2022-08-25T19:14:03+03:00[Europe/Moscow] en true <p>Biologic product</p>, <p>First-in-class</p>, <p>Fast track</p>, <p>Breakthrough Therapy</p>, <p>Orphan diseases</p>, <p>Phosphorylation</p>, <p>-ase</p>, <p>Monoclonal antibodies</p>, <p>-mab</p>, <p>MOA - monoclonal antibodies</p>, <p>AS-ON (Antisense Oligonucleotides)</p>, <p>-rsen</p>, <p>Aptamers</p>, <p>-APT</p>, <p>siRNA</p>, <p>Absorption, distribution, metabolism, elimination, toxicity</p>, <p>Absorption</p>, <p>Distribution</p>, <p>Metabolism</p>, <p>Elimination</p>, <p>Toxicity</p>, <p>catabolized by proteases, water soluble, large MWT</p>, <p>Bioavailability</p>, <p>circulatory system</p>, <p>molecular weight, lipohilicity, number of HBD, number of HBA</p>, <p>&lt;=500</p>, <p>&lt;=10</p>, <p>&lt;=5</p>, <p>0&lt; Log P &lt; 5</p>, <p>Enzymes, Monoclonal antibodies</p>, <p>AS-ON, Aptamers, siRNA</p>, <p>&lt;= 5</p>, <p>&lt;=10</p> flashcards
Pharmacogenomics Module 1

Pharmacogenomics Module 1

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  • Biologic product

    a substance that is made from a living organism or its products and is used in the prevention, diagnosis, treatment, or cure of a disease.

  • First-in-class

    drugs that possess a mechanism of action different from those of existing therapies (indicator of drug's degree of innovation)

  • Fast track

    designated drugs have the potential to address unmet medical needs. Fast Track speeds new drug development and review.

  • Breakthrough Therapy

    destination assigned to drugs with preliminary clonal evidence demonstrating that the drug may result in substantial improvement on at least one clinically significant endpoint over other available therapies for serious or life-threatening diseases for which there is unmet medical need.

  • Orphan diseases

    affect fewer than 200,000 patient per year in the U.S

  • Phosphorylation

    attachment of a phosphate group to an ion or molecule; important in activating enzymes

  • -ase

    Protein therapeutics contain what stem suffix?

  • Monoclonal antibodies

    large glycosylated proteins-produced from cell culture

  • -mab

    Monoclonal antibodies contain what stem suffix?

  • MOA - monoclonal antibodies

    (very specific) exert their effect on cell surface receptors, or scavenge proteins in extracellular matrix. Block signaling pathways.

  • AS-ON (Antisense Oligonucleotides)

    synthetic nucleic acid based drugs that bind to specific mRNA strains.

    -composed of short sequences; 13-25 nucleotides

    -complementary to mRNA strands

    -stop translation-> stops protein synthesis

  • -rsen

    Which end suffix do Antisense Oligonucleotides contain?

  • Aptamers

    RNA or DNA nucleic acid drugs that recognize specific proteins. The fold up into unique 3-D structures, allowing them to bind specifically to proteins.

  • -APT

    Which suffix do most Aptamers contain?

  • siRNA

    - therapeutics that target host mRNA

    -commonly referred to as "kill the messenger"

    -made from nucleic acids

  • Absorption, distribution, metabolism, elimination, toxicity

    What does ADMET stand for?

  • Absorption

    -movement of drug from site of application into bloodstream or target tissue

    -measure of Bioavailability

  • Distribution

    -movement of drug from blood to target site of action

  • Metabolism

    Transformation of drug

  • Elimination

    elimination of drug from body

  • Toxicity

    Effect of drug on non-target tissues or cells

  • catabolized by proteases, water soluble, large MWT

    Why are biologics NOT administered orally?

  • Bioavailability

    amount of drug absorbed relative to quantity given

  • circulatory system

    The fraction of oral drug that makes it to the ___ is the bioavailability of that drug

  • molecular weight, lipohilicity, number of HBD, number of HBA

    What are Lipinski's Parameters for predicting Oral Bioavailability ?

  • <=500

    What must the molecular weight be for a drug?

  • <=10

    Number of Hydrogen Bond acceptors?

  • <=5

    Number of hydrogen Bond donors?

  • 0< Log P < 5

    What must the log P be?

  • Enzymes, Monoclonal antibodies

    Types of protein biologics

  • AS-ON, Aptamers, siRNA

    Types of Nucleic Acid biologics

  • <= 5

    What is the number of hydrogen bond donors to qualify for Lipinski's rule ?

  • <=10

    What is the number of hydrogen bond acceptors to qualify for Lipniski's rule?