Birinapant is a small molecule peptidomimetic of SMAC that is mechanistically differentiated from other classes of cancer drugs. It potently and selectively antagonizes inhibitors of apoptosis proteins (IAPs), resulting in caspase-dependent apoptosis and inactivation of NF-κB survival signaling. Preclinical studies have shown that birinapant causes tumor-regressions as a single agent and that it has potent anti-tumor activity when combined with chemotherapies and death receptor ligands.
Birinapant Clinical Development
Birinapant is being developed for the treatment of both solid tumors and hematological malignancies. In Phase 1 clinical trials as a single agent and in combination with standard-of-care chemotherapies, birinapant has demonstrated strong correlation between drug exposure, target coverage and promising anti-tumor activity at well-tolerated doses in patients.
TetraLogic has an ongoing Phase 2 clinical program to demonstrate the therapeutic activity of birinapant in various cancers and has a biomarker program to develop validated assays to support randomized clinical trials.