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drug discovery > lecture 2 > Flashcards

lecture 2 Flashcards

1
Q

how are compounds in development named

A

the company developing them gives them a name and a number code

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2
Q

how are compounds that show promise as a therapeutic drug named

A

they are names referring to the disease theyre effective against

saquinavir + ritonavir for antiviral drugs (hiv)

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3
Q

what are marked medicines

A

medicine with a proprietry (owned by someone)

they have a name that only the owner company can use

nurofen, calpol etc

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4
Q

what is a proprietry name

A

a name given by the company that owns the medicine

the name is specific to the drug formulation

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5
Q

what is generic medicine

A

a drug that isnt covered by a patent application

many companies can sell, formulate and make profit from it (paracetamol)

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6
Q

similarity between generic medicine vs marketed medicine

A

same active principle
diff trade name

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7
Q

european law on generic drugs

A

generic medicines must have a international, non-proprietary name (rINN)

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8
Q

rINN

A

international
non proprietry name

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9
Q

what is the european, international non proprietary name

A

usually the name of the drug

paracetamol, ibuprofen

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10
Q

british approved names had to be changed to what

A

the international
non proprietry
names

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11
Q

what is a drug class

A

medicine with:

similar chemical structures

same mechanism of action (binds to the same target)

used to treat similar diseases

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12
Q

what is a drug class defined by

A

a prototype drug

usually the first developed drug in that class

used as a reference to allow comparison

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13
Q

what is the ATC

A

anatomical
therapeutic
chemical
classification
system

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14
Q

how does ATC classify drugs

A

classifies the active ingredient based on the organ or system that its therapeutic, pharmacological or chemical properties act upon

aka what does this drug affect!!

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15
Q

what is the purpose of classifying drugs under ATC

A

allows us to monitor its use for research + improve quality medication use

eg: oh wow this is classified under cardiovascular system so it is probably mostly used for the heart<3

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16
Q

how many levels of ATC are there

A

5

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17
Q

what is the first level of ATC system

A

anatomical group it effects

1letter (a,b,c,d)

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18
Q

2nd level of ATC system

A

therapeutic subgroup

2 digits

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19
Q

what is therapeutics

A

treatment + healing

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20
Q

what is pharmacological

A

uses + effects

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21
Q

third level of ATC system

A

indicated the therapeutic/pharmacological subgroup

1 letter

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22
Q

forth level of ATC system

A

chemical/therapeutic/pharmacological subgroup

1 letter

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23
Q

5th level of ATC system

A

chemical substance

2 digits

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24
Q

drug definition

A

raw material from animal/vegetable origin that contains active principles that alterates the normal functioning of the CNS when introduced to the b ody via any administration

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25
Q

drug || definition

A

a biologically active, chemically pure substance that has a therapeutic action.

  • reacts with biological environment + has the ability of curing, mitigating or preventing disease in humans/animals)
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26
Q

mitigating meaning

A

reducing severity of something

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27
Q

medicine definition

A

drug in its proper dosage form, used in medication

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28
Q

drug / medicine definition difference

A

drug: compound

medicine: tablet: its proper dosage

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29
Q

drug target

A

biological entity (protein/gene) that interacts + has its activity modulated by a particular compound

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30
Q

modulated meaning

A

controlling somethings influence

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31
Q

druggable meaning

A

smt is druggable if its activity, behaviour or function, can be modulated by a therapeutic

therapeutic: small molecule/ biologics

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32
Q

biological target example

A

nucleic acids
proteins

33
Q

7 stages from finding a drug to getting it on the market

A
  • early stage research + discovery
  • preclinical studies in animals
  • phase 1
  • phase 2
  • phase 3
  • fda review + approval
  • post approval
34
Q

what is phase 1 clinical development

A

focuses on safety
20-80 healthy ppts

1-2 years

35
Q

what is phase 2 of the clinical development

A

efficacy + safety

100-300 patients

1-2 years

36
Q

what is phase 3 clinical development

A

efficacy + safety
1,000-3,000 patients

2-3 years

37
Q

how long does approval from the fda last

A

1 - 2 years

38
Q

how many compounds are are lost during the process

A

from 5,000 - 10,000 (drug discovery + preclinical)

to 1 fda approved drug (fda review)

39
Q

how much does drug discovery cost + take

from the original idea to launching the finished product

A

1.5 billion dollars

12 - 15 years

40
Q

what must u do before identifying a target

A

find an unmet medical need

we must identify a disease in order to identify targets

41
Q

who is the concept of unmet medical need important to

A

stakeholders and regulators

42
Q

what is a stakeholder

A

rich companies that have interests in ‘x’

43
Q

what is a regulator

A

payers
academics
pharma industries
health technology assessment agencies (HTA)

