How are medicines developed?

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Presentation on drug development accompanying the hands-on experiment "How are drugs developed?"

To download the experiment protocol and other educational resources on health research, visit: www.xplorehealth.eu

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How are medicines developed?

  1. 1. How are medicinesdeveloped?
  2. 2. What is it?What’s inside?
  3. 3. What is inside a medicine?
  4. 4. Active ingredientIt looks for thetherapeutic target to Therapeutic targethave an effect and curethe disease
  5. 5. Active ingredientIt looks for thetherapeutic target to Therapeutic targethave an effect and curethe disease
  6. 6. How are medicines developed?
  7. 7. DEVELOPMENT SEQUENCE IN THE SEARCH FOR A MEDICINE The search for a medicine is a long (10-25 years), complex and expensive process consisting of several stages. DRUG PRECLINICAL Launch CLINICAL DEVELOPMENT of the R&D STUDIES(2-10 years) (2-6 years) drug PHASE I  PHASE II  PHASE III In vitro/In vivo PHASE IV
  8. 8. HOW IS A DRUG CANDIDATE DISCOVERED? • A drug candidate can be discovered in different ways: ?
  9. 9. HOW IS A DRUG CANDIDATE DISCOVERED?A drug candidate can be discovered in different ways: Serendipity Massive screening chance Chemical modification Rational design
  10. 10. WE NOW HAVE A DRUG CANDIDATE!
  11. 11. PRECLINICAL DEVELOPMENT• A thorough and complete preclinical study is required before we can test a drug in humans:• These preclinical studies include: – Stability and toxicity studies ©Parc Científic Barcelona. Author: J. Planagumà – In-vitro tests (proteins, cells, tissues and organs) – In-vivo tests (animals)
  12. 12. CLINICAL DEVELOPMENT• Clinical development is the longest and most costly part of the search for new medicines. It consists of three phases: PHASE III PHASE II PHASE I Healthy volunteers Patients (100-300) Patients Safety and (drug or placebo) (1300-3000) dose Efficacy and Long-term side effects effects
  13. 13. AND FINALLY… THE DRUG IS LAUNCHED ON THE MARKET!• If the drug has successfully passed the three clinical phases, it is launched on the market, but the study continues (Phase IV) PHASE III PHASE II PHASE I PHASE IV
  14. 14. SEARCH for DRUGS forPARKINSON’S DISEASEThe Barcelona Science Park research project
  15. 15. INTRODUCTION – WHAT IS PARKINSON’S DISEASE?• Parkinson’s disease (PD) is a chronic and progressive movement disorder characterised by: – Coordination problems – Slowed movements – Generalised tremor• It is the second most common neurodegenerative disease and affects 1-2% of people over 60. There are currently more than 4 million people suffering from PD worldwide.
  16. 16. INTRODUCTION – PARKINSON’S DISEASE, CAUSES• Our brain is our body’s control centre and the cells responsible for it are called neurons. These cells self- regenerate very slowly.• Neurotransmitters are special chemical compounds that enable neurones to “talk to each other” and communicate.
  17. 17. INTRODUCTION – PARKINSON’S DISEASE, CAUSES• We still do not know what causes Parkinson’s disease, but we do know that it is due to the loss or incorrect functioning of the neurons responsible for producing dopamine, a neurotransmitter. • Dopamine  Control of movement• Dopamine is responsible for transmitting the signals required to control the movement  our muscles. the control Low dopamine levels of Difficulties in of movement• A dopamine deficiency therefore leads to an imbalance in neuronal transmission, preventing neurons from communicating properly. This leads to a loss of motor function.
