rigidin prodrug

The rigidin prodrug is a photoactivatable chemotherapy (PACT) agent consisting of a cytotoxic marine alkaloid rigidin analogue caged by coordination to a photosensitive ruthenium polypyridyl complex. In the dark, the coordinated ruthenium fragment prevents the rigidin analogue from binding to tubulin and inhibiting tubulin polymerization, thereby reducing systemic toxicity. Upon local irradiation with green or red light, photosubstitution of the thioether ligand by water occurs, releasing the active rigidin analogue. The released rigidin analogue acts as a microtubule-targeting agent that inhibits tubulin polymerization, leading to cell cycle arrest and apoptotic cell death. This prodrug has demonstrated significant antitumor efficacy in vivo in human lung cancer (A549) and uveal melanoma xenograft models, showing activity under both normoxic and hypoxic conditions.

Other names

caged rigidinphotoactivatable microtubule-targeting rigidin prodrugruthenium-based photocaged rigidinruthenium-caged rigidin