SlideShare a Scribd company logo
1 of 42
DR ANTHONY M CRASTO (Ph.D) PRINCIPAL SCIENTIST PROCESS RESEARCH DEC 2011 “ A SHORT PRESENTATION”
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Net Cost: $802 Million  Invested Over 15 Years  5,000–10,000 Screened 250 Enter Preclinical Testing 5 Enter Clinical Testing 1 Compound Success  Rates by Stage 16 14 12 10 8 6 4 2 0 Phase II 100–300 Patient Volunteers Used to Look for Efficacy  and Side Effects Phase III 1,000–5,000 Patient Volunteers Used to Monitor Adverse Reactions to Long-Term Use FDA Review Approval Additional Post-Marketing Testing Phase I  20–80 Healthy Volunteers Used to Determine Safety and Dosage Preclinical Testing Laboratory and Animal Testing Discovery (2–10 Years) Years New Product Development –  A Risky and Expensive Proposition Approved by the FDA
[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object]
Med Chem Clinical  Chem E R&D Pharm  R&D Safety Analytical Process
responsible for developing In-process assay and critical evaluation of  drug substance and intermediates Med Chem Clinical  Chem E R&D Pharm  R&D Safety Analytical Process
responsible for toxicity studies:  (carcinogen, teratogen, gene toxicity ) Med Chem Clinical  Chem E R&D Pharm  R&D Safety Analytical Process
responsible for formulating drug substance (API) into drug product Med Chem Clinical  Chem E R&D Pharm  R&D Safety Analytical Process
Oversee process transfer into Pilot plants Med Chem Clinical  Chem E R&D Pharm  R&D Safety Analytical Process
Conducts clinical trials  (Ph I-III) and evaluates data Med Chem Clinical  Chem E R&D Pharm  R&D Safety Analytical Process
Discovers new chemical  entities (NCE’s) and  prepares intitial quantities Med Chem Clinical  Chem E R&D Pharm  R&D Safety Analytical Process
[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object]
Selective Dopamine-2 Antagonist Indication: Anti-psychotic (Depression/Schizophrenia) Clinical Trials: halted in 1993 due to anemia side-effects
 
 
Auerbach, Weissman  Tet Letters   1993,  931
 
Drawbacks: 1. Use of costly Oxalyl Chloride 2. CO and CO 2  by-products 3. Lengthy time cycle due to exothermic amination reaction 4. Need for 3 equiv of volatile  t -butylamine 5. Filtration/Disposal of voluminous amine hydrochloride salt
 
A: 179/[124+127+73+73]  = 45 % B: 179/[105 + 98 +74 +18] = 61%
 
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object]
[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object]

More Related Content

What's hot

Process Research and Development Chemistry 15 03 31
Process Research and Development Chemistry 15 03 31Process Research and Development Chemistry 15 03 31
Process Research and Development Chemistry 15 03 31
Paul Fishbein
 

What's hot (20)

CHEMISTRY OF PEPTIDES [M.PHARM, M.SC, BSC, B.PHARM]
CHEMISTRY OF PEPTIDES [M.PHARM, M.SC, BSC, B.PHARM]CHEMISTRY OF PEPTIDES [M.PHARM, M.SC, BSC, B.PHARM]
CHEMISTRY OF PEPTIDES [M.PHARM, M.SC, BSC, B.PHARM]
 
Fermentation
FermentationFermentation
Fermentation
 
UNIT OPERATIONS (unit 2) pharmaceutical process chemistry
UNIT OPERATIONS (unit 2) pharmaceutical process chemistryUNIT OPERATIONS (unit 2) pharmaceutical process chemistry
UNIT OPERATIONS (unit 2) pharmaceutical process chemistry
 
statin of fermentation.pptx
statin of fermentation.pptxstatin of fermentation.pptx
statin of fermentation.pptx
 
