KZR-261 is the first clinical candidate to be nominated from our in-house research and discovery efforts targeting protein secretion pathways. KZR-261 is a broad-spectrum, anti-tumor agent that acts through direct interaction and inhibition of the Sec61 translocon. The compound was discovered at Kezar through a robust medicinal chemistry campaign in which several scaffolds were progressed through our proprietary platform evaluating Sec61 modulation.
KZR-261 has demonstrated several encouraging properties that lead to its potential to be an anti-cancer agent for the treatment of solid and hematologic malignancies. Pre-clinical data to date have shown that KZR-261 blocked expression of numerous therapeutically relevant cancer targets and inhibited tumor growth in vivo, pointing to its potential to be a combination therapy in a single drug.
Activities towards an Investigational New Drug (IND) application in the first quarter of 2021 are currently underway, and we expect to initiate a clinical trial with KZR-261 in solid tumors shortly thereafter.