In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered.
Historically, drugs were discovered by identifying the active ingredient from traditional remedies or by serendipitous discovery, as with penicillin. More recently, chemical libraries of synthetic small molecules, natural products or extracts were screened in intact cells or whole organisms to identify substances that had a desirable therapeutic effect in a process known as classical pharmacology. After sequencing of the human genome allowed rapid cloning and synthesis of large quantities of purified proteins, it has become common practice to use high throughput screening of large compounds libraries against isolated biological targets which are hypothesized to be disease-modifying in a process known as reverse pharmacology. Hits from these screens are then tested in cells and then in animals for efficacy.
Modern drug discovery involves the identification of screening hits, medicinal chemistry and optimization of those hits to increase the affinity, selectivity (to reduce the potential of side effects), efficacy/potency, metabolic stability (to increase the half-life), and oral bioavailability. Once a compound that fulfills all of these requirements has been identified, the process of drug development can continue. If successful, clinical trials are developed.
Modern drug discovery is thus usually a capital-intensive process that involves large investments by pharmaceutical industry corporations as well as national governments (who provide grants and loan guarantees). Despite advances in technology and understanding of biological systems, drug discovery is still a lengthy, "expensive, difficult, and inefficient process" with low rate of new therapeutic discovery. In 2010, the research and development cost of each new molecular entity was about US$1.8 billion. In the 21st century, basic discovery research is funded primarily by governments and by philanthropic organizations, while late-stage development is funded primarily by pharmaceutical companies or venture capitalists.
Cette page est générée automatiquement et peut contenir des informations qui ne sont pas correctes, complètes, à jour ou pertinentes par rapport à votre recherche. Il en va de même pour toutes les autres pages de ce site. Veillez à vérifier les informations auprès des sources officielles de l'EPFL.
Biochemistry is a key discipline in the Life Sciences. Biological Chemistry I and II are two tightly interconnected courses that aims to understand in molecular terms the processes that make life poss
The goal of this course is to instruct the student how fundamental scientific knowledge can be applied for drug discovery and development. We will demonstrate these principles with examples, including
The course discusses methods in modern drug development. Each week, a short introduction to a drug development method / field is provided and a recent research paper is discussed in depth. Students pa
La chimie combinatoire combine (au hasard ou parfois, à ses débuts, puis de manière automatique et codifiée ensuite) des molécules ou structures apparentées pour former des matières à propriétés nouvelles via des synthèses divergentes, par exemple. Elle est née de la génomique et de la protéomique qui cherchent à étudier le fonctionnement du Vivant aux échelles les plus petites, notamment pour trouver de nouvelles cibles thérapeutiques, constituant pour cela des ciblothèques.
L'industrie pharmaceutique est le secteur économique qui regroupe les activités de recherche, de fabrication et de commercialisation des médicaments pour la médecine humaine ou vétérinaire. Cette activité est exercée par les laboratoires pharmaceutiques et les sociétés de biotechnologie. La pharmacie la plus ancienne recensée dans l’histoire date de 754. Ouverte à Bagdad par des pharmaciens arabes, sous le califat Abbasside, les sayadilas, elle a rapidement été rejointe par d’autres, initialement dans le monde médiéval islamique et, par la suite, en Europe.
La conception de médicament, plus précisément conception de substance pharmacologiquement active plus connue sous sa dénomination anglaise Drug design est l'ensemble des processus nécessaires à l'élaboration d'un médicament. Dans l'industrie pharmaceutique, ces processus peuvent-être subdivisés et répartis en quatre phases ou étapes : La phase de recherche La phase de développement La phase clinique La phase de mise sur le marché Remarque : Les phases de recherche et développement sont communément dénommées R&D.
Explore le profilage quantitatif des protéomes pour l'identification des cibles de médicaments au moyen du profilage des protéines basé sur l'activité et des techniques avancées de spectrométrie de masse.
S'insère dans les fondamentaux de la chimie médicinale, mettant l'accent sur l'interrogation des relations structure-activité (SAR) dans la conception des drogues.
Explore les réseaux d'interaction protéines-protéines, l'importance de la liaison, les approches expérimentales, l'identification des cibles médicamenteuses et la construction de réseaux.
Sample efficiency is a fundamental challenge in de novo molecular design. Ideally, molecular generative models should learn to satisfy a desired objective under minimal calls to oracles (computational property predictors). This problem becomes more apparen ...
Amer Chemical Soc2024
, , ,
Large language models (LLMs) have shown strong performance in tasks across domains but struggle with chemistry-related problems. These models also lack access to external knowledge sources, limiting their usefulness in scientific applications. We introduce ...
Ex-vivo drug sensitivity screening (DSS) allows the prediction of cancer treatment effectiveness in a personalized fashion. However, it only provides a readout on mixtures of cells, potentially occulting important information on clinically relevant cell su ...