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PHA6125 Drug Discovery and Development > 2 | Overview of DDD > Flashcards

2 | Overview of DDD Flashcards

1
Q

Majority of research at this stage is publicly funded at universities, colleges and independent research institutions in every state

A

Basic Research

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2
Q

Once a disease target is identified, drugs are designed and tested.

A

Clinical trials

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3
Q

T/F: Both public and privately funded research are involved in clinical trials.

A

True

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4
Q

Human trials are completed including FDA approval

A

Regulatory approval

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5
Q

Industry is responsible for bringing a drug to market

A

Regulatory approval

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6
Q

T/F: Safety and evaluation does not continue after regulatory approvals

A

False

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7
Q

Practice of Pharmacy

A

Patient Care

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8
Q

Deals with drug formulations and dosage forms

A

Pharmaceutics

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9
Q

Deals with pharmacotherapeutics and clinical pharmacy

A

Pharmaceutical Chemistry

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10
Q

Clinical trials include how many phases?

A

Three

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11
Q

Basic research is involved in?

A

Medicinal Chemistry

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12
Q

Therapeutic concept is also known as

A

Objective

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13
Q

Pertains to finding a protein responsible for disease development

A

Target Selection

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14
Q

Steps involved in Discovery

A
  1. Target selection
  2. Target validation
  3. Lead finding
  4. Lead optimization
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15
Q

Lead finding

A

Lead compound

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16
Q

Lead optimization

A

Candidate drug

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17
Q

Steps involved in Development

A
  1. Preclinical development
  2. Clinical development
  3. Regulatory approval
  4. Registration
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18
Q

Commercialization involves

A
  1. Clinical development
  2. Regulatory approval
  3. Registration
  4. Product
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19
Q

biomolecule to which the drug will bind (through a specific binding site)

A

Target

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20
Q

Often responsible for (or related to) the disease chosen for the research

A

Target

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21
Q

T/F: Majority of drugs target nucleic acids and lipids, although a protein molecule is occasionally targeted too

A

False

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22
Q

Blockbuster drug that targets beta-adrenergic receptors

A

Salbutamol

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23
Q

Blockbuster drug that targets alpha-adrenergic receptors

A

Phenylephrine

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24
Q

Blockbuster drug that targets muscarinic receptors

A

Atropine

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25
Q

Blockbuster drug that targets serotonin transporters

A

Sertraline

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26
Q

Blockbuster drug that targets calcium channels

A

Nifedipine

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27
Q

Blockbuster drug that targets angiotensin converting enzyme

A

Enalapril

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28
Q

Blockbuster drug that targets acetylcholinesterase

A

Neostigmine

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29
Q

Drug that acts as HMG CoA reductase inhibitor

A

Atorvastatin

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30
Q

Possess an opposite effect as compared to atropine

A

Physostigmine

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31
Q

Medication category of Nifedipine which lowers BP

A

CCBs

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32
Q

Requires molecular biology techniques to allow testing of multiple candidate targets

A

Target Identification and Validation

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33
Q

Use of microarray plates to find which proteins are responsive to a disease

A

Target Identification and Validation

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34
Q

Found between target validation and lead finding

A

Compound preparation

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35
Q

Prepares compound found in the boundary of target identification and target finding

A

Compound preparation

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36
Q

T/F: DDD projects can start without the presence of a series of compounds to test

A

False

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37
Q

A series of compounds also pertain to

A

A compound library

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38
Q

Cycle of prepare, test, prepare, test, prepare…

A

Compound preparation

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39
Q

Series of trials and errors

A

Compound preparation

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40
Q

For _________________ projects, simple modifications to make a handful of compounds is enough

A

small scale

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41
Q

For ___________________, synthetic strategies can produce thousands to millions of compounds

A

pharmaceutical companies

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42
Q

Small scale project (e.g, academic research) is usually funded by?

A

Government

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43
Q

molecules with potential to be selected as leads

A

Hit

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44
Q

generated during the initial screening process

A

Hit

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45
Q

type of hit that is chosen during lead finding to become leads

A

most active hits

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46
Q

contains toxicity, not refined

A

Hit

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47
Q

can be a candidate for a drug compound

A

Hit

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48
Q

selected hits that can have not only potency but also safety and other qualities wanted in a drug

A

Leads

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49
Q

less toxic than hit, but is not considered safe due to lack of animal testing done

A

Leads

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50
Q

How does a molecule become a hit?

