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Dermal Drug Selection and Development
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An Industrial Perspective
eBook
Sofort lieferbar | Lieferzeit: Sofort lieferbar
Artikel-Nr:
9783319595047
Veröffentl:
2017
Einband:
eBook
Seiten:
148
Autor:
Lionel Trottet
eBook Typ:
PDF
eBook Format:
Reflowable eBook
Kopierschutz:
Digital Watermark [Social-DRM]
Sprache:
Englisch
Beschreibung:
The authors show how the pharmaceutical industry faces the development of dermal drugs and provide the only book of its kind that describes how the industry develops and selects dermal drugs, complete with the challenges and opportunities of the field. Delivery of drugs through the skin has been an attractive and challenging area for research, and advances in modern technologies have resulted in a larger number of drugs being delivered transdermally, including conventional hydrophobic small molecule drugs, hydrophilic drugs and macromolecules. Offering the perspective from the industrial side of selection and development of drugs, the primary audience is geared towards the pharmaceutical industry but can also offer valuable information to clinicians, compounding pharmacists, and similarly pharmacy students. Dermal Drug Selection and Development covers the scientific gaps that exist in terms of dermal pharmacokinetics and the resulting uncertainty by clinicians when choosing a drug candidate.
The authors show how the pharmaceutical industry faces the development of dermal drugs and provide the only book of its kind that describes how the industry develops and selects dermal drugs, complete with the challenges and opportunities of the field. Delivery of drugs through the skin has been an attractive and challenging area for research, and advances in modern technologies have resulted in a larger number of drugs being delivered transdermally, including conventional hydrophobic small molecule drugs, hydrophilic drugs and macromolecules. Offering the perspective from the industrial side of selection and development of drugs, the primary audience is geared towards the pharmaceutical industry but can also offer valuable information to clinicians, compounding pharmacists, and similarly pharmacy students. Dermal Drug Selection and Development covers the
scientific gaps that exist in terms of dermal pharmacokinetics and the resulting uncertainty by clinicians when choosing a drug candidate.CHAPTER 1. INTRODUCTION 7
1.1. Developing a new medicine
1.2. Key risks at the candidate selection stage
1.3. Attrition in the pharmaceutical industry
1.4. Evolution of the Pharma R&D over the last 2 decades
1.5. Pharma R&D productivity in decline
1.6. Cost of Pharma R&D and cost up to Candidate selection
1.7. Increased risks to develop a topical drug
1.8. Increased opportunities to develop a topical drug
CHAPTER 2. CHOOSING THE TOPICAL DRUG CANDIDATE : AN HISTORICAL OVERVIEW 19
TOPICAL DRUG DEVELOPMENT 312.1. The pragmatic topical drug development approach: An existing oral/systemic drug is further developed as a topical
2.2. Moving towards improved topical drug candidate selection processes: Use of in vivo models
2.3. Historical topical drug candidate selection summary
CHAPTER 3. KEY FACTORS AFFECTING THE EFFICACY OF A TOPICAL DRUG CANDIDATE: LEARNINGS FROM PAST
3.1. Skin barrier condition vs. “Easiness” of topical drug development
3.2. Drug potency and clinical efficacy
CHAPTER 4. TOPICAL VS ORAL/SYSTEMIC DRUG DISCOVERY 40
4.1. Drug Discovery Evolution
4.2. Oral/Systemic Drug Discovery
4.3. Topical Drug Discovery
4.4. The Two Key Differences in discharging risk in between the Oral/Systemic and Topical Drug Discovery Processes
4.5. Consequences for the Preclinical Stage: “Maximising the Percutaneous Flux”
4.6. What can be learned from the Oral Drug Development Process?
CHAPTER 5. ASSESSING DRUG CONCENTRATION IN SKIN: DIRECT AND INDIRECT METHODS 52
5.1. Direct Methods
5.2. Indirect Methods
5.3. Potential Use of the various skin PharmacoKinetic Sampling Methods, Comparisons of the Methods and Consequences
5.4. Using the Percutaneous Flux or the Plasma concentrati
on as surrogate measurement of skin concentrationCHAPTER 6. ASSESSING TOPICAL EFFICACY 72
6.1. Assessing efficacy and dose prediction for a systemic target
6.2. In vivo PD Models:
6.3. Conclusion
CHAPTER 7. ASSESSING THE THERAPEUTIC INDEX 86
7.1. Introduction
7.2. A “crude” Approach: Comparing the mass of target tissue with total body mass
7.3. Calculated Approach
7.4. Comparative Approach
CHAPTER 8. TOPICAL VEHICLE SELECTION: MYTHS AND REALITY 93
8.1. Introduction :
or a non systemic indication on a new target class8.2. Skin Penetration Enhancement
8.3. Retention in Skin
8.4. For each compound, a specific formulation: A must ?
8.5. Vehicle Aesthetics
8.6. Drug formulated as a dispersion or as a solution?
8.7. Conclusion
CHAPTER 9. TOPICAL DRUG DEVELOPMENT STRATEGIES 107
9.1. Option#1: Clinical molecule repurposing - Developed drug f
9.2. Option#2: Full lead optimization - New drug from a new mechanism of action for a topical application
9.3. Option#3: “Me better” - Improved drug for a known topical target class
9.4. Option#4: Chemical Series Repurposing - Advanced lead optimized chemicals series screened against for a topical indication
CHAPTER 10. TOPICAL DRUG CANDIDATE SELECTION CRITERIA AND CASCADE 111
10.1. General principles: Discharging risk
10.2. Medicinal chemistry and chemical space
10.3. Potency
10.4. Percutaneous Flux
10.5. Pharmacological Kinetics Response
10.6. Preclinical Proof of Concept
10.7. Solution Stability – Water Stability
10.8. UV Absorption
10.9. Local Irritation
10.10. Systemic Effect (Clearance & Protein Binding)
10.11. Other criterias not important for a topical candidate
10.12. Comparison of the criterias used to select an oral/systemic candidate and a topical one
10.13. Example of candidate selection cascade when repurposing a whole chemical series
CHAPTER 11. SELECTING A DERMAL DRUG CANDIDATE: SOME USEFUL QUOTATIONS AND RULES 127
CHAPTER 12. CONCLUSIONS AND PERSPECTIVES 131