  18. 18. INTRODUCTION – PARKINSON’S DISEASE, TREATMENT • The way to treat the disease’s progression is by taking oral medicines. tyrosine L-dopa dopamine vesicles with the dopamine transmitter • The most commonly used medicine today is levodopa, or L-dopa, which consists of a chemical compoundsynapse that the brain uses to produce dopamine.dopaminereceptor receptor cell
  19. 19. INTRODUCTION – PARKINSON’S DISEASE, TREATMENT• Other medicines, which imitate the effect of dopamine in the brain, are also used. – e.g. bromocriptine, lisuride, pergolide, ropinirole, etc. dopamine imitator receptor receptor Cell Cell membrane membrane Cell response Cell response
  20. 20. INTRODUCTION – PARKINSON’S DISEASE, TREATMENT• Unfortunately, these medicines have a large number of side effects: – Appearance of involuntary movements and tics – Depression – Hallucinations• These medicines also cease to be effective with time.• We need to produce new medicines with less side effects that are active for longer periods.
  21. 21. RESEARCH, SYNTHESIS OF DRUGS FOR THE TREATMENT OF PARKINSON’S DISEASE• In the Barcelona Science Park, on the Combinatory Chemistry Platform, scientists are working on the synthesis of new compounds that can be used as therapeutic agents in the treatment of neurodegenerative diseases such as Parkinson’s or Schizophrenia that are: – More active – Less toxic
  22. 22. RESEARCH, SYNTHESIS OF DRUGS FOR THE TREATMENTOF PARKINSON’S DISEASE • A drug cocktail is currently administered to increase the efficacy of these anti-Parkinson’s agents. • The objective is to synthesise new molecules that are more effective or have less side effects. D AAnti-Parkinson’s agents Drug cocktail A single drug
  23. 23. RESEARCH, SYNTHESIS OF DRUGS FOR THE TREATMENTOF PARKINSON’S DISEASE New drug Cell response
  24. 24. RESEARCH, DESIGN AND SYNTHESIS OF NEW MOLECULES D A OH O A D N O N N O OHO N NH XAC-COOH ( )-PPHT NH2
  25. 25. HOW DO WE SYNTHESISE THESE NEW MOLECULES IN THELAB? O CN O H H N N N N NaOH 70% O Ac2O O pH 10-11 N 2 h, 80 ºC NH NH2 O + 96% 96% HOOC CN NaNO2 AcOH O N O Na2S2O4 N O NH2 O NO N EtOAc/H2O NH2 N NH2 76% 75% K2CO3 OHC OH + I OHC O COOH COOH reflujo en EtOH DMF, 60ºC 3 dias 62% O O N COOH DIAD N N O N O N O N N NH2 H O 75% 80% COOH
  26. 26. HOW DO WE SYNTHESISE THESE NEW MOLECULESIN THE LAB? O CN O H H N N N N NaOH 70% O Ac2O O pH 10-11 N 2 h, 80 ºC NH NH2 O + 96% 96% HOOC CN NaNO2 AcOH O N O Na2S2O4 N O NH2 O NO N EtOAc/H2O NH2 N NH2 76% 75% K2CO3 OHC OH + I OHC O COOH COOH reflujo en EtOH reflux in EtOH DMF, 60ºC 3 days dias 62% O O N COOH DIAD N N O N O N O N N NH2 H O 75% 80% COOH 27
  27. 27. HOW DO WE SYNTHESISE THESE NEW MOLECULESIN THE LAB? O CN O H H N N NaOH 70% 1. Chemical reaction N N Ac2O 2 h, 80 ºC O NH pH 10-11 O N NH2 O + 96% 96% HOOC CN NaNO2 AcOH O N O Na2S2O4 N O NH2 O NO N EtOAc/H2O NH2 N NH2 76% 75% K2CO3 OHC OH + I OHC O COOH COOH reflujo en EtOH DMF, 60ºC 3 dias 62% O O N COOH DIAD N N O N O N O N N NH2 H O 75% 80% COOH 28
  28. 28. HOW DO WE SYNTHESISE THESE NEW MOLECULES IN THE LAB?2. Isolation and purification of the product3. Characterisation of the product
  29. 29. WHAT ARE WEGOING TO DO TODAY?
  30. 30. HOW DO WE SYNTHESISE THESE NEW MOLECULES INTHE LAB? O CN O H H N N N N NaOH 70% O Ac2O O pH 10-11 N 2 h, 80 ºC NH NH2 O + 96% 96% HOOC CN NaNO2 Chemical reaction AcOH O N O Na2S2O4 N O NH2 O NO N EtOAc/H2O NH2 N NH2 76% 75% K2CO3 OHC OH + I OHC O COOH COOH reflujo en EtOH reflux in EtOH DMF, 60ºC 3 dias days 62% O O N COOH DIAD N N O N O N O N N NH2 H O 75% 80% COOH
  31. 31. WHAT ARE WE GOING TO DO TODAY? Chemical reaction Isolation of product by filtration  ?  Characterisation of product by chromatography
  32. 32. Let’s research!

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