This technology is a method of linking the cytotoxic cancer drugs epothilone B (Epo B) and dictyostatin to antibodies or other delivery systems for targeted cancer treatment.
Epo B and Dictyostatin are potent microtubule-stabilizing agents and are used therapeutically for the treatment of cancer. Strategies for the selective delivery of small molecule chemotherapeutic agents to tumor cells, such as antibody-drug conjugates (ADCs), hold promise as a way to increase their therapeutic specificity. An important hurdle for many of these approaches is the development of a strategy to link the drug to the selective agent, which requires identification of a site on the drug that may be modified without any deleterious impact on its activity. With their high potency, dictyostatin and Epo B are worthy candidates for linker strategy validation; however, there is currently no linker strategy available that retains the drugs’ cytotoxicity.
This technology is a method of linking Epo B and dictyostatin to antibodies or other targeted delivery systems. These Epo B and dictyostatin analogs were modified to incorporate a linker moiety capable of linking the drug to an agent, while maintaining or improving activity of the parent compound. As a result, these analogs provide a drug conjugate in which the analog is linked to various molecules, such as an antibody, polymer, lipid, albumin, reporter molecule, or imaging agent. These analogs offer a versatile and effective strategy to generate ADCs using the potent compounds Epo B and dictyostatin for targeted therapeutics with reduced interactions with healthy cells.
This technology has been validated in human cancer cell lines.
IR CU15319, CU15318
Licensing Contact: Beth Kauderer