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Staurosporine class compounds
Staralogs exhibit marked promise clinically but are hindered by suboptimal pharmacokinetic and toxicity profiles. However, Lemma scientists have developed an innovative patent pending method to load STS and UCN-01 into liposomes with almost 100% efficiency. Using liposomally encapsulated staurosporine, the class parent, Lemma has acquired physiological and biochemical data revealing a transformative degree of improvement in therapeutic index. Our targeting of the liposomes to tumor and tumor vessel markers has further enhanced tumor accumulation, tumor cell uptake, and potency. Lemma’s proprietary compositions and methods now enable clinical product development of liposomal staralogs and set the stage for a range of clinical opportunities in the oncology space. Our analyses indicate that these staralog formulations will have far reaching and very exciting prospects in terms of commercialization, as the market for brain, breast, prostate, and other solid tumors is very large.
The potency of staurosporine (STS) class compounds exceeds that of front-line anti-tumor agents and even kills chemotherapy resistant Jurkat cells. STS compounds, coined “staralogs” by Lopez* and colleagues are significantly more potent than many front line agents. Some staralogs have entered Phase I - III clinical trials for GBM and other CNS tumors, and although improved in terms of circulation and toxicity, most nonetheless still have stability and toxicity limitations. Staralogs however are extremely potent against all types of tumors as they engage a unique pattern of signaling pathways, driving caspase pathways of apoptosis, and inhibiting the phosphorylation of Akt, which is a key convergence node for intracellular signaling, proliferation, invasion, and apoptosis cascades, in tumor cells.