rebimastat

Rebimastat is a sulfhydryl-based, second-generation, broad-spectrum matrix metalloproteinase (MMP) inhibitor developed as an investigational antineoplastic agent. It was designed to inhibit several zinc-dependent MMPs—including MMP1, MMP2, MMP7, MMP9, and MMP14—which are enzymes involved in the degradation of the extracellular matrix (ECM). By binding to the catalytic zinc ion within these enzymes' active sites, rebimastat aimed to disrupt processes such as angiogenesis (formation of new blood vessels), tumor invasion, and metastasis. Its "sheddase-sparing" design sought to minimize inhibition of ADAMs (a disintegrin and metalloproteinases), potentially reducing side effects seen with earlier inhibitors. Rebimastat was investigated for use in various cancers including prostate cancer, non-small cell lung cancer, breast cancer, and HIV-related Kaposi’s sarcoma. Despite promising preclinical results and multiple phase II/III trials completed or attempted in these indications, clinical development was ultimately discontinued due to adverse effects and lack of efficacy improvements[2][3][4][5][7].

Other names

rebimastat