Curis, Inc, a drug development company that is committed to leveraging its innovative signaling pathway drug technologies to create new medicines, announced that its scientists presented a poster entitled “Design and synthesis of quinazoline derivatives as novel, potent multi-acting HDAC and receptor tyrosine kinase inhibitors for the treatment of cancer,” at the 235th ACS National Meeting. The ACS National Meeting is being held from April 6th through the 10th.
The compound design and research underlying the development of proprietary drug compounds, belonging to a class of chemical structures called quinazonlines, was described at the presentation. The compounds were designed to inhibit multiple validated biological targets known to play key roles in the development and maintenance of certain cancers and inhibit the epidermal growth factor receptor (EGFR) and related family member, Her2. CUDC-101, Curis’ first development candidate from its targeted cancer drug development platform, emerged from this class of compounds and is the first-in-class inhibitor of EGFR, Her2 and HDAC.
Daniel R. Passeri, MSc., J.D., President and Chief Executive Officer said, “We are extremely pleased with the innovation of our scientists behind the design of this class of compounds, which includes CUDC-101, a drug candidate that we believe may represent a significant advancement over existing drugs that inhibit EGFR and/or Her2. With increasing trends toward combination therapies for the treatment of cancer, the targeting of EGFR, Her2 and HDAC in a single drug such as CUDC-101 could potentially provide cancer patients with the advantages of pathway synergies without the cost and administration burdens associated with the delivery of multiple separate drugs.”
The ACS presentation talked about the design of this chemical class, presenting structure and activity relationship requirements, as well as pre-clinical data demonstrating CUDC-101’s potency and efficacy across 30 different cancer cell lines and several animal xenograft models, including lung, liver, pancreas, colon, breast and other cancers. Of particular notice is CUDC-101’s compelling activity in preclinical xenograft cancer models of cell lines that are resistant to inhibitors that target only EGFR and/or Her2.
EGFR and Her2, members of a family of proteins called receptor tyrosine kinases (RTKs), have been known for their role in the uncontrolled growth and proliferation of tumor cells. Usually, drugs on the market or in development that particularly target EGFR and/or Her2 have faced problems of acquired drug resistance and limited responsiveness in patient populations. Curis’ unique approach aims to circumvent these issues by developing multi-targeted compounds that are chemically designed to inhibit EGFR, Her2 and HDAC activities simultaneously. Curis’ proprietary data and published reports have shown that HDAC inhibition might overcome some of the limitations of currently used receptor tyrosine kinase inhibitors by providing enhanced potency and potentially reducing the occurrence of drug resistance.
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