Cymanquines: Metallo-Chloroquine Therapeutics

Inhibition of autophagy has become an attractive target for the clinical management of drug resistant cancers. Towards this end, the potent anti-malarial chloroquine (CQ) has been explored as an autophagy inhibitor in multiple studies. Unfortunately, CQ’s inability to exhibit cytotoxic effects in the low PH tumor microenvironment has presented some limitations for this use.

In response to the limitations of CQ, UVM researchers developed a novel organometallic analog of CQ, cymanquine (CymQ).CymQ displays superior single agent cytotoxicity compared to CQ and other CQ analogs, while maintaining that cytotoxicity at low PH. In addition to its use as an autophagy inhibitor for cancer therapy, CymQ also shows improved anti-malarial activity over CQ and may have therapeutic capabilities in other diseases with autophagy disorders, such as SLE/Lupus.

Applications:

• Treatment of cancers.
• Anti-Malarial therapeutic.
• Treatment of other autophagy disorders.

Advantages:

• Low steric bulk allows CymQ to cross membranes and be metabolized.
• Cytotoxic in the acidic tumor microenvironment.
• Low tendency to undergo oxidation in vivo, reducing side effects.

References:

Novel organometallic chloroquine derivative inhibits tumor growth J Cell Biochem. 2018 Mar 25. doi: 10.1002/jcb.26787

Synthesis and anodic electrochemistry of cymanquine and related Complexes Journal of Organometallic Chemistry 817 (2016) 15e20

Opportunity:

• Looking for research and development partners and licensing opportunities.

Patents: 

• US Patent Nos. 10,512,652 and 10,370,395 and 10,954,260

Seeking:

• Licensing
• Development partner