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Learning Objectives - Drug Discovery

Total questions: 96

Worksheet time: 48mins

Name
Class
Date
1.

Sources of new drugs include:

a)

Natural products, synthetic chemicals, biotechnology, and molecular modeling

b)

Only natural products

c)

Only synthetic chemicals

d)

Only biotechnology

2.

An “old” drug can be classified as “new” under which of the following circumstances?

a)

When it is used for a new indication, dosage form, route of administration, or patient population.

b)

When it is manufactured by a different company with the same formulation.

c)

When it is prescribed by a new physician.

d)

When it is sold under a different brand name without any change in formulation.

3.

Which of the following correctly defines goal drug, lead compound, drug candidate, and prodrug?

a)

Goal drug is the ideal drug, lead compound is a chemical with desired biological activity, drug candidate is a compound selected for development, and prodrug is an inactive compound converted to active form in the body.

b)

Goal drug is a compound selected for development, lead compound is an inactive compound, drug candidate is the ideal drug, and prodrug is a chemical with desired biological activity.

c)

Goal drug is an inactive compound, lead compound is the ideal drug, drug candidate is a chemical with desired biological activity, and prodrug is a compound selected for development.

d)

Goal drug is a chemical with desired biological activity, lead compound is a compound selected for development, drug candidate is an inactive compound, and prodrug is the ideal drug.

4.

Which of the following lists five lead discovery methods?

a)

High-throughput screening, virtual screening, fragment-based screening, natural product screening, de novo design

b)

High-throughput screening, chromatography, distillation, extraction, crystallization

c)

Virtual screening, PCR, gel electrophoresis, mass spectrometry, NMR

d)

Fragment-based screening, Western blotting, ELISA, immunoprecipitation, flow cytometry

5.

Activity and potency are differentiated as follows:

a)

Activity refers to the effect produced by a drug, while potency refers to the amount needed to produce that effect.

b)

Activity refers to the amount of drug needed, while potency refers to the effect produced.

c)

Activity and potency both mean the same thing in pharmacology.

d)

Activity is only related to side effects, while potency is related to therapeutic effects.

6.

Key requirements for an oral drug include:

a)

Stability in gastric acid, adequate absorption, and minimal first-pass metabolism

b)

Immediate excretion by the kidneys

c)

Insolubility in water

d)

Requirement for intravenous administration

7.

Which stage of the New Drug Approval Process involves laboratory research, assays, target discovery, target validation, and lead generation?

a)

Preclinical Research

b)

Clinical Research

c)

Discovery/Development

d)

Data Review

8.

In which stage of the New Drug Approval Process are in vitro, in vivo, and ex vivo testing used to assess safety and formulate dosing, resulting in an IND application?

a)

Clinical Research

b)

Preclinical Research

c)

Data Review

d)

Post-Market Monitoring/Lifecycle Management

9.

Human trials to test safety and effectiveness, including Phase I, II, and III, are conducted during which stage of the New Drug Approval Process?

a)

Clinical Research

b)

Preclinical Research

c)

Drug Discovery

d)

Post-Marketing Surveillance

10.

What is the main focus of the Data Review stage in the New Drug Approval Process?

a)

FDA review of application. If approved, moves to registration and post-market monitoring.

b)

Initial laboratory research and animal testing.

c)

Marketing and advertising strategies for the new drug.

d)

Distribution of the drug to pharmacies and hospitals.

11.

Ongoing safety monitoring of marketed drugs and studies to optimize and enhance the value of a drug after launch occur in which stage of the New Drug Approval Process?

a)

Post-Market Monitoring/Lifecycle Management

b)

Preclinical Testing

c)

Clinical Trials Phase I-III

d)

Regulatory Submission/Approval

12.

According to the FDA, what is a new drug? Fill in the blank: Any drug that is not yet recognized as ______ and ______ in conditions recommended for its use in the labeling among qualified experts.

a)

safe and effective

b)

affordable and available

c)

tested and marketed

d)

approved and prescribed

13.

Which of the following is considered a new drug according to the FDA?

a)

A new chemical entity

b)

A new formulation of an old drug

c)

A new combination of old drugs

d)

All of the above

14.

Fill in the blank: A new drug can be a new ______ entity.

a)

chemical

b)

physical

c)

mechanical

d)

thermal

15.

Fill in the blank: A new drug can be a new formulation or method of manufacture of an "______" drug.

a)

old

b)

rare

c)

expensive

d)

foreign

16.

Fill in the blank: A new drug can be a new combination (including proportions) of two or more "______" drugs.

a)

old

b)

rare

c)

expensive

d)

foreign

17.

