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Biomedical Pharmacology > Lecture 6 - Drug Discovery > Flashcards

Lecture 6 - Drug Discovery Flashcards

1
Q

Preclinical development

A

Ensure you are developing a drug that has a suitable target for the disease

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2
Q

Why is it necessary to have appropriate formulation of a drug?

A

Aid it’s absorption

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3
Q

Drug discovery

A

Target selection Lead finding Lead optimisation Pharmacological profiling (2-5 years)

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4
Q

Preclinical development

A

Pharmacokinetics Short term toxicology Formulation Synthesis scale up (1.5 years)

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5
Q

Clinical Development: Phase I

A

Pharmacokinetics Tolerability Side-efffects in healthy volunteer

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6
Q

Clinical Development: Phase II

A

Small-scale rials in patients to assess efficacy and dosage Long-term toxicology studies

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7
Q

Clinical Development: Phase III

A

Large scale controlled clinical trials

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8
Q

Regulatory Approval

A

Submission of full date and review by regulatory agencies (1-2 years)

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9
Q

Phase IV

A

Post marketing surveillance

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10
Q

Main aims of pre-clinical

A

Pharmacology Toxicology

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11
Q

Subjects of pre-clinical

A

In vitro, laboratory, animals

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12
Q

Main aims of Phase I

A

Clinical pharmacology and toxicology Drug metabolism and bioavailability Evaluate safety

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13
Q

Subjects of Phase I

A

Healthy individuals and/or patients

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14
Q

What is the main aim of phase II?

A

Initial treatment studies Evaluate efficacy

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15
Q

Subjects for phase II ?

A

Small number of patients

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16
Q

What is main aim of Phase III?

A

Large randomised controlled trials Comparing new to old treatments Evaluate safety and efficacy

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17
Q

Subjects for phase III?

A

Large number of patients

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18
Q

What is the main aim of Phase IV?

A

Post-marketing surveillance Long term safety and rare events Yellow card scheme

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19
Q

Subjects of Phase IV?

A

All patients prescribed the drug

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20
Q

Drugs acting on GPCR have what percentage of market value?

A

50%

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21
Q

what do current drugs interact with?

A

Only a fraction of the available receptors

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22
Q

What do other functional proteins include?

A

Other receptors, enzymes, transport proteins

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23
Q

What are targets?

A

Proteins in the patient body associated with disease Identify which proteins are relevant

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24
Q

What are the methods utilised to identify lead compounds?

A

Synthetic or medicinal chemistry

25
Q

How to identify lead compound?

A

Put them through high-throughout screening (HTS) Purified proteins are target

26
Q

Fluorescence-based assay

A

Preferred in terms of how quickly they can give results on time scale basis

27
Q

A lot of high-throughout screening is what?

A

Automated

28
Q

What does HTS allow researchers to do?

A

Identify active compounds, antibodies or genes that modulate a biomolecular pathway

29
Q

Filter down compounds

A

See which one produces a desired effect Look at the affinity of a compound for a receptor that generate a dose response curve

30
Q

Lead compound

A

Prototype chemical with biological activity May not have all desired qualities of target drug Might have undesired properties

31
Q

How do you narrow down 1000s of compound into a single molecule?

A

High-throughout screening Silicon profiling (computer modelling)

32
Q

Efficacy in disease model

A

Cell culture model Use cells that are cultured to express receptor of interest Certain strains of laboratory rats are bred because they are spontaneously hypertensive As they age: develop hypertensive profile

33
Q

What is the hypertensive profile used for?

A

To investigate the potential efficacy of drugs used for the treatment of high blood pr sure or hypertension

34
Q

What can high dosage of drug be?

A

Poisonous

35
Q

Maximal response EC50

A

Desired effect

36
Q

How does undesirable effect emerge?

A

As the drug concentration increases

37
Q

Therapeutic index

A

Measurement of drug safety

38
Q

Therapeutic index

A

Indication of separation between 2 EC50

39
Q

Low therapeutic index

A

Little separation

40
Q

What does non life-threatening disorder often demand?

A

High therapeutic index

41
Q

What may life-threatening disorder be able to tolerate?

A

Side effects

42
Q

What are the preclinical development?

A

Safety pharmacology Preliminary toxicology Pharmacokinetic testing Chemical and pharmaceutical development

43
Q

Where does toxicology start?

A

Non-GLP (non-good laboratory practice)

44
Q

What is GLP used for?

A

New drug application

45
Q

Who does the toxic exploratory toxicology inform?

A

Regulatory toxicology

46
Q

Which toxicology is more intensive?

A

regulatory

47
Q

What is the Ames test used to screen?

A

Chemicals that may be mutagens

48
Q

What does Ames test use?

A

Bacteria to identify potential carcinogen

49
Q

What is the first steps of Ames Test?

A

Selection of the suspected mutagens

50
Q

Second step of Ames test

A

The selected mutagens is mixed with rat liver extract (stimulate body chemisry)

51
Q

Third step of Ames Test

A

Expose bacteria to mutagen-rat liver mix

52
Q

When is the first submission to the regularity authorities madeV

A

Before a drug is taken into preclinical studies phase of the drug developmental process

53
Q

Where are regulatory authorities found?

A

Different countries/ different regions

54
Q

Phase I Trial Design

A

Small group of volunteers (20-80) Subjects intensively monitored for signs of toxicity: ECG/blood pressure/heart rate/Liver and Renal function/ Blood/ Urinalysis Tolerability Pharmacokinetic properties Pharmacodynamic effect “proof of concepts”

55
Q

What lead compound was developed an anti-inflammatory found in pre-clinical settings?

A

TGN1412

56
Q

What compound is used in analgesics?

A

BIA 10-2474

57
Q

Phase II / initial patient studies

A

Study patients with the disease (100-300) Typically performed in hospital clinic setting with experienced clinic investigator Determine pharmacodynamic effect, establish dose regimen to use in definitive Phase III studies Completion allows determination of whether initial hypothesis was correct (drug will treat condition X)

58
Q

Phase III - large scale Efficacy Trials

A

Multi-centred trials involving upwards of 1000 patients Usually double blind, randomised trials comparing with existing standard drugs. Pharmacoeconmic analysis undertaken

59
Q

Phase IV - post marketing surveillance

A

Long term monitoring of value of drug

Biomedical Pharmacology (19 decks)

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