UNIT OPERATIONS (unit 2) process chemistry
UNIT OPERATIONS (unit 2) process chemistryUNIT OPERATIONS (unit 2) process chemistry
UNIT OPERATIONS (unit 2) process chemistry
 
Route selection
Route selectionRoute selection
Route selection
 
Nitration (2)
Nitration (2)Nitration (2)
Nitration (2)
 
Chemistry of peptide (BPHARM,MPHARM,MSC,BSC)
Chemistry of peptide (BPHARM,MPHARM,MSC,BSC)Chemistry of peptide (BPHARM,MPHARM,MSC,BSC)
Chemistry of peptide (BPHARM,MPHARM,MSC,BSC)
 
Nitration as per M.pharm syllabus of PCI
Nitration as per M.pharm syllabus of PCINitration as per M.pharm syllabus of PCI
Nitration as per M.pharm syllabus of PCI
 
Spps and side reactions in peptide synthesis
Spps and side reactions in peptide synthesisSpps and side reactions in peptide synthesis
Spps and side reactions in peptide synthesis
 
IMPURITIES IN API’s INCLUDING GENOTOXIC IMPURITIES.pptx
IMPURITIES IN API’s INCLUDING GENOTOXIC IMPURITIES.pptxIMPURITIES IN API’s INCLUDING GENOTOXIC IMPURITIES.pptx
IMPURITIES IN API’s INCLUDING GENOTOXIC IMPURITIES.pptx
 
Homogeneous catalysis 2021
Homogeneous catalysis 2021Homogeneous catalysis 2021
Homogeneous catalysis 2021
 
Process Research and Development Chemistry 15 03 31
Process Research and Development Chemistry 15 03 31Process Research and Development Chemistry 15 03 31
Process Research and Development Chemistry 15 03 31
 
Continuous flow reaction/ Chemistry
Continuous flow reaction/ ChemistryContinuous flow reaction/ Chemistry
Continuous flow reaction/ Chemistry
 
Mass spectroscopy (advanced spectral analysis)
Mass spectroscopy (advanced spectral analysis)Mass spectroscopy (advanced spectral analysis)
Mass spectroscopy (advanced spectral analysis)
 
Flow chemistry
Flow chemistryFlow chemistry
Flow chemistry
 
Asymmetric synthesis FOR BSc, MSc, Bpharm, M,pharm
Asymmetric synthesis FOR BSc, MSc, Bpharm, M,pharmAsymmetric synthesis FOR BSc, MSc, Bpharm, M,pharm
Asymmetric synthesis FOR BSc, MSc, Bpharm, M,pharm
 
Effluents and its management
Effluents and its management Effluents and its management
Effluents and its management
 
Extraction
ExtractionExtraction
Extraction
 
INTRODUCTION TO PROCESS CHEMISTRY.pptx
INTRODUCTION TO PROCESS CHEMISTRY.pptxINTRODUCTION TO PROCESS CHEMISTRY.pptx
INTRODUCTION TO PROCESS CHEMISTRY.pptx
 

Viewers also liked

Drug development and clinical trial phases
Drug development and clinical trial phasesDrug development and clinical trial phases
Drug development and clinical trial phases
Sunil Boreddy Rx
 

Viewers also liked (16)

Powerpoint presentation parvez1
Powerpoint presentation parvez1Powerpoint presentation parvez1
Powerpoint presentation parvez1
 
Anthony crasto glenmark scientist, helping millions with websites
Anthony crasto glenmark scientist, helping millions with websitesAnthony crasto glenmark scientist, helping millions with websites
Anthony crasto glenmark scientist, helping millions with websites
 
IDC Launch in India
IDC Launch in IndiaIDC Launch in India
IDC Launch in India
 
Drug discovery and development
Drug discovery and developmentDrug discovery and development
Drug discovery and development
 
