Drug intelligence / Profile preview

batimastat

Development stage
Discontinued
Lead developer
British Biotech
Modality
Peptides, Small Molecules
Administration
Intraperitoneal
01

Overview

Batimastat is a synthetic small molecule that acts as a broad-spectrum inhibitor of matrix metalloproteinases (MMPs), enzymes involved in the breakdown of extracellular matrix components. By inhibiting MMPs, batimastat exhibits antineoplastic and antiangiogenic activity, making it an angiogenesis inhibitor and antimetastatic agent. It was developed by British Biotech (now Vernalis) and was the first MMP inhibitor to enter clinical trials for cancer treatment. Batimastat reached Phase III clinical trials but was never marketed due to administration challenges; it cannot be given orally and intraperitoneal injection led to complications such as peritonitis. Its mechanism involves mimicking natural MMPI peptides, competitively binding to the active site of MMPs via its peptide backbone and hydroxamic acid group[1][2][3][4][5].

02

Targets

ACE (Angiotensin Converting Enzyme)ADAM17 (A disintegrin and metalloprotease 17)ADAM10 (Disintegrin and metalloproteinase domain-containing protein 10)MMP12 (Macrophage Metalloelastase)

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