En los campos de la medicina, biotecnología y farmacología, descubrimiento de drogas es el proceso por el cual las drogas son descubiertas y/o diseñadas. En el pasado las drogan fueron descubiertas por la identificación de los ingredientes activos de remedios tradicionales o por casualidad. Una nueva aproximación ha sido entender como la enfermedad e infección se controlan en el nivel molecular y fisiológico y a entidades diana específicas basadas en este conocimiento. El proceso de descubrimiento de drogas involucra la identificación de candidatos, síntesis, caracterización, investigación, y ensayo de eficacia terapéutica. Una vez que un compuesto ha mostrado su valor en estas pruebas, comenzará el proceso de desarrollo de la droga anterior a los ensayos clínicos. A pesar de los avances en tecnología y comprensión de los sistemas biológicos, el descubrimiento de drogas es aún un proceso “largo, costoso, difícil, e ineficiente" con bajas tasas de descubrimiento de terapéuticos nuevos. La información sobre el genoma humano, su secuencia y lo que el codifica has sido proclamado como de una potencial bonanza para el descubrimiento de drogas, que promete virtualmente eliminar el cuello de botella en blancos terapéuticos que han sido uno de los factores limitantes en la tasa de descubrimientos terapéuticos. this requires substantiation with one or more reputable sources from the time of enthusiasm following "completion" of the human genome sequence[cita requerida] Sin embargo, los datos indican que "nuevos blancos" como opuestos a "blancos establecidos" son más propensos a fallos en el descubrimiento de drogas en general [cita requerida] Estos datos corroboran algunos pensamientos subyacentes una tendencia de la industria farmacéutica que comienza a finales del siglo XX y continúa en la actualidad la cual encuentra más aversión de riesgo en la selección de blancos entre las compañías farmacéuticas multinacionales.[cita requerida]

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In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered. Historically, drugs were discovered through identifying the active ingredient from traditional remedies or by serendipitous discovery. Later chemical libraries of synthetic small molecules, natural products or extracts were screened in intact cells or whole organisms to identify substances that have a desirable therapeutic effect in a process known as classical pharmacology. Since sequencing of the human genome which 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, it will begin the process of drug development prior to clinical trials. One or more of these steps may, but not necessarily, involve computer-aided drug design. 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 (NME) was approximately US$1.8 billion. Drug discovery is done by pharmaceutical companies, with research assistance from universities. The "final product" of drug discovery is a patent on the potential drug. The drug requires very expensive Phase I, II and III clinical trials, and most of them fail. Small companies have a critical role, often then selling the rights to larger companies that have the resources to run the clinical trials. Discovering drugs that may be a commercial success, or a public health success, involves a complex interaction between investors, industry, academia, patent laws, regulatory exclusivity, marketing and the need to balance secrecy with communication. Meanwhile, for disorders whose rarity means that no large commercial success or public health effect can be expected, the orphan drug funding process ensures that people who experience those disorders can have some hope of pharmacotherapeutic advances.

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