IPR NDA and ANDA
IPR NDA and ANDAIPR NDA and ANDA
IPR NDA and ANDA
 
What is IP, Patents in Pharma Industry
What is IP, Patents in Pharma IndustryWhat is IP, Patents in Pharma Industry
What is IP, Patents in Pharma Industry
 
Fragment Based Drug Discovery
Fragment Based Drug DiscoveryFragment Based Drug Discovery
Fragment Based Drug Discovery
 
Anda
AndaAnda
Anda
 
2D NMR ORGANIC SPECTROSCOPY by DR ANTHONY CRASTO
2D NMR ORGANIC SPECTROSCOPY by DR ANTHONY CRASTO2D NMR ORGANIC SPECTROSCOPY by DR ANTHONY CRASTO
2D NMR ORGANIC SPECTROSCOPY by DR ANTHONY CRASTO
 
Drug discovery hit to lead
Drug discovery hit to leadDrug discovery hit to lead
Drug discovery hit to lead
 
DMF by Anthony Crasto
DMF by Anthony CrastoDMF by Anthony Crasto
DMF by Anthony Crasto
 
STRUCTURE BASED DRUG DESIGN - MOLECULAR MODELLING AND DRUG DISCOVERY
STRUCTURE BASED DRUG DESIGN - MOLECULAR MODELLING AND DRUG DISCOVERYSTRUCTURE BASED DRUG DESIGN - MOLECULAR MODELLING AND DRUG DISCOVERY
STRUCTURE BASED DRUG DESIGN - MOLECULAR MODELLING AND DRUG DISCOVERY
 
Drug discovery anthony crasto
Drug discovery  anthony crastoDrug discovery  anthony crasto
Drug discovery anthony crasto
 
C-C Cross Coupling Reactions in Organic chemistry by Anthony crasto
C-C Cross Coupling Reactions in Organic chemistry by Anthony crastoC-C Cross Coupling Reactions in Organic chemistry by Anthony crasto
C-C Cross Coupling Reactions in Organic chemistry by Anthony crasto
 
Drug development and clinical trial phases
Drug development and clinical trial phasesDrug development and clinical trial phases
Drug development and clinical trial phases
 
Drug discovery and development
Drug discovery and developmentDrug discovery and development
Drug discovery and development
 

Similar to Process research overview

Parveen Bhatarah CV Appendix
Parveen Bhatarah CV AppendixParveen Bhatarah CV Appendix
Parveen Bhatarah CV Appendix
Parveen Bhatarah
 
Pilot plant scaleuptechnique
Pilot plant scaleuptechniquePilot plant scaleuptechnique
Pilot plant scaleuptechnique
jiten patel
 
Pilot scaleuptechnique
Pilot scaleuptechniquePilot scaleuptechnique
Pilot scaleuptechnique
jiten patel
 
Pilot scaleuptechnique
Pilot scaleuptechniquePilot scaleuptechnique
Pilot scaleuptechnique
jiten patel
 

Similar to Process research overview (20)

Green Chemistry Principles
Green Chemistry  PrinciplesGreen Chemistry  Principles
Green Chemistry Principles
 
Parveen Bhatarah CV Appendix
Parveen Bhatarah CV AppendixParveen Bhatarah CV Appendix
Parveen Bhatarah CV Appendix
 
AlokCV
AlokCVAlokCV
AlokCV
 
Pharmaceutical Process Chemistry Presentation.pdf
Pharmaceutical Process Chemistry Presentation.pdfPharmaceutical Process Chemistry Presentation.pdf
Pharmaceutical Process Chemistry Presentation.pdf
 
Process chemistry AS PER PCI SYLLABUS FOR M.PHARM
Process chemistry AS PER PCI SYLLABUS FOR M.PHARMProcess chemistry AS PER PCI SYLLABUS FOR M.PHARM
Process chemistry AS PER PCI SYLLABUS FOR M.PHARM
 
