage
Phase 2
Lead developer
LEO Pharma
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Prednimustine is an orally administered **single-molecule ester prodrug** linking the nitrogen-mustard alkylating agent chlorambucil to the glucocorticoid prednisolone. Following esterase-mediated hydrolysis, it releases chlorambucil, which forms covalent DNA adducts and crosslinks that impair DNA replication and cell division, together with prednisolone, a glucocorticoid receptor agonist with lympholytic and anti-inflammatory activity. It was historically investigated and used in hematologic malignancies, including chronic lymphocytic leukemia and low-grade non-Hodgkin lymphoma, and was also studied in advanced breast cancer and small-cell lung cancer. ([pubchem.ncbi.nlm.nih.gov](https://pubchem.ncbi.nlm.nih.gov/compound/prednimustine))

Brand names
MostarinaSterecytStereocyt
Other names
prednisolone chlorambucil esterchlorambucil prednisolone esterprednisolone 21-[4-[p-[bis(2-chloroethyl)amino]phenyl]butyrate
02

Targets

GR (Glucocorticoid receptor)DNA

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