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The First Class New Anti-alzheimer Drug Phenchlobenpyrrone Completed Phase I Clinical Study
source:     author:     2009-10-23

   August 25th, 2009, Yunnan Provincial Science and Technology Department organized relevant experts to check and accept the project 'the clinical study (Phase I) of the first Class new drug Phenchlobenpyrrone' undertaken by Prof. Hao Xiaojiang of State Key Laboratory of Phytochemistry and Plant Resources in West China, KIB. The experts contrasted the assignment statement of project plan, listened to the project implementation and completion work report , reviewed relevant materials and commonly agreed that the project had finished the required tasks in the assignment statement and agreed to accept.

  It is learnt that the project has achieved the following progresses:

  1.     Completed the synthesizing of clinical Active Pharmaceutical Ingredients(API) and made troche for Phsae I clinical use.
  2.      According to mission requirements, mensurate the purity detection work of standard type for clinical pharmacokinetics is no longer needed to mensurate the drug vivo metabolite. The experiment results indicated that Fen Keluo Ketone's Experimental samples were crystal pure.
  3.   Finished 24 clinical tolerance tests and 48 clinical pharmacokinetics in the clinical observation Phase I. The preliminary results proved that the Phenchlobenpyrrone developed by KIB of CAS was well tolerated by the subjects in the content of 300mg.

     Accomplished clinical pharmacokinetics research. The results are as follows:

  1.   Single medication: the pharmacokinetics progress of healthy volunteers' single oral administration of Phenchlobenpyrrone on low, medium and high dose is all in line with the two-compartment model of first-order absorption; the absorption is rapid and drug content in the blood can be detected 0.25h after administration, while Tmax can be detected 1h later. The drug concentration in the blood both fell to a lower level 12h after the administration. AUC and Cmax separately showed good linear dependence with administration dose. The biological half-life of three doses was all about 6h. Fen Keluo Ketone has no accumulation effect in the healthy volunteers and absorption and elimination has nothing to do with dosage.
  2.   The healthy volunteers took 30mg oral Phenchlobenpyrrone for 7 consecutive days and the kinetics progress of Phenchlobenpyrrone in blood plasma did not change. The drug valley value in blood plasma was low, fluctuating around detection limit. So the dosage regimen of oral Phenchlobenpyrrone for 7 consecutive days will not caused drug accumulation in the body.
  3.   When the healthy volunteers took oral Phenchlobenpyrrone, the urinary excretion rate as prototype was low, accounting for under 1% of all the dosage and the excretion was fast 1-6h after oral administration. Thus, Fen Keluo Ketone may be primarily eliminated in metabolic conversion mode.
  4.   Completed the arranging of clinical research data Phase I and now the clinical record of Phase II and III is under preparation. This project has won support of national special funds for key new drug.
  5.   Carried out the improvement of API synthesizing technology and the pre-trial of large-scale production technology. In the preliminary study, the project has established various synthesis methods of Pyrrolidone Class 2 compounds, new method of g-nitro-carboxylate' cyclization and deoxidiaition and configuration transformation of synthetic intermediate in the solution and fulfilled the synthetic route technology that could be industrial-scale production. During the project implementation process, according to the principle of 'simple and feasible technology, reasonable cost and good reproduction', the project continue to further study the original optimal synthesis technology and ensure the best synthesis technology. Besides, the project has resolved the issue of getting high-purity raw material medicine directly through the re-crystallization without column chromatography, further reducing the cost.


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