CUDC-101

Purity >99%

The need for a potent receptor tyrosine kinase inhibitor in the treatment of different types of tumor cells has taken on enormous significance today. This has come about because of the multitude of responses to therapeutic agents that some tumors are exhibiting, as well as the particular nature of several of these tumors. The poor responses along with the gradual build-up of drug resistance in many tumors has caused a decrease in the effectiveness of many agents.

CUDC-101 was developed. It is able to target several inhibitors at the same time. Histone deacetylase, epidermal growth factor receptor (EGFR), and human epidermal growth factor 2 (HEGF2) are the principal ones identified so far. It has also shown itself to be very antagonistic against cancer cells. The CUDC-101 molecule is rather small, but novel in it's makeup. Because it can inhibit key receptors like histone deacetylase, EGFR and HEGF2, it was found to block key regulators of EGFR/HER2 signal paths. By blocking these signal pathways, this in turn lead to the creation of compensating pathways, like AKT, HER3, and MET.

Cancer cells were then able to escape the effects of the conventional inhibitors. CUDC-101 has also exhibited a very strong tendency to stop multiplication of tumor cells and displayed a pro-apoptotic response when it was used on a number of known cells that had previously been proved to be resistant to many conventional drugs. Because of this, it has been suggested that further studies on a broader scope using other tumor types is warranted.

On August 17, 2011, drug development company, Curis, Inc. announced the start of a Phase I combination trial of CUDC-101. The University of Colorado Cancer Treatment Center treated their first patient with a combination of radiation therapy, the chemotherapeutic drug, cisplatin, and CUDC-101. Patients in this initial study had a confirmed diagnosis of squamous cell carcinoma of the head or neck, primarily of the oral cavity, oropharynx, hypopharynx or larynx. Curis, Inc. has since then announced that in October of 2012, they had started Phase I trials of oral CUDC-101 in a cancer treatment center in Texas. A spokesman for Curis said that early responses to their initial trials have shown a favorable safety margin using the agent, and there have been good signs of therapeutic activity with CUDC-101. This news leaves CUDC-101 open to further studies in it's use in other types of tumors, including non-small cell carcinomas of the lung as well as gastric tumors.

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