Silimitasertib

 

CX-4945 is a potent and selective inhibitor of CK2 to which Cylene owns all IP. As a small molecule with drug-like physicochemical properties and ease of synthesis, it has flexible routes and schedules of administration. Although designed for use as a combination agent, CX-4945 represents the first CK2 inhibitor to enter the clinic, therefore the Phase I setting was used to de-risk this new class of agent. A successful Phase I clinical trial demonstrated that it has favorable safety, pharmacokinetic and pharmacodynamic characteristics. CX-4945 hits the CK2 target and it modulated the expected pathways without displaying toxicity. The monitoring of circulating tumor cells demonstrated the ability of CX-4945 to kill tumor cells in patients which supports the observation that CX-4945 achieved clinical benefit as a single agent CK2 inhibitor, demonstrating stable disease and extended duration on treatment in a several patients. These findings positions CX-4945 for success in upcoming Phase II trials. The Phase II randomized drug combination trials are supported by compelling mechanistic rationales which guide selection of indications and shape trial designs. As such Cylene is initiating a trial with gemcitabine/carboplatin in ovarian cancer (DNA damage repair) and also initiating a trial with erlotinib in NSCLC (EGFR pathway).

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CAS No.:        

M.W.:          349.8

Formula:      C19H12ClN3O2 

Synonym:    CX-4,945  

Targets:       CK2 inhibitor   

URL:            http://www.cylenepharma.com/pipeline/ck2-program

SMILES:       O=C(O)c1ccc4c(c1)nc(Nc2cccc(Cl)c2)c3ccncc34