Drug Discovery 00000002

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Cancer Cells demonstrate

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Uncontrolled cell growth, Ability to invade territories normally reserved for other cell types, Genetic changes

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Cancer is more common in older people because

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they have accumulated more mutations

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How would you expect the lack of selectivity of non-specific cancer chemotherapeutic agents such as nitrogen mustard drugs to be manifested clinically?

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Impaired synthesis of new blood cells

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How did luck play a role in the discovery of the mustard liquid chemotherapy drugs?

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Physicians observed that rapidly dividing cells such as bone marrow cells were killed in soldiers exposed to mustard gas in WWI

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The discovery of the mustard liquid drugs would best be described as

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Phenotypic drug discovery

Front 6

The Philadelphia chromosome is associated with which type of cancer?

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leukemia

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What kinds of cells are most likely to give rise to a tumor?

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cells that normally divide

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What are oncogenes?

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Genes that have the potential to become cancerous

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Using a "car and driver" analogy, which of the following accurately describes the role of tumor-suppressor
genes and oncogenes in normal cells?

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Tumor-suppressor genes are the brakes while oncogenes are the gas.

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Pharmacodynamics (Select the best answer)

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actions of the biologically active compounds in the body

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Which of the following methods of drug discovery requires knowledge of the 3D protein receptor structure?

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Rational drug design

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The story of the development of Gleevec illustrates the process of

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a target-centered approach to drug design

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The method of comparing the costs and benefits of health care interventions in which benefits are
quantiled as length and quality of life is:

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a cost-utility analysis

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An assumption behind the use of QALYs (quality adjusted life years) as \measuring sticks" is that people
may be willing to accept

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Shorter life with better health

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Why is Gleevec a \speci c therapy" for chronic myeloid leukemia?

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Gleevec selectively binds the BCR-Abl protein in abnormally growing blood cells

Front 16

How does acetaminophen (Tylenol) cause toxicity in overdose

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Acetaminophen is metabolized to a toxic metabolite

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Which of the following is not a pharmacokinetic process?

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The drug causes dilation of blood vessels

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What the body does to a drug is called

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pharmacokinetics

Front 19

HIV is the virus that causes AIDS. In the mid-1990s, researchers discovered an enzyme in HIV called
a protease. Once the enzyme's structure was known, researchers began looking for drugs that would fit
into the active site and block it. If this strategy for stopping HIV infections were successful, it would be
an example of which of the following?

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antagonist

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The relationship between the amount of a drug taken and the intensity or type of the resulting e ect is
called the

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dose-response function

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Gleevec is a new drug used in the treatment of chronic myelogenous leukemia (CML). Gleevec binds to the Abl protein and inhibits its activity. GLeevec also shows promise in the treatment of gasterointestinal stromal tumors (GST), but has no effect on lung cancer. Which statement is the most consistent with the above statement?

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Abl activation is probably one of the genetic changes that that results in GSTs

Front 22

Legislation passed after a legally marketed drug killed 107 people, most whom where children

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Food, Drug, and Cosmetic Act of 1938

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The effective drug does 50% ED50 is most closely associated with a drugs

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potency

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Which of the following metabolically active issues is the principle organ for drug metabolism

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Liver

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Which of the following statements is not true about cytochrome P450 enzyme

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They are responsible for the biological activity of early chemotherapy agents

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Which of the following is usually the goal of a drug metabolism

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Metabolism makes drugs more water soluable

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Which of the following do patent examiners not consider when evaluating patent-ability of a new product or process?

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Will it make money

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Pharmacokinetics considers

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The way in which the body affects a drug by the process of absorption, distribution, metabolism and excretion

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Most drugs and metabolites are excreted in the

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Urine

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Who is David Franklin?

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The medical laision at Pfizer who filed the whistle blower lawsuit exposing Pfizers illegal promotion of Neurontin

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Pharmacodynamics considers

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The effects of the drug on the body and the mode of the drug action

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Pharmacoeconomics is used to estimate and compare cost and health related outcomes for drugs, but this information is typically not considered by the FDA when reviewing a new drug application

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True

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A drug that binds to a cell receptor and causes a direct response is called an

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Agonist

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What the body doe to a drug is called

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Pharmacokinetics

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The most common factor associated with a variation in an individual's response to a drug is

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Genetic variation in enzymes that metabolize drugs

Front 36

In a qui tam action, the citizen who files the law suit is called a

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whistle blower or relator

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During the early years of cancer research there were two schools of though regarding the cause of cancer. 1) cancer was caused entirely by environmental factors and 2) that cancer wa caused by genetic factors. Which is correct?

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Both, most chemical carcinogens function by altering genes

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Pharmacodnynamics is defined

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The effect a drug has on our bodies

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NSAIDs works by

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blocking production of prostaglandins

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Which of the following laws established that drugs should be accurately labeled with contents and dosage

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Pure Food and Drug Act 1906

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Which federal law would a pharmaceutical company be accused of violating if their television advertisement was misleading?

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Food, Drug and Cosmetic Act of 1938

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Which pharmacoeconomic analysis has the advantage of being the simplest to conduct because the outcomes assume to be equivalent

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Cost minimization

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A law suit brought by a citizen against another citizen for corporation who has defrauded the government is called

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Qui Tam suit

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Informed consent in clinical trials is important because

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It enables the participant to understand vital information on the proposed trial

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Why are some prescription drugs not avaible as less expensive generic drugs

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The prescribed drug may be a pioneer drug and the 20 year patent protection period may not have expired

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Which of the following best describes a fiduciary relationship such as that between a physician and patient.

