DDD
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First drug created containing an active ingredient with established efficacy, safety, & quality and received approval for use
Innovator Drug
First retroviral inhibitor approved for the tx of AIDS
Zidovudine (Azidothymidine - AZT)
On average, drug discovery and development could take about ____ years.
12
The identification of a single marketed drug has a success rate of ____.
< 0.001%
DRUG DISCOVERY The choice of disease and identification of biological target Identify the step in drug discovery.
(1) Target Discovery
DRUG DISCOVERY Expected molecular target (gene, protein, nucleic acid of a small molecule) is certified Identify the step in drug discovery.
(2) Target Validation
DRUG DISCOVERY Structurally related compounds with identified desired biologically activity are identified (HIT and LEAD) through biological screening of large numbers of compounds Identify the step in drug discovery.
(3) Lead Discovery
DRUG DISCOVERY Lead compounds are modified and studied to identify potential candidate for drug development Identify the step in drug discovery.
(4) Lead Optimization
DRUG DISCOVERY Maintain favorable properties and enhance deficiency on structure Identify the step in drug discovery.
(4) Lead Optimization Goals
DRUG DISCOVERY Early stages of pharmacological studies are helpful to characterize the MOA of the compound Identify the step in drug discovery.
(5) Product Characterization
DRUG DISCOVERY A stage of drug development during which the physicochemical properties of APIS are characterized to produce a bioavailable, stable, and optimal dosage form for a specific administration route Identify the step in drug discovery.
(6) Pharmaceutical Formulation/ Formulational Development
DRUG DISCOVERY Data mining using bioinformatics Identify the step in drug discovery.
(1) Target Discovery Approaches
DRUG DISCOVERY Genetic association Identify the step in drug discovery.
(1) Target Discovery Approaches
DRUG DISCOVERY Expression profile Identify the step in drug discovery.
(1) Target Discovery Approaches
DRUG DISCOVERY Pathway and phenotypic analysis Identify the step in drug discovery.
(1) Target Discovery Approaches
DRUG DISCOVERY Functional screening Identify the step in drug discovery.
(1) Target Discovery Approaches
DRUG DISCOVERY SAR of the analogs Identify the step in drug discovery.
(2) Target Validation Strategies
DRUG DISCOVERY Generation of drug-resistant mutant Identify the step in drug discovery.
(2) Target Validation Strategies
DRUG DISCOVERY Knockdown/over expression of target Identify the step in drug discovery.
(2) Target Validation Strategies
DRUG DISCOVERY Monitoring the known signaling systems downstream of the presumed target Identify the step in drug discovery.
(2) Target Validation Strategies
DRUG DISCOVERY Reproducibility Identify the step in drug discovery.
(2) Target Validation Key Steps
DRUG DISCOVERY Introduce variation to drug-target environment Identify the step in drug discovery.
(2) Target Validation Key Steps
DRUG DISCOVERY SAR identified Identify the step in drug discovery.
(3) Lead Discovery Characteristics
DRUG DISCOVERY Drug ability (preliminary toxicity) Identify the step in drug discovery.
(3) Lead Discovery Characteristics