Our client’s lead candidate is a novel targeted and dual-functional analog with significantly higher efficacy and markedly lower toxicity when compared to established first line treatments such as Irinotecan, Topotecan Etoposide, and Imatinib and targeted therapy drug called tyrosine kinase inhibitor (TKI) in the treatment of resistant colon and lung cancers, and CML. It produced 37.5% cure rate in mice bearing human CML xenografts that were highly resistant to Imatinib.
The lead candidate has proven to be very effective at killing human colon and lung cancer cells in vitro while also being remarkably effective at inhibiting the growth of human colon cancer xenografts. Perhaps most importantly, its toxicity is extremely low with a maximum tolerated dose (MTD) of 300 mg/kg (i.p.) and 180 mg/kg (i.v.) in mice, respectively. Its toxicity is much lower than that of Topotecan (MTD: 15 mg/kg, i.v. in mice), Etoposide (LD50: 15.07 mg/kg, i.v. in mice), Irinotecan (LD50: 132 mg/kg, i.v. in mice and other known clinically available drugs.