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The party who is fiduciary must avoid any conflict of interest and she must not put her personal interest before those to whom fiduciary obligations are owned

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For intravenous IV dosages what is the bioavailability assumed to be

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100%

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Relationship between the amount of drug taken and the intensity or type of the resulting effect is called the

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dose-response function

Front 49

Metastasis in the context of Cancer is the process of

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Loss of cell adhesion that leads to spread of cancer

Front 50

Which of the following is the process of transporting a drug from its administration site to its site of action

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Distribution

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Opiates such as morphine and codeine both contain molecules that are similar to endorphins, the bodys natural pain killer. Opiates like these bind to receptor sites that are keyed to endorphins that trigger similar pain reducing responses. Given tha the characteristics, both morphine and codeine would be classified as

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agonists

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Which of the following statements about pharmaceutical sales is true

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pharmaceutical firm can only advertise a drug product for indications approved in the label

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Pharmaceutical companies historically marketed only to doctors. More recently they have spent millions of dollars to advertise prescription drugs directly to consumers. Which of the following is not a consequence of DTC pharmaceutical advertising.

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DTC advertising can educate patients bout the many off-label uses for their medication.

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Lisa Simpson identified a drug candidate by testing thousands of compounds in a chemical library for activity against the isolated protein target. This approach to drug discovery would best be classified

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High through put screening

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Some components in food (grapefruit juice) inhibits one of the major CYP enzymes that metabolize many drugs. This inhibitor would result in the following out come

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Parent drug concentrations of drugs metabolized by this enzyme are increased due to inhibition of the enzyme

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The method of comparing the cost and benefits of health care intervention in which benefits are quantified as length and quality of life is

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a cost utility analysis

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Probably the most important reason for obesity today in America is

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overfeeding and inactivity

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If a company has a patent on a drug that treats a particular disease

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They are the only ones that can cell the drug while the patent is in forced

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With prescription drugs there is a trade off between

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the benefits of motivating innovation with patents and high prices and the ability of people to afford those drugs

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Briey describe the main goals of phase 1, 2, and 3 clinical trials

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Phase I: Safety
Phase II: Efficacy – “Finding the dose”
Phase III: Show it works. To compare experimental or new therapies with standard therapy or competitive therapies.
Phase IV: Postmarking Surveillance

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What are NSAIDs and how do they work?

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Acetylsalicylic acid (aspirin) Bind to COX and prevents formation of
Prostaglandins
Prostaglandins are produced within the body's cells by the enzyme cyclooxygenase (COX1 and 2). Enzymes produce prostaglandins that promote inflammation, pain, and fever.
Nonsteroidal antiinflammatory drugs (NSAIDs) block the COX enzymes and reduce prostaglandins

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Morphine

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binding to a opioid receptor essentially ‘blocks’ neuron signaling and in doing so block the relaying of pain signals from pain receptors

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Agonist

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A drug that binds to receptor and has a cellular (pharmacological) effect

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Antagonist

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A drug that binds to a receptor but produces no direct cellular effect. Blocking the action of an agonist, or an endogenous ligand

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dose-effect curve

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The magnitude of a drug effect should be proportional to the number of receptors occupied by the drug, and A drug should have a maximal effect when all receptors are occupied

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dose-response curves
-Threshold
-ED50
-Ceiling

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Threshold: Dose that produces a just-noticeable effect.
ED50: Dose that produces a 50% of maximum response.
Ceiling: Lowest dose that produces a maximal effect.

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Efficacy vs Potency (Dose)

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Efficacy: drug is able to produce desired response
Potency:drug needed to produce 50% of the maximal response

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Therapeutic Window (TW)

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Useful range of concentration between
-ED50 = Efficacious dose 50%
-TD50 = Toxic dose at which 50%

TW=TD50/ED50

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Potency vs Efficacy

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Potency, A measure of the concentrations of a drug at which it is effective. Efficacy,
measure of the maximal response to a test agonist as a fraction of that to a full agonist of the same pharmacological class.

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Pharmacodynamics

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the study of the biochemical and physiological effects of drugs and the mechanisms of their actions

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Pharmacokinetics

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the activity or fate of drugs in the body over a period of time, including the processes of absorption, distribution, localization in tissues, biotransformation and excretion.

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Three types of injection

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intravenous - blood stream
intramuscular - in muscle
subcutaneous - under skin

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Alcohol induced toxicity of acetaminophen (Tylenol)

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Larger ingestions result in production of a toxic metabolite N-acetyl-p-benzoquinoneimine (NAPQI) by P450.

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Types of Excretion

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urination, exhalation, defecation, and/or sweating

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Rate of elimination

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refers to the amount of drug removed per unit of time from the body by normal physiological processes. (how long the effect is)

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malignant tumor

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If the tumor cells escape from their site of origin and move off to grow elsewhere

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Types of Cancer
Carcinomas
Sarcomas
Lymphomas
Leukemias

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Carcinomas - epidermal
Sarcomas - connective tissue
Lymphomas - immune system
Leukemias - blood cells

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Stages of Tumore 1-4

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Stage 1 - Tumor confined to organ
Stage 2 - Tumor has invaded adjacent tissue
Stage 3 - Tumors have metastasized to regional lymph nodes
Stage 4 - Tumors have metastasized to distant organs

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Cause of Cancer

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Carcinogenic chemicals
Radiation
Some viruses
Heredity (germ-line)

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Mustard gas

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alkylate the guanine nucleotide in DNA strands, which prevents cellular division and generally leads directly to programmed cell death