Pilot plant scaleup
Pilot plant scaleupPilot plant scaleup
Pilot plant scaleup
 
Basic approach to Chemical Industries.pdf
Basic approach  to Chemical Industries.pdfBasic approach  to Chemical Industries.pdf
Basic approach to Chemical Industries.pdf
 
Considerations to Extractables and Leachables Testing
Considerations to Extractables and Leachables Testing Considerations to Extractables and Leachables Testing
Considerations to Extractables and Leachables Testing
 
SMi Group's Pharmaceutical Microbiology USA 2017 conference
SMi Group's Pharmaceutical Microbiology USA 2017 conferenceSMi Group's Pharmaceutical Microbiology USA 2017 conference
SMi Group's Pharmaceutical Microbiology USA 2017 conference
 
Pilot plant scaleuptechnique
Pilot plant scaleuptechniquePilot plant scaleuptechnique
Pilot plant scaleuptechnique
 
Pilot scaleuptechnique
Pilot scaleuptechniquePilot scaleuptechnique
Pilot scaleuptechnique
 
Pilot scaleuptechnique
Pilot scaleuptechniquePilot scaleuptechnique
Pilot scaleuptechnique
 
3980 s1 10_gardner
3980 s1 10_gardner3980 s1 10_gardner
3980 s1 10_gardner
 
Detailed Professional Resume for Chris Harding: Chemical Engineer/Biological ...
Detailed Professional Resume for Chris Harding: Chemical Engineer/Biological ...Detailed Professional Resume for Chris Harding: Chemical Engineer/Biological ...
Detailed Professional Resume for Chris Harding: Chemical Engineer/Biological ...
 
USP <665> draft standard : A rational risk-based approach to characterization...
USP <665> draft standard : A rational risk-based approach to characterization...USP <665> draft standard : A rational risk-based approach to characterization...
USP <665> draft standard : A rational risk-based approach to characterization...
 
USP <665> draft standard : A rational risk-based approach to characterization...
USP <665> draft standard : A rational risk-based approach to characterization...USP <665> draft standard : A rational risk-based approach to characterization...
USP <665> draft standard : A rational risk-based approach to characterization...
 
cGMP
cGMPcGMP
cGMP
 
Pilot Plant Scale up Technique Ppt.pdf
Pilot Plant Scale up Technique Ppt.pdfPilot Plant Scale up Technique Ppt.pdf
Pilot Plant Scale up Technique Ppt.pdf
 
Process development
Process developmentProcess development
Process development
 
Green Chemistry
Green ChemistryGreen Chemistry
Green Chemistry
 

More from Anthony Melvin Crasto Ph.D

More from Anthony Melvin Crasto Ph.D (20)

What are Supergenerics
What are SupergenericsWhat are Supergenerics
What are Supergenerics
 
Accelerating Generic Approvals by Dr Anthony Crasto
Accelerating Generic Approvals by Dr Anthony CrastoAccelerating Generic Approvals by Dr Anthony Crasto
Accelerating Generic Approvals by Dr Anthony Crasto
 
13 C NMR Spectroscopy with examples by Dr Anthony Crasto
13 C NMR Spectroscopy with examples by Dr Anthony Crasto13 C NMR Spectroscopy with examples by Dr Anthony Crasto
13 C NMR Spectroscopy with examples by Dr Anthony Crasto
 
13 C NMR Spectroscopy by Dr Anthony Melvin Crasto
13 C NMR Spectroscopy by Dr Anthony Melvin Crasto13 C NMR Spectroscopy by Dr Anthony Melvin Crasto
13 C NMR Spectroscopy by Dr Anthony Melvin Crasto
 
DR ANTHONY MELVIN CRASTO
DR ANTHONY MELVIN CRASTODR ANTHONY MELVIN CRASTO
DR ANTHONY MELVIN CRASTO
 
NDA ANDA IND by Anthony Crasto
NDA ANDA IND by Anthony CrastoNDA ANDA IND by Anthony Crasto
NDA ANDA IND by Anthony Crasto
 