44
Q

whats so important about unmet medical needs

A

theyre personal to everyone
everyones unmet need is different

should focus on all unmet needs as theyre all uncomforatble (not just unmet needs for critical or debilitating conditions)

45
Q

whats a debilitating condition

A

a condition that makes someone weak or infirm

46
Q

how and where do UMN occur

A
  • when current therapies that are available do not address a condition
  • when there are no approved molecules
  • when there are a few molecules in the late part of clinical studies (not out yet)
  • existing molecules are compromised by taking the effective dose of ‘x’.
47
Q

development of new medicine is driven by what ambition

A

treating unmet medical needs

the UMN drives ppl to want to meet these needs.

48
Q

list of therapeutic areas

A

-cancer
-cardiovascular diseases
-diabetes
-hiv , aids
- immune system diseases
- neurodegenerative diseases
- viral diseases

49
Q

what is a drug target

A

a biomolecule that is directly associated with the disease + is responsible for the cellular or molecular function

50
Q

drug target examples

A

enzymes // proteins
receptors
metabolic pathways / apoptosis
lipid membrane
ion channles
dna/rna

51
Q

what is the benefit of discovering a drug target

A

allows researchers to optimize the drug for a particular disease or condition

52
Q

optimise meaning

A

make it the best
identify its most effective use

53
Q

drug target characteristics

A
  • confirmed role in pathophysiology of a disease/ is disease modifying
  • expression is not evenly distributed throughout the body
  • its 3d structure is availabe to assess druggability
  • easily assayable/tested allowing screening
  • has a promising toxicity profile, adverse affects can be predicted using phenotypic data
  • favourable intellectual property status (IP) (relavent for big pharma as it shows how its marketed and sold)
54
Q

what is the modern drug discovery process

A

target identification
target charactisation
target validation

55
Q

initial hypothesis in drug discovery

A

that a particular molecule is the key or causes a pathogenic or symptomatic mechanism in a disease.

eg: hypothesising that this molecule causes the inflammation etccc.

56
Q

target identification in drug discovery

A

identifying the function of a possible therapeutic target (gene/protein) and its role in the disease

eg: identifying ‘x’ is the drug target bc iit causes the inflammation

57
Q

in drug discovery what is target identification followed by

A

target characterisation of the molecular mechanism addressed by the target

  • u found the target, now u need to see its mechanism for how it causes the inflammation
58
Q

target validation in drug discovery

A

shows that modulation of the target is likely to have a therapeutic effect

59
Q

modulation meaning

A

controlling its influence

60
Q

what is the goal in target identification

A

to find a biological target (protein//nucleic acid) whos activity can be regulated with a therapeutic

61
Q

target identification techniques

A

in silico
laboratory

62
Q

in silico target identification technique

A

silico screening
machine based methods
experimentation performed by a computer

63
Q

laboratory target identification technique

A

biological assays such as expression profiling of rna or proteins

aka measuring which genes from the genome are being expressed in particular cells at any given time

or functional screening: gene knockdown, knockout, overexpression

64
Q

what is gene knockdown

A

reducing the genes expression

65
Q

what is gene knockout

A

eliminating the gene

66
Q

what is gene overexpression

A

turning certain genes on

67
Q

what is target validation

A

ensuring that engagement of the target has potential therapeutic benefits

aka if we do smt to the target, will it lead to a positive effect.

68
Q

2 approaches to target validation

A

chemical + genetic approach

69
Q

chemical approach to target validation

A

involves the use of drugs to show that inhibition of the target results in disease inhibition

70
Q

genetic approach to target validation

A

target gene knockdown (reduced expression) - rna

target gene knockout (gene elimination) - gene

71
Q

target validations can be divided into what 2 groups

A

in vivo

in vitro lab tests

72
Q

in vivo division of target validation

A

use of disease models (animals)
use of animal alternatives: worms, microorganisms, computer models, 3d tissue cultures.

73
Q

in vitro division of target validation

A

lab tests
- cell/ tissue based experiments
- parameters are studied (ionic conc, enzyme activity, protein expression profiles)
-study of the targets biological function when bound to different ligands (diff drug candidates)

74
Q

what is a parameter

A

a measurable factor that defines a system

75
Q

stages of early stage research + discovery

A

target identification
hit generation
lead generation

76
Q

what is found in the hit generation

A

%wegotahit!

finding compounds that engage with the bio target + have good properties

77
Q

what is the lead generation in the early research and discovery stage of drug discovery

A

%theyretakingthelead

from the possible hits

analysis + improvement of compounds with pharmacological activity, the correct potency, solubility + stability

78
Q
A

drug discovery (18 decks)

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