Fill in the blank: A new drug can be a new use or route of administration or dosage form of an ______ drug.

a)

established

b)

expired

c)

experimental

d)

exclusive

18.

What are the three main sources of new drugs? Fill in the blanks: natural sources, ______ synthesis, ______ engineering.

a)

organic, genetic

b)

inorganic, chemical

c)

synthetic, molecular

d)

herbal, protein

19.

Which of the following is a natural source of drugs?

a)

Plants

b)

Minerals

c)

Animals

d)

Microorganisms

20.

Fill in the blank: Drugs can be obtained from natural sources such as ________.

a)

Plants

b)

Plastic

c)

Steel

d)

Glass

21.

Fill in the blank: Drugs can be obtained from natural sources such as ________.

a)

Minerals

b)

Plastics

c)

Metals

d)

Glass

22.

Fill in the blank: Drugs can be obtained from natural sources such as ________.

a)

Animals

b)

Plastic

c)

Steel

d)

Glass

23.

Fill in the blank: Drugs can be obtained from natural sources such as ________.

a)

Microorganisms

b)

Plastic

c)

Glass

d)

Metal

24.

What is the most common source of new drugs, even if originally obtained from natural sources?

a)

Organic synthesis

b)

Animal extraction

c)

Plant extraction

d)

Mineral extraction

25.

Which of the following is an example of a semisynthetic drug?

a)

Amoxicillin

b)

Benzodiazepines

c)

Aspirin

d)

Penicillin

26.

Fill in the blank: Semisynthetic drugs are produced by chemically altering a substance from a ________ source.

a)

natural

b)

synthetic

c)

artificial

d)

mineral

27.

Which of the following statements is true about synthetic drugs?

a)

They are produced entirely from chemical components with no natural source used.

b)

They are extracted from plants.

c)

They are always more expensive.

d)

They are less pure than natural drugs.

28.

Which of the following is NOT an advantage of drugs synthesized in the chemical laboratory?

a)

High purity

b)

Less expensive

c)

Slow production

d)

Large scale production quickly

29.

Fill in the blank: One advantage of drugs synthesized in the chemical laboratory is ________ purity.

a)

high

b)

low

c)

variable

d)

unknown

30.

What is genetic engineering in the context of drug sources?

a)

Direct manipulation of an organism’s genome (DNA chain) to produce drug

b)

Mixing chemicals to create drugs

c)

Extracting drugs from plants only

d)

Using only natural sources for drugs

31.

Which of the following is a technique used in genetic engineering for drug production?

a)

Recombinant DNA (rDNA)

b)

Herbal extraction

c)

Fermentation

d)

Distillation

32.

Fill in the blank: Monoclonal ________ are a technique used in genetic engineering to produce drugs.

a)

antibodies

b)

enzymes

c)

hormones

d)

cells

33.

In the diagram, a recipe is to cookies as a gene is to ________.

a)

protein

b)

sugar

c)

flour

d)

enzyme

34.

What is recombinant DNA (rDNA)?

a)

Ability to selectively hydrolyze a population of DNA molecules then join two different DNA molecules creating recombinant DNA (rDNA).

b)

A type of DNA found only in bacteria.

c)

A process of DNA replication in the nucleus.

d)

A method of synthesizing proteins from amino acids.

35.

Which type of cells are commonly used to manufacture proteins identical to those produced in human cells?

a)

Plant cells

b)

Nonhuman cells such as E. coli

c)

Fungi

d)

Animal cells

36.

Fill in the blank: Recombinant DNA technology utilizes _______ cells (ex: strain of E. coli) to manufacture proteins identical to proteins produced in human cells.

a)

nonhuman

b)

plant

c)

fungal

d)

animal

37.

According to the diagram, what enzyme is used to seal the overhangs after mixing donor and vector DNA?

a)

DNA polymerase

b)

DNA ligase

c)

RNA polymerase

d)

Restriction enzyme

38.

According to the diagram, what happens after recombinant DNA molecules are introduced into bacterial cells?

a)

The cells die

b)

The recombinant DNA molecules replicate and cells divide

c)

The DNA is destroyed

d)

Nothing happens

39.

What does mAb stand for?

a)

Monoclonal antibody

b)

Molecular acid base

c)

Microbial antigen binder

d)

Mammalian albumin

40.

Which of the following is an advantage of monoclonal antibodies?

a)

They can target multiple antigens at once

b)

They can design to specifically target one antigen

c)

They are produced only in bacteria

d)

They cannot be administered to patients

41.

