Ternary Co-crystal, a Novel Dual-acting Pharmaceutical

来源 :中国上海第七届国际新药发明科技年会 | 被引量 : 0次 | 上传用户:neilakw
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  The paper reports the first example of the design of a ternary co-crystal and the first-in-class,dual-acting pharmaceutical,LCZ696.The molecular structure displays highly surprising features,such as stabilization of the supramolecular complex by monovalent metal cation and numerous noncovalent molecular interactions.LCZ696 is the first example of a supramolecular complex incorporating moieties which modulate separate pharmacological targets.LCZ696 does not fall into the category of mutual prodrugs,such as mutual salts,pharmaceutical co-crystals or a carrier-linked prodrug where the carrier used is another drug (for the latter,the linkage between the host drug and the carrier should be a covalent bond).In the LCZ696 structure,the two pharmaceutically active molecular moieties form a unique new molecule,a supramolecular sodium complex held together by noncovalent bonds,such as ionic interactions and hydrogen bonds.These interactions,although individually weak,collectively greatly contribute to the stability of the structure.
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