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Blockbuster Drugs > Case Study: Advair/Seretide > Flashcards

Case Study: Advair/Seretide Flashcards

1
Q

When was it launched and who by?

A

1999 by GSK

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2
Q

What is it a combination of?

A

fluticasone propionate (Flovent) and salmeterol xinofoate (Serevent)

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3
Q

What is Advair used to treat?

A

Asthma and COPD

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4
Q

What form is it available in?

A

A dry powder or aerosol

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5
Q

What is Salmeterol?

A

A long acting B2-agonist (LABA)

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6
Q

What does activation of B2-receptors do?

A

Relaxes smooth muscle

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7
Q

What are B2 receptors?

A

Adrenergic receptors

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8
Q

Where are B2 receptors mostly found?

A

Bronchial smooth muscle for dilation of airways

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9
Q

What interactions are important for binding?

A

Pi bonds betwee Phe-290 and drug. H bonds to Asn-293, H bonds to Ser-207 and Ser-204

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10
Q

What happens if you increase the chain length between the ring and N?

A

It reduces the activity

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11
Q

When is adrenaline used but why is it bad?

A

In an emergency, is short acting and has no selectivity so will act on adrenergic receptors all over the body

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12
Q

What is good and bad about isoprenaline?

A

It is selective for B-receptors but not B2 receptors and is short acting

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13
Q

Why is isoprenaline short acting?

A

Metabolism by COMT enzyme which converts the meta OH phenol to an OMe and inactive metabolite

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14
Q

What modification does Salbutamol have and what does this mean for selectivity?

A

extra CH2 group before OH group and has the same potency but is 2000 times less active on the heart and lasts 4 hours.

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15
Q

What are the enantiomeric effects of Salbutamol?

A

R-salbutamol is 68x more active than S but S enantiomer tended to coagulate in tissue so more undesirable side effects though lots of doctors still prescribe the racemate.

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16
Q

Name and describe the benefits of an extension analogue

A

Salmefamol has 1.5x potency and lasts 6 hours

17
Q

What is good about Salmeterol?

A

More lipophilic drug increases duration of action-stronger binding in tissues, accumulates. Has 2x potency and 12 hour duration.

18
Q

What is fluticasone?

A

Glucocorticoid and inhaled corticosteroid

19
Q

What does fluticasone do?

A

Reduces inflammation in the lungs

20
Q

What is fluticasone’s mode of action?

A

It binds to glucocorticoid receptors causing suppression of inflammatory response and increase of anti-inflammatory proteins. reduces blood flow to mucosal linings.

21
Q

What are the advantages of the combination?

A

It is the best selling FDC drug, the combined ISC/LABA is now the accepted standard. greater efficacy than just increasing the steroid dose. Synergistic efficacy shown in comparison to use of individual inhalers. Improved patient compliance.

22
Q

What are the competitors, who made them and what are they?

A

Symbicort (AstraZeneca) made of Budesonide (ISC) and Formoterol (LABA). Dulera (Merck) made of Mometasone (ICS) and Formoterol (LABA)

23
Q

Of the ISC and LABA, which is the longer lasting?

A

ISC

24
Q

Describe the patent history

A

Salmeterol patent eexpired 2005 and generic launched in 2011 (TEVA)
patent on active ingredients expired in 2010 (US) and 2013 in UK/EU
Still selling over $7b worldwide/year
inhaler devices difficult to copy and patent on the discuss inhaler expired in 2016.

25
Q

When was AirFluSal approved and what rare there disputes about?

A

2013/14 and disputes over its colour

26
Q

What happened when TEVA organised a generic launch in Jan 2017?

A

Advair revenues down 13% first half of 2017

27
Q

What are the new drugs for COPD?

A

Breo/Relovair produced Fluticasone furoate (ISC) and vilanterol (LABA) and Anoro produced Umeclidinium (anticholinergic) and vilanterol (LABA)

28
Q

What are two advantages of the fluticasone furoate?

A

Furan has enhanced selectivity for receptor sites and can be taken once a day instead of twice.

29
Q

What factors are important in protecting the market share?

A

Marketing, price, compliance

Blockbuster Drugs (5 decks)

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