Fill in the blank: Laboratory-produced copies of a specific protein (antibody) are called ________.

a)

monoclonal antibodies

b)

polyclonal antibodies

c)

antigens

d)

enzymes

42.

Which cells are fused with myeloma (cancer) cells to produce hybridomas in the production of monoclonal antibodies?

a)

T cells

b)

B cells

c)

Red blood cells

d)

Platelets

43.

What is the purpose of injecting a specific antigen into a mouse during the production of monoclonal antibodies?

a)

To trigger an immune response producing antibodies by B cells.

b)

To increase the mouse's lifespan.

c)

To make the mouse resistant to diseases.

d)

To improve the mouse's memory.

44.

Refer to the diagram showing an antibody binding to a biological substance (e.g., virus, bacteria, pollen) with antigens. What is the main function of the antibody as described in the diagram?

a)

To destroy the biological substance directly

b)

To bind to antigens and induce immune responses to eliminate the foreign intruder

c)

To produce more antigens

d)

To become part of the biological substance

45.

In the diagram, what are the structures on the surface of the biological substance that antibodies bind to called?

a)

Antigens

b)

Enzymes

c)

Hormones

d)

Receptors

46.

According to the diagram, bound antibody induces downstream immune responses to eliminate the ________.

a)

foreign intruder

b)

red blood cell

c)

antibody itself

d)

immune cell

47.

What is the purpose of drug discovery? (Fill in the blank)

a)

To find active ingredients or modify chemical structures of existing active ingredients of drugs to form the basis of a new agent.

b)

To increase the cost of medications for patients.

c)

To reduce the effectiveness of existing drugs.

d)

To create drugs with more side effects.

48.

Ideally, what does the process of drug discovery result in?

a)

A) A failed experiment

b)

B) A goal drug

c)

C) A new disease

d)

D) A new laboratory

49.

Fill in the blank: A goal drug can produce ________ effect.

a)

desired

b)

harmful

c)

temporary

d)

adverse

50.

Fill in the blank: A goal drug can be administered through the most desired route, usually ________.

a)

oral

b)

intravenous

c)

topical

d)

sublingual

51.

Fill in the blank: A goal drug can be administered at minimal ________ and frequency.

a)

dosage

b)

temperature

c)

pressure

d)

volume

52.

Fill in the blank: A goal drug shows optimal ________ and duration of activity.

a)

onset

b)

toxicity

c)

solubility

d)

cost

53.

Fill in the blank: A goal drug has ________ side effects.

a)

no

b)

many

c)

severe

d)

unpredictable

54.

Fill in the blank: A goal drug is eliminated from the body efficiently, with no ________ effects.

a)

residual

b)

immediate

c)

positive

d)

therapeutic

55.

Fill in the blank: The first step in starting a scientific investigation or drug discovery process is to _________.

a)

Identify target disease or indication

b)

Conduct clinical trials

c)

Develop a marketing strategy

d)

Submit a patent application

56.

Which backgrounds should be included when forming an investigative team?

a)

Chemistry, biology, toxicology, pharmaceutics, pharmacokinetics

b)

Literature, history, art, music

c)

Engineering, architecture, design, law

d)

None of the above

57.

Fill in the blank: Target validation involves ________ that action at that target affects disease progression.

a)

analysis

b)

guessing

c)

ignoring

d)

hoping

58.

What is the final step listed in the process of starting a scientific investigation or drug discovery process?

a)

Establish lead compound

b)

Formulate hypothesis

c)

Collect data

d)

Analyze results

59.

What is a lead compound?

a)

A compound with no biological activity

b)

A prototype with desired activity but other undesirable characteristics (ex: poor ADME profile)

c)

A compound with perfect ADME profile

d)

A compound used only in clinical trials

60.

Which of the following is a lead discovery method?

a)

Random screening

b)

Chromatography

c)

Spectroscopy

d)

Crystallization

61.

Which of the following is a lead discovery method?

a)

Drug metabolism studies

b)

X-ray diffraction

c)

Polymerase chain reaction

d)

Gel electrophoresis

62.

Which of the following is a lead discovery method?

a)

Clinical observations

b)

DNA sequencing

c)

Protein folding

d)

Cell lysis

63.

Which of the following is a lead discovery method?

a)

Rational design

b)

Mass spectrometry

c)

Western blotting

d)

Immunoprecipitation

64.

Which of the following is a lead discovery method?

a)

High-throughput screening (HTS)

b)

Southern blotting

c)

ELISA

d)

Flow cytometry

65.

Metabolites are isolated and screened to determine if the observed activity is derived from drug or metabolite.

a)

True

b)

False

66.

