Cyterix Pharmaceuticals

About

About Cyterix’s OncoCYP™-targeted prodrug discovery approach

Cytochrome P450 enzymes are highly expressed in normal tissue; for example, phase 1 metabolism in the liver is a major pharmacological liability for many drugs during development. However, the Human Genome Project has identified a cohort of extra-hepatic cytochrome P450s that are over-expressed during the malignant progression of most cancers (both solid and hematological malignancies) but not in normal tissue. This apparent tumor-specific expression of, so-called OncoCYP™ enzymes, make them encouraging targets for prodrug therapy. OncoCYP™ substrate specificity has been poorly understood making the design of prodrugs specifically activated by these enzymes a major challenge. Research at the University of Dundee in Scotland, supported by the Cancer Research UK, has generated a technology platform, now exclusively licensed worldwide to Cyterix Pharmaceuticals, Inc., that overcomes the design issue and has the potential to generate multiple classes of tumor-selective prodrug therapeutics. Such therapeutics are inactive in the prodrug form, but once activated by OncoCYP™ enzymes they fragment to release a ‘warhead’ which kill the tumor cells but spare the normal tissue. Since certain OncoCYP™ enzymes are expressed in the majority of tumor cells, an analogy would be ‘carpet and precision bombing’ of the tumor. Cyterix is currently developing two lead prodrugs bearing different potent cytotoxic warheads (which exhibit broad anti-tumor activity) where the ‘free’ drug is an approved agent where the safety and efficacy profile are well understood in the clinic. Cyterix plans to advance one or more of the existing lead prodrugs through IND-enabling studies into phase 1 clinical trials in cancer patients to acquire proof-of-concept. In addition, the company will expand the technology platform to validate additional OncoCYP™ enzyme targets and generate multiple new classes of tumor-selective prodrugs with improved therapeutic index.

Programs

Cyterix wants to advance one or more of the existing lead prodrugs through IND-enabling studies into phase 1 clinical trials in cancer patients to acquire proof-of-concept. In addition, the company will expand the technology platform to validate additional OncoCYP™ enzyme targets and generate multiple new classes of tumor-selective prodrugs with improved therapeutic index.

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