ABBREVIATED NEW DRUG APPLICATION (ANDA) by Anthony crasto
ABBREVIATED NEW DRUG APPLICATION (ANDA) by Anthony crastoABBREVIATED NEW DRUG APPLICATION (ANDA) by Anthony crasto
ABBREVIATED NEW DRUG APPLICATION (ANDA) by Anthony crasto
 
Anti viral-drug synthesis by Dr Anthony Crasto
Anti viral-drug synthesis by Dr Anthony CrastoAnti viral-drug synthesis by Dr Anthony Crasto
Anti viral-drug synthesis by Dr Anthony Crasto
 
Qbd by Anthony Melvin Crasto for API
Qbd by Anthony Melvin Crasto for APIQbd by Anthony Melvin Crasto for API
Qbd by Anthony Melvin Crasto for API
 
FDA’s drug review process
FDA’s drug review processFDA’s drug review process
FDA’s drug review process
 
The magic of cubane
The magic of cubaneThe magic of cubane
The magic of cubane
 
Nanoputians
NanoputiansNanoputians
Nanoputians
 
How to handle drug polymorphs... case study of trelagliptin succinate
How to handle drug polymorphs... case study of trelagliptin succinateHow to handle drug polymorphs... case study of trelagliptin succinate
How to handle drug polymorphs... case study of trelagliptin succinate
 
Benazepril Synthesis by Dr Anthony Crasto
Benazepril Synthesis  by Dr Anthony CrastoBenazepril Synthesis  by Dr Anthony Crasto
Benazepril Synthesis by Dr Anthony Crasto
 
Sildenafil by Anthony Crasto
Sildenafil by Anthony CrastoSildenafil by Anthony Crasto
Sildenafil by Anthony Crasto
 
Anthony crasto flavors and fragrances
Anthony crasto  flavors and fragrancesAnthony crasto  flavors and fragrances
Anthony crasto flavors and fragrances
 
Anthony crasto colchinine
Anthony crasto  colchinineAnthony crasto  colchinine
Anthony crasto colchinine
 
Anthony crasto bombykol
Anthony crasto  bombykolAnthony crasto  bombykol
Anthony crasto bombykol
 
Anthony crasto buckyball
Anthony crasto  buckyballAnthony crasto  buckyball
Anthony crasto buckyball
 
Anthony crasto brevetoxin synthesis
Anthony crasto brevetoxin synthesisAnthony crasto brevetoxin synthesis
Anthony crasto brevetoxin synthesis
 

Recently uploaded

The basics of sentences session 4pptx.pptx
The basics of sentences session 4pptx.pptxThe basics of sentences session 4pptx.pptx
The basics of sentences session 4pptx.pptx
heathfieldcps1
 
ppt your views.ppt your views of your college in your eyes
ppt your views.ppt your views of your college in your eyesppt your views.ppt your views of your college in your eyes
ppt your views.ppt your views of your college in your eyes
ashishpaul799
 
Neurulation and the formation of the neural tube
Neurulation and the formation of the neural tubeNeurulation and the formation of the neural tube
Neurulation and the formation of the neural tube
SaadHumayun7
 

Recently uploaded (20)

The basics of sentences session 4pptx.pptx
The basics of sentences session 4pptx.pptxThe basics of sentences session 4pptx.pptx
The basics of sentences session 4pptx.pptx
 
Application of Matrices in real life. Presentation on application of matrices
Application of Matrices in real life. Presentation on application of matricesApplication of Matrices in real life. Presentation on application of matrices
Application of Matrices in real life. Presentation on application of matrices
 
Telling Your Story_ Simple Steps to Build Your Nonprofit's Brand Webinar.pdf
Telling Your Story_ Simple Steps to Build Your Nonprofit's Brand Webinar.pdfTelling Your Story_ Simple Steps to Build Your Nonprofit's Brand Webinar.pdf
Telling Your Story_ Simple Steps to Build Your Nonprofit's Brand Webinar.pdf
 
