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CUDC-427
- Development stage
- Phase 1
- Lead developer
- Curis
- Modality
- Peptides, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
CUDC-427 is an orally bioavailable small molecule that acts as a second-generation pan-selective inhibitor of apoptosis protein (IAP) antagonist. It is designed to mimic the activity of the second mitochondrial-derived activator of caspases (Smac/DIABLO), binding to the Smac binding groove on IAPs such as XIAP and cellular IAPs 1 and 2. By inhibiting these proteins, CUDC-427 promotes apoptosis in tumor cells through activation of apoptotic signaling pathways. Preclinical studies demonstrated antitumor activity both as a single agent and in combination with chemotherapeutic agents or TRAIL receptor-targeting antibodies. The drug was developed for cancer indications including solid tumors and lymphomas, with phase I clinical trials showing manageable toxicity profiles but no further development reported beyond early-stage trials[1][3][4][5][6][8].
- Other names
- Smac mimetic CUDC-427
02
Targets
BIRC3 (Baculoviral IAP repeat-containing protein 3)XIAP (Baculoviral IAP repeat-containing protein 4)BIRC2 (Cellular inhibitor of apoptosis protein 1)
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