Module 2 Flashcards
Years of - Target identification, Lead Discovery, Lead optimization, and Preclinical Trials.
7-10 years
Phases l, ll, lll
6-12 years
FDA approval and Post-Approval
1-2 years
Cover a huge range of biological moieties such as; Protein, Genes, and Nucleic acid.
Target
Property should be able to bind with high-affinity to presumed drug moiety.
Druggability
Should develop pharmacologic activity that can be established by in-vitro and in-vivo.
Pressumed drug moiety
Identifying, selecting, prioritizing, potential disease targets.
Data mining using bioinformatics
Genetic polymorphism and connection with disease
Genetic association
Changes in mRNA or protein levels
Expulsion profile
I’m vitro cell based mechanistic studies
Pathway and phenotypic analysis
Knock down and knock out
Functional screening
Demonstrate a pertinence of site of action and involves an exhaustive functional group of characterization
Validation
Identification of ___ and ____ are crucial in drug delivery process.
Hit and lead compound
Chemical compound that exhibits a desired biological activity
Hit
Most popular and authentic rational approach for identifying new chemical entities
HTS - High Throughput Screening
True or False
Ultra HTS - 100,000 molecules per day.
True
When the exact hit molecule is identified, it is refined further to improve
its selectivity, binding properties, potency, and physicochemical properties by a process called
Hit to lead development
Valuable approach when known chemical entities with desired activity are unavailable
Random screening
No intellectual approach, only approach in 1935, and is a method of choice to discover drugs or lead when nothing is known. It is also sort of blind.
Random screening
Accidental discovery
Serendipity
Analogues of existing established drugs are synthesized and is more scientific and logical approach.
Molecular manipulation
Synthetic Penicillin and Cephalosporin were developed in this manner
Molecular manipulation
Most rational approach of drug research and development.
Molecular designing
Formed in body after metabolism. Example is Nortriptyline.
Active metabolites
Active metabolites of amitriptyline
Nortriptyline
Involves an iterative series of synthesis. Maintain favorable properties
Lead optimization
Evaluated for range of properties
Potential lead
associated with many concept-based methods.
Computer aided drug design
Equally important in CADD
Science
Technology
should be used as complimentary techniques to the experimental methods
during drug discovery, to obtain viable results.
CADD methods
employ statistical methods
extensively
Quantitative Structure Activity relationship
an attempt to identify and quantify the physicochemical properties of a drug and
relate these to biological activities.
QSAR
Can be studied by QSAR
Hydrophobic
Electrical
Steric properties
measure of its distribution in a lipophilic-hydrophilic
phase system and indicates its ability to penetrate biologic multiphase systems.
Partition coefficient
The crystal or amorphous forms and/or the particle size of a powdered drug can affect
Dissolution rate