Removal Strategy _ FEFO _ Working with Perishable Products in Odoo 17
Removal Strategy _ FEFO _ Working with Perishable Products in Odoo 17Removal Strategy _ FEFO _ Working with Perishable Products in Odoo 17
Removal Strategy _ FEFO _ Working with Perishable Products in Odoo 17
 
Pragya Champions Chalice 2024 Prelims & Finals Q/A set, General Quiz
Pragya Champions Chalice 2024 Prelims & Finals Q/A set, General QuizPragya Champions Chalice 2024 Prelims & Finals Q/A set, General Quiz
Pragya Champions Chalice 2024 Prelims & Finals Q/A set, General Quiz
 
INU_CAPSTONEDESIGN_비밀번호486_업로드용 발표자료.pdf
INU_CAPSTONEDESIGN_비밀번호486_업로드용 발표자료.pdfINU_CAPSTONEDESIGN_비밀번호486_업로드용 발표자료.pdf
INU_CAPSTONEDESIGN_비밀번호486_업로드용 발표자료.pdf
 
Exploring Gemini AI and Integration with MuleSoft | MuleSoft Mysore Meetup #45
Exploring Gemini AI and Integration with MuleSoft | MuleSoft Mysore Meetup #45Exploring Gemini AI and Integration with MuleSoft | MuleSoft Mysore Meetup #45
Exploring Gemini AI and Integration with MuleSoft | MuleSoft Mysore Meetup #45
 
Navigating the Misinformation Minefield: The Role of Higher Education in the ...
Navigating the Misinformation Minefield: The Role of Higher Education in the ...Navigating the Misinformation Minefield: The Role of Higher Education in the ...
Navigating the Misinformation Minefield: The Role of Higher Education in the ...
 
Essential Safety precautions during monsoon season
Essential Safety precautions during monsoon seasonEssential Safety precautions during monsoon season
Essential Safety precautions during monsoon season
 
ppt your views.ppt your views of your college in your eyes
ppt your views.ppt your views of your college in your eyesppt your views.ppt your views of your college in your eyes
ppt your views.ppt your views of your college in your eyes
 
factors influencing drug absorption-final-2.pptx
factors influencing drug absorption-final-2.pptxfactors influencing drug absorption-final-2.pptx
factors influencing drug absorption-final-2.pptx
 
How to the fix Attribute Error in odoo 17
How to the fix Attribute Error in odoo 17How to the fix Attribute Error in odoo 17
How to the fix Attribute Error in odoo 17
 
[GDSC YCCE] Build with AI Online Presentation
[GDSC YCCE] Build with AI Online Presentation[GDSC YCCE] Build with AI Online Presentation
[GDSC YCCE] Build with AI Online Presentation
 
Basic Civil Engineering notes on Transportation Engineering, Modes of Transpo...
Basic Civil Engineering notes on Transportation Engineering, Modes of Transpo...Basic Civil Engineering notes on Transportation Engineering, Modes of Transpo...
Basic Civil Engineering notes on Transportation Engineering, Modes of Transpo...
 
Neurulation and the formation of the neural tube
Neurulation and the formation of the neural tubeNeurulation and the formation of the neural tube
Neurulation and the formation of the neural tube
 
slides CapTechTalks Webinar May 2024 Alexander Perry.pptx
slides CapTechTalks Webinar May 2024 Alexander Perry.pptxslides CapTechTalks Webinar May 2024 Alexander Perry.pptx
slides CapTechTalks Webinar May 2024 Alexander Perry.pptx
 
philosophy and it's principles based on the life
philosophy and it's principles based on the lifephilosophy and it's principles based on the life
philosophy and it's principles based on the life
 
Morse OER Some Benefits and Challenges.pptx
Morse OER Some Benefits and Challenges.pptxMorse OER Some Benefits and Challenges.pptx
Morse OER Some Benefits and Challenges.pptx
 
UNIT – IV_PCI Complaints: Complaints and evaluation of complaints, Handling o...
UNIT – IV_PCI Complaints: Complaints and evaluation of complaints, Handling o...UNIT – IV_PCI Complaints: Complaints and evaluation of complaints, Handling o...
UNIT – IV_PCI Complaints: Complaints and evaluation of complaints, Handling o...
 