A

Needs to have confirmed activity

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51
Q

Requirements to become a lead

A
  1. Must have confirmed activity
  2. Show evidence of desired selectivity
  3. Have activity in cellular systems
  4. Stability in biologic systems
  5. Free from toxicity alerts
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52
Q

T/F: If a lead becomes toxic, it should be stopped

A

True

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53
Q

hits are validated, then tested to assess if they can become leads

A

Lead generation/ identification/ finding

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54
Q

The stage of finding hits to finding leads

A

Lead generation/ identification/ finding

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55
Q

Stage done just before optimization and is sometimes combined to the term H2L generation

A

Lead generation/ identification/ finding

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56
Q

H2L generation means

A

hit-to-lead generation

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57
Q

Requires selection and validation of target first

A

Lead generation

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58
Q

generated during the initial screening process

A

Hit

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59
Q

closer but still not perfect, so they undergo an extra process

A

Lead

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60
Q

Leads are closer but still not perfect, so they undergo an extra process called

A

lead optimization

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61
Q

Improvement of a lead’s PD, PK, and toxicity profiles suitable for future stages of the DDD pipeline

A

lead optimization

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62
Q

T/F: Already-existing leads will never be perfect for very specific purposes

A

True

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63
Q

The first and only stage in discovery where synthesis is intentional and not a mere guessing game

A

lead optimization

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64
Q

May involve improvements in potency, efficacy, or safety profile of a drug

A

lead optimization

65
Q

Converts “close enough” leads to “certain” drug candidates

A

lead optimization

66
Q

biological/ biochemical testing to get initial data

A

Structure-activity relationship (SAR)

67
Q

Results to diagrams showing how modifying a part of the lead’s/drug’s structure changes it’s activities

A

lead optimization

68
Q

Gives birth to drug analogues and drug generations

A

lead optimization

69
Q

Potent activity against gram-positive

A

1st generation cephalosporin

70
Q

Mediocre activity against gram-negative bacteria

A

1st generation cephalosporin

71
Q

Example of a 1st generation cephalosporin

A

Cephalotin

72
Q

1st generation cephalosporin became available for use during [year]

A

1964

73
Q

Expanded spectrum of activity

A

2nd generation cephalosporin

74
Q

Better cell penetration

A

2nd generation cephalosporin

75
Q

Increased resistance to Beta-lactamases

A

2nd generation cephalosporin

76
Q

Slightly less potent against gram-positive

A

2nd generation cephalosporin

77
Q

Considerable more active against gram-negative

A

2nd generation cephalosporin

78
Q

Example of a 2nd generation cephalosporin

A

Cefuroxine

79
Q

2nd generation cephalosporin became available for use during [year]

A

1983

80
Q

Improved activity against gram-negative

A

3rd generation cephalosporin

81
Q

Like a 2nd gen cephalosporin, it also has better cell penetration

A

3rd generation cephalosporin

82
Q

Higher binding towards bacterial arget

A

3rd generation cephalosporin

83
Q

Example of a 3rd generation cephalosporin

A

Ceftazidime

84
Q

3rd generation cephalosporin became available for use during [year]

A

1985

85
Q

Improved resistance to beta-lactamases

A

4th generation cephalosporin

86
Q

Wider spectrum of activity

A

4th generation cephalosporin

87
Q

Higher activity against both gram-positive and against gram-negative

A

4th generation cephalosporin

88
Q

Example of a 4th generation cephalosporin

A

Cefepime

89
Q

4th generation cephalosporin became available for use during [year]

A

1994

90
Q

Approved for tx of critical infections (e.g., hospital-acquired pneumonia)

A

5th generation cephalosporin

91
Q

Example of a 5th generation cephalosporin

A

Ceftobiprole

92
Q

5th generation cephalosporin became available for use during [year]

A

2013

93
Q

T/F: Discovery is shorter, but development is more expensive.

A

True

94
Q

Studies involving animals extensive toxicity studies in animals

A

Preclinical testing

95
Q

Done to predict the risks that will be associated with administering the drug to humans

A

Preclinical testing

96
Q

May not reveal all of the adverse effects that will be found in human subjects

A

Preclinical testing

97
Q

the first occasion at which a compound is tested in live organisms

A

Preclinical PK study

98
Q

Compounds targeted as oral therapies are administered as?

A

IV and PO

99
Q

Why are compounds targeted as oral therapies are administered as both IV and PO?

A

to compute bioavailability

100
Q

residence time in lung is considered for?

A

inhaled/topical drugs

101
Q

high solubility is given even more importance for

A

IV drugs

102
Q

Concurrent to pharmaceutical development

A

Preclinical testing

103
Q

proper dosage form, delivery system, and route of administration for the final product

A

Pharmaceutical development

104
Q

Pharmaceutical development involves two phases

A
  1. Preformulation studies
  2. Formulation phase
105
Q

Preparatory analysis

A

Preformulation studies

106
Q

Utilizes pharmaceutical analysis and physical pharmacy tests

A

Preformulation studies

107
Q

In Preformulation studies, ________ is tested all the time to assess shelf life

A

Stability

108
Q

actual formulation of the product

A

Formulation phase

109
Q

Requires good background of excipients and drug manufacturing

A

Formulation phase

110
Q

Includes a complete description of the drug, results of preclinical studies, and description of the proposed clinical studies and the qualifications of the investigators

