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T-1101 is a novel, first-in-class small molecule oral agent developed for the treatment of cancer. It acts by specifically disrupting the interaction between Hec1 (highly expressed in cancer 1) and Nek2 (NIMA-related kinase 2), both of which are involved in mitotic regulation of cancer cells. This disruption leads to downregulation of Nek2, chromosomal misalignment, and subsequent apoptotic cell death in cancer cells. T-1101 has demonstrated potent anti-tumor effects in vitro across various cancer cell types—including breast, liver, leukemia, colorectal cancers—and multidrug-resistant lines. In animal models with liver and triple-negative breast cancers, it showed effective tumor growth inhibition. The drug is orally administered (capsule or powder form), offering advantages such as ease of use and improved patient compliance. Clinical trials have shown rapid absorption and favorable safety with no dose-limiting toxicities observed; the recommended Phase II dose is 200 mg/day. T-1101 has received FDA approval to initiate Phase II clinical trials for advanced neuroendocrine tumors after failure of standard treatments[1][6][7].
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