Open Educational Resources Primer PowerPoint
Open Educational Resources Primer PowerPointOpen Educational Resources Primer PowerPoint
Open Educational Resources Primer PowerPoint
 

Process research overview

  • 1. DR ANTHONY M CRASTO (Ph.D) PRINCIPAL SCIENTIST PROCESS RESEARCH DEC 2011 “ A SHORT PRESENTATION”
  • 2.
  • 3. Net Cost: $802 Million Invested Over 15 Years 5,000–10,000 Screened 250 Enter Preclinical Testing 5 Enter Clinical Testing 1 Compound Success Rates by Stage 16 14 12 10 8 6 4 2 0 Phase II 100–300 Patient Volunteers Used to Look for Efficacy and Side Effects Phase III 1,000–5,000 Patient Volunteers Used to Monitor Adverse Reactions to Long-Term Use FDA Review Approval Additional Post-Marketing Testing Phase I 20–80 Healthy Volunteers Used to Determine Safety and Dosage Preclinical Testing Laboratory and Animal Testing Discovery (2–10 Years) Years New Product Development – A Risky and Expensive Proposition Approved by the FDA
  • 4.
  • 5.
  • 6.
  • 7.
  • 8.
  • 9.
  • 10.
  • 11.
  • 12.
  • 13.
  • 14. Med Chem Clinical Chem E R&D Pharm R&D Safety Analytical Process
  • 15. responsible for developing In-process assay and critical evaluation of drug substance and intermediates Med Chem Clinical Chem E R&D Pharm R&D Safety Analytical Process
  • 16. responsible for toxicity studies: (carcinogen, teratogen, gene toxicity ) Med Chem Clinical Chem E R&D Pharm R&D Safety Analytical Process
  • 17. responsible for formulating drug substance (API) into drug product Med Chem Clinical Chem E R&D Pharm R&D Safety Analytical Process
  • 18. Oversee process transfer into Pilot plants Med Chem Clinical Chem E R&D Pharm R&D Safety Analytical Process
  • 19. Conducts clinical trials (Ph I-III) and evaluates data Med Chem Clinical Chem E R&D Pharm R&D Safety Analytical Process
  • 20. Discovers new chemical entities (NCE’s) and prepares intitial quantities Med Chem Clinical Chem E R&D Pharm R&D Safety Analytical Process
  • 21.
  • 22.
  • 23.
  • 24.
  • 25.
  • 26.
  • 27.
  • 28.
  • 29. Selective Dopamine-2 Antagonist Indication: Anti-psychotic (Depression/Schizophrenia) Clinical Trials: halted in 1993 due to anemia side-effects
  • 30.  
  • 31.  
  • 32. Auerbach, Weissman Tet Letters 1993, 931
  • 33.  
  • 34. Drawbacks: 1. Use of costly Oxalyl Chloride 2. CO and CO 2 by-products 3. Lengthy time cycle due to exothermic amination reaction 4. Need for 3 equiv of volatile t -butylamine 5. Filtration/Disposal of voluminous amine hydrochloride salt
  • 35.  
  • 36. A: 179/[124+127+73+73] = 45 % B: 179/[105 + 98 +74 +18] = 61%
  • 37.  
  • 38.
  • 39.
  • 40.
  • 41.
  • 42.

Editor's Notes

  1. Regulatory- talk of CMC (“chemistry and manufacturing controls”) section