Serravino, a new anti-AIDS drug developed by the Kunming Institute of Zoology, Chinese Academy of Sciences and the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, received the clinical trial notice issued by the China State Drug Administration on May 5, 2019, and agreed to conduct clinical trials . The project is currently preparing for clinical phase I studies. If the research and development is successful, it will better meet the clinical medication needs of the majority of AIDS patients.
Serravino is China's first CCR5 receptor antagonist approved for clinical research. It has won the 13th Five-Year "Major New Drug Creation" Science and Technology Major Project, the Chinese Academy of Sciences 'Strategic Leading Science and Technology Project, the Chinese Academy of Sciences' Independent Deployment Project, Yunnan Funded by the Provincial Science and Technology Department and other funds.
Researchers first used computer-aided drug design, drug design strategies based on structure and altered metabolic pathways, and designed new structural types of CCR5 antagonists; they also carried out multiple rounds of structural transformation and drug optimization of CCR5 antagonists through efficient synthetic techniques. Currently the only marketed clinical drug Maravino targeting CCR5 target and the crystal complex structure of multiple CCR5 antagonists and CCR5 receptors, carry out screening and research on the anti-HIV activity of CCR5 antagonists; in-depth on this basis Structural modification, evaluation of drug efficacy and optimization of druggability, found a new drug candidate Serravino CCR5 antagonist.
The results of pre-clinical studies show that compared with Maravino, Serravino has better antagonistic activity on CCR5 receptor, and has better inhibitory activity and therapeutic index on various HIV strains, clinical strains and drug-resistant strains Maravino or equivalent; but Serravino has good pharmacokinetic properties in rats and dogs, small species differences, no inhibition and induction of CYP450 enzymes, no potential drug-drug interaction , Good security.
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