Drug Evaluation, Preclinical/*methods ; Statistics

Antitussive Agents/*pharmacology ; Drug Evaluation, Preclinical/methods

Antitussive Agents/*pharmacology ; Drug Evaluation, Preclinical/methods

China Food and Drug Administration didn't issue any guideline on the pre-clinical study of drug-eluting coronary stent system, the basic requirement of the authorized administration was summarized to help manufacture prepare the document during the registration process.
China ; Drug Evaluation, Preclinical ; methods ; Drug-Eluting Stents ; Guidelines as Topic

Animals ; Dogs ; Drug Evaluation, Preclinical ; methods ; Statistics as Topic

Animals ; Antitussive Agents ; pharmacology ; Drug Evaluation, Preclinical ; methods ; Mice

Anticholesteremic Agents/*pharmacology ; Cholesterol/blood ; Drug Evaluation, Preclinical/methods

Hits, leads and drug candidates constitute three millstones in the course of drug discovery and development. The definition of drug candidates is a critical point in the value chain of drug innovation, which not only differentiates the research and development stages, but more importantly, determines the perspective and destiny of the pre-clinical and clinical studies. All outcomes from the development stage are actually attributed to the chemical structure of candidates. The quality of candidates, however, is restricted by the drug-likeness of lead compounds, which in turn is decided by the characteristics of hits. The hit-to-lead is to provide a promising and druggable structure for further development, whereas the optimization of lead compounds is a process to transform an active compound into a drug, which in essence is molecular manipulation in multi-dimensional space related to pharmacodynamic, pharmacokinetic, physico-chemical, and safety properties. This review discusses the strategic principles in hit discovery, lead identification and optimization, as well as drug candidate definition with practical examples.
Animals ; Drug Design ; Drug Evaluation, Preclinical ; methods ; Drug Industry ; methods ; Humans ; Molecular Structure ; Pharmaceutical Preparations ; chemistry

With the constant development of the drug screening technology, new screening methods and techniques have came to the fore, driving drug screening to grow rapidly and efficiently with a high throughput. Characterized by micro-scale analysis, high throughput, inheritability and good biocompatibility, the micro-fluidic analytical technology provides a new method and technical platform for screening active ingredients from natural products. This essay introduces multiple methods used for screening active ingredients from natural products and focuses on the micro-fluidic chip screening technology combined with cell culture and its characteristics, the composition of the platform of the micro-fluidic chip screening technology and its application in screening active ingredients from natural products.
Animals ; Biological Products ; chemistry ; Drug Evaluation, Preclinical ; methods ; Humans ; Microfluidic Analytical Techniques ; methods

Natural products (NPs) are compounds that are derived from natural sources such as plants, animals, and micro-organisms. Therapeutics has benefited from numerous drug classes derived from natural product sources. The Biopharmaceutics Drug Disposition Classification System (BDDCS) was proposed to serve as a basis for predicting the importance of transporters and enzymes in determining drug bioavailability and disposition. It categorizes drugs into one of four biopharmaceutical classes according to their water solubility and extent of metabolism. The present paper reviews 109 drugs from natural product sources: 29% belong to class 1 (high solubility, extensive metabolism), 22% to class 2 (low solubility, extensive metabolism), 40% to class 3 (high solubility, poor metabolism), and 9% to class 4 (low solubility, poor metabolism). Herein we evaluated the characteristics of NPs in terms of BDDCS class for all 109 drugs as wells as for subsets of NPs drugs derived from plant sources as antibiotics. In the 109 NPs drugs, we compiled 32 drugs from plants, 50% (16) of total in class 1, 22% (7) in class 2 and 28% (9) in class 3, none found in class 4; Meantime, the antibiotics were found 5 (16%) in class 2, 22 (71%) in class 3, and 4 (13%) in class 4; no drug was found in class 1. Based on this classification, we anticipate BDDCS to serve as a useful adjunct in evaluating the potential characteristics of new natural products.
Animals ; Biological Products ; classification ; metabolism ; pharmacokinetics ; Biopharmaceutics ; methods ; Drug Evaluation, Preclinical ; methods ; Humans