Nortriptyline is classified as which of the following?

a)

Antibiotic

b)

Antidepressant

c)

Antiviral

d)

Analgesic

67.

Nortriptyline is the active metabolite of ________.

a)

amitriptyline

b)

imipramine

c)

clomipramine

d)

desipramine

68.

Which is more potent: nortriptyline or amitriptyline?

a)

Nortriptyline

b)

Amitriptyline

c)

Imipramine

d)

Doxepin

69.

What is one way new uses for existing drugs are discovered according to clinical observations?

a)

When clinicians notice unexpected therapeutic effects.

b)

When drugs are only tested in animals.

c)

When patients request new uses for drugs.

d)

When drugs are used without any monitoring.

70.

Minoxidil was originally used for which condition?

a)

Hair loss

b)

High blood pressure

c)

Diabetes

d)

Morning sickness

71.

Thalidomide was used as a treatment for ________.

a)

morning sickness

b)

headache

c)

diabetes

d)

hypertension

72.

What does SAR stand for in the context of lead optimization?

a)

Structure-activity relationship

b)

Structure-activity reaction

c)

Substance-activity relationship

d)

Substance-activity reaction

73.

A drug candidate is a compound worthy of extensive biological, pharmacological, and animal testing.

a)

True

b)

False

74.

Fill in the blank: Activity refers to a particular ________ effect (e.g., antibacterial).

a)

biological

b)

chemical

c)

physical

d)

mechanical

75.

What does potency refer to in the context of lead optimization?

a)

The cost of the drug

b)

The strength of the biological effect

c)

The color of the compound

d)

The duration of testing

76.

IC50 is defined as ________.

a)

half maximal inhibitory concentration

b)

half maximal effective concentration

c)

maximum inhibitory concentration

d)

initial concentration of inhibitor

77.

EC50 is defined as ________.

a)

half the maximal effective concentration

b)

the dose that produces no effect

c)

the maximum tolerated dose

d)

the concentration at which 100% of the effect is observed

78.

What is the inhibition of AChE IC50 [nM] for compound number 15?

a)

6.4

b)

12.8

c)

0.9

d)

25.0

79.

Which compound has the lowest inhibition of AChE IC50 [nM]?

a)

9

b)

15

c)

E2020

d)

18

80.

What is the value of R2 for compound number 14?

a)

OMe

b)

NO2

c)

Cl

d)

CF3

81.

What is the value of R4 for compound number 16?

a)

OMe

b)

Cl

c)

NO2

d)

Br

82.

Which compound has R1 = OMe and R2 = H?

a)

17

b)

18

c)

19

d)

20

83.

What is the inhibition of AChE IC50 [nM] for compound number 20?

a)

20

b)

5

c)

50

d)

100

84.

What is the value of R3 for compound number 18?

a)

OMe

b)

NO2

c)

Cl

d)

Br

85.

Which compound has the highest inhibition of AChE IC50 [nM]?

a)

9

b)

14

c)

15

d)

16

86.

What is the name of the complex shown in the molecular diagram?

a)

E2020/AChE Complex

b)

Hemoglobin/Oxygen Complex

c)

ATP Synthase/ADP Complex

d)

DNA Polymerase/DNA Complex

87.

An oral drug must be able to ________.

a)

dissolve

b)

evaporate

c)

freeze

d)

ignite

88.

An oral drug must be able to survive a range of pHs. What is the pH range mentioned in the image?

a)

1.5 to 8.0

b)

2.0 to 10.0

c)

5.0 to 9.0

d)

0.5 to 7.0

89.

Which of the following must an oral drug be able to survive?

a)

Intestinal bacteria

b)

High temperature

c)

Low oxygen

d)

High pressure

90.

An oral drug must be able to cross membranes.

a)

True

b)

False

91.

An oral drug must be able to survive ________ metabolism.

a)

liver

b)

renal

c)

pulmonary

d)

gastric

92.

Which organ is responsible for excreting drugs via urine?

a)

Liver

b)

Kidneys

c)

Bile duct

d)

Bladder

93.

An oral drug must avoid active transport to ________.

a)

bile

b)

blood

c)

lymph

d)

saliva

94.

An oral drug must avoid excretion by which organ?

a)

kidneys

b)

lungs

c)

liver

d)

skin

95.

An oral drug should partition into the target organ.

a)

True

b)

False

96.

An oral drug must avoid partition into undesired places such as the ________ or foetus. (Fill in the blank)

a)

brain

b)

liver

c)

stomach

d)

intestine

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