A

Investigational New Drug (IND) Application

111
Q

Pharmacokinetic properties and safety of an IND in healthy human subjects

A

Phase I IND

112
Q

Efficacy on diseased subjects not yet measured

A

Phase I IND

113
Q

First studies on human subjects who have the particular disease the IND is targeting

A

Phase II IND

114
Q

Small number of patients only

A

Phase II IND

115
Q

Employ a larger group of subjects (hundreds to thousands)

A

Phase III IND

116
Q

Multiple centers, wide variation of study methods

A

Phase III IND

117
Q

Final phase before approval

A

Phase III IND

118
Q

Toxicity testing is still significant further into the preclinical and clinical phases of the DDD pipeline

A

Safety

119
Q

Post-Development includes

A
  1. New Drug Application (NDA)
  2. Postmarketing Surveillance
120
Q

Includes the results of all preclinical and clinical studies, as well as the proposed labeling and clinical indications for the drug

A

New Drug Application (NDA)

121
Q

Last hurdle before reaching the market

A

New Drug Application (NDA)

122
Q

Also referred to as Phase IV

A

Postmarketing Surveillance

123
Q

Some drugs are found to have other clinical uses after the drug has been introduced to the market

A

Postmarketing Surveillance

124
Q

Covered by the pharmacovigilance sector

A

Postmarketing Surveillance

125
Q

In some cases, old drugs are revisited for new purposes

A

Postmarketing Surveillance

126
Q

Within the glass

A

In vitro

127
Q

Use of isolated tissue/ cell samples for testing

A

In vitro

128
Q

Versatile and applicable on a wide range of tissues

A

In vitro

129
Q

Approximation to the normal functioning of the tissue

A

In vitro

130
Q

In vitro

Activity depends on permeation through the membrane for?

A

Compounds acting on intracellular activity

131
Q

In vitro

T/F: A very wide range of physiologic responses can be addressed by studies on isolated tissues

A

True

132
Q

Concentration-effect relationships can be accurately measured, and design of the experiments is flexible

A

In vitro

133
Q

In vitro shortcomings

T/F: Tissues does not normally have to be obtained from small laboratory animals

A

False (normally)

134
Q

In vitro shortcomings

T/F: Preparations often survive for more than a day, allowing only short-term experiments

A

False (rarely survive)

135
Q

Within the living

A

In vivo

136
Q

Uses animals that express similar physiology/ pathology relevant to the research

A

In vivo

137
Q

time-consuming, technically demanding and expensive

A

In vivo

138
Q

Subject to considerable ethical and legal constraints, and face public opposition

A

In vivo

139
Q

Use today is much more limited, especially to later stages

A

In vivo

140
Q

In vivo

T/F: Imaging technologies are increasingly being used for studies on whole animals

A

True

141
Q

In vivo

T/F: Physiology of disease processes and drug metabolism differs markedly in different species

A

True

142
Q

Nevertheless is essential part of every major drug discovery project and represents a valuable link in the chain of evidence

A

In vivo

143
Q

intended to mimic certain manifestations of the clinical disorder

A

Acute models

144
Q

Histamine- induced bronchoconstriction, hotplate test for inflammation, elevated maze for anxiety, etc. are examples of?

A

Acute models

145
Q

Involve use of agents that induce an abnormality similar to the clinical conditions

A

Chronic models

146
Q

Alloxan- induced DM1, administration of dependence-inducing drugs, cholesterol feeding for atherosclerosis, etc. are examples of?

A

Chronic models

147
Q

Allowed inbred strains to be produced that over- or under-express particular genes that lead to conditions (e.g., inborn disease) that allow testing to take place

A

In vivo

148
Q

In vivo

T/F: Use of transgenic animal models has led to an increase, rather than decrease, in animal experimentation

A

True

149
Q

When used in DDD context, is often called
computer-aided drug design (CADD)

A

In silico/Virtual

150
Q

Computational programs that generate “models” to separate molecules that are likely to work vs. those that are less likely to work

A

In silico/Virtual

151
Q

Used early in the discovery phase to avoid costs from using in vitro methods

A

In silico/Virtual

152
Q

Considered dry lab experiments as it does not use actual reagents or lab apparatuses (traditional wet lab)

A

In silico

153
Q

though with altruistic and commercial aims in their mission statements, the profit necessarily takes priority

A

Industry

154
Q

In Industry:

Freedom is ___________________, teamwork ______________, and has little room for the lone genius

A

more limited; obligatory

155
Q

In Industry:

Publication means compromising ________________, and compromising _____________

A

patent; profit

156
Q

researchers are substantially constrained to work on projects that attract funding support; more free to publish

A

Academia

157
Q

In Academia:

Under much more pressure to do so since _____________ are their measure of research achievement

A

publications

158
Q

Publish or perish culture

A

Academia

PHA6125 Drug Discovery and Development (3 decks)

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