No. 90

August 2013

Headline News Innovation and Development

Applied Technology

Basic Science

Cooperation between CAS and Local Authorities

Bioscience International Cooperation Brief News Geoscience Hightlight Events
Applied Technology

TPN729 Seeks Clinical Trial

A drug candidate, TPN729, for the treatment of erectile dysfunction (ED), was approved by China Food and Drug Administration (CFDA) for clinical trial phase I on June 25, 2013. TPN729 is discovered and developed by Prof. Shen Jingshans group (Department of Medical Chemistry) and Prof. Jiang Hualiangs group (Drug Discovery and Design Center, DDDC) of the Shanghai Institute of Materia Medica (SIMM). The Center for Drug Safety Evaluation and Research of SIMM, the Center for Drug Metabolism Research of SIMM, and the College of Pharmaceutical Sciences (CPS) of the Zhejiang University have also contributed to the preclinical research of TPN729 program. Male erectile dysfunction(ED) affects more than 150 million men worldwide. Currently, treatment for ED predominantly consists of oral Phosphodiesterase type 5 (PDE5) inhibitors therapies. In mammals, 21 different PDE-encoding genes have been identified so far, classified in 11 families. Because of the insufficient selectivity, currently available PDE5 inhibitors also inhibit other PDE isozymes, affecting their target tissues (e.g., PDE1: heart; PDE6: retina; and PDE11: skeletal muscle), which in some cases can cause unwanted side effects and therapy discontinuation. As the unmet clinical needs with current PDE5 inhibitors, research is ongoing to develop even better and safer alternatives. TPN729 is a drug candidate for the treatment of erectile dysfunction (ED). It is a novel, orally available PDE5 inhibitor with high activity and selectivity. TPN729 is about 3-fold more selective against PDE1 and 2.5-fold more selective against PDE6 than sildenafil, and about 500-fold more selective against PDE11 than tadalafil, showing a more balanced selectivity profile. Thus it is expected to have fewer side effects in comparison with current available PDE5 inhibitors. TPN729 also shows excellent in vivo potency, low toxicity and superior pharmacokinetic property.  

Prototype of Novel Ionic Liquid Absorption Refrigeration Developed

Through the efforts of nearly three years, researchers from the CAS Institute of Engineering Thermophysics have screened out a novel ionic liquid absorption refrigeration working pair, the [mmim] DMP/CH3OH, which is provided with excellent theoretical cycle performance and good commercial application prospect. The first [mmim] DMP/CH3OH absorption experiment model machine with cooling power of 12 kW have been successfully designed and manufactured. From the research, it is indicated that each technical indicators of the novel working pair, [mmim] DMP/CH3OH, are better than that of any other ionic liquid type working pairs reported in the literatures, which can even be compared with that of the conventional working pair, LiBr/H2O. Recently, the researchers have developed a new absorption refrigeration/heat pump working pair, [bmim]Zn2Cl5/NH3, which possesses the domain advantages of the absorption and adsorption refrigeration systems and can overcome several traditional issues remain in the adsorption systems, such as poor performance of heat transfer and attenuation of adsorptive capacity. Two SCI papers and one special chapter in an international English monograph have been published reporting relevant results of the work.

Other Issues
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