Prodrugs (eBook)
XVIII, 1464 Seiten
Springer New York (Verlag)
978-0-387-49785-3 (ISBN)
These volumes represent a comprehensive guide to prodrugs. They guide the reader through the current status of the prodrug concept and its many applications and highlight its many successes in overcoming formulation and delivery of problematic drugs. Replete with examples of approved and marketed prodrugs, these volumes introduce the topic to the novice as well as professional in the design of prodrugs.
Prodrugs are substances administered in an inactive form that is then metabolized in the body in vivo into the active compound. The rationale behind administering prodrugs is to optimize absorption, distribution, metabolism, and excretion of these drugs. Since first described in the 1950s, prodrugs continue to be a fertile area of research. There are a number of small pharmaceutical/biotech companies dedicated to using prodrugs for the delivery of older but problematic drugs as well as to developing broad-based prodrug technologies for application to new and future drugs. These volumes represent a comprehensive guide to prodrugs and will guide the reader through the current status of the prodrug concept and its many applications and to highlight its many successes in overcoming formulation and delivery of problematic drugs.
Prodrugs Part 1 2
Preface 6
Contents 8
Part I 10
A Case for Prodrugs 11
Part II Problems Addressable by Prodrugs 42
Prodrug Approaches to Enhancing the Oral Delivery of Poorly Permeable Drugs 43
Topical Delivery Using Prodrugs 89
Prodrug approaches to ophthalmic drug delivery 130
Overcoming Poor Aqueous Solubility of Drugs for Oral Delivery 161
Prodrugs and Parenteral Drug Delivery 220
Poly (ethylene glycol) Prodrugs: Altered Pharmacokinetics and Pharmacodynamics 285
Prodrugs to Reduce Presystemic Metabolism 341
Controlled Release - Small Molecules 358
Controlled Release - Macromolecular Prodrugs 379
Controlled Release - Proenzymes 417
Targeting - Theoretical and Computational Models 429
Targeting - Cancer – Small Molecules 446
Monoclonal Antibody Drug Conjugates for Cancer Therapy 506
Antibody-Directed Enzyme Prodrug Therapy 524
Prodrugs for Liver-targeted Drug Delivery 540
Prodrug Approaches for Drug Delivery to the Brain 572
Lymphatic Absorption of Orally Administered Prodrugs 651
Colonic Delivery 681
Index 698
Prodrugs Part 2 732
Preface 736
Contents 738
Part III Functional Group Approach to Prodrugs 741
Prodrugs of Carboxylic Acids 742
Prodrugs of Alcohols and Phenols 769
Prodrugs of Amines 838
Prodrugs of Amides, Imides and Other NH-acidic Compounds 869
Prodrugs of Benzamidines 924
Prodrugs of Phosphonates, Phosphinates, and Phosphates 958
Functional Group Approaches to Prodrugs: Functional Groups in Peptides 1000
Macromolecular Prodrugs of Small Molecules 1024
Miscellaneous Functional Groups 1057
Part 4.1 Prodrugs – Preclinical and Clinical Considerations 1074
Prodrugs:Absorption, Distribution, Metabolism, Excretion (ADME) Issues 1075
Formulation Challenges of Prodrugs 1114
Safety Assessment of Prodrugs 1142
Toxicological Issues with Pivalate Prodrugs 1156
Part 5 Case Studies 1180
Case Study: Adefovir Dipivoxil: An Oral Prodrug of Adefovir 1181
Case Study: Amifostine: (Ethyol®) 1192
Case Study: Capecitabine: A Prodrug of 5-Fluorouracil 1201
Case Study: Cefditoren Pivoxil: An Oral Prodrug of Cefditoren 1212
Case Study: Cefuroxime Axetil: An Oral Prodrug of Cefuroxime 1222
Case Study: Clindamycin 2-Phosphate, A Prodrug of Clindamycin 1233
Case Study: Enalapril: A Prodrug of Enalaprilat 1246
Case Study: Famciclovir: A Prodrug of Penciclovir 1255
Case Study: Fosamprenavir: A Prodrug of Amprenavir 1264
Case Study: Fosinopril 1273
Case Study: Fosphenytoin: A Prodrug of Phenytoin 1281
Case Study: Irinotecan (CPT-11), A Water-soluble Prodrug of SN-38 1290
Case Study: Latanoprost: Isopropylester of a Prostaglandin F2 Analog 1301
Case Study: Moexipril Hydrochloride: A Prodrug of Moexiprilat 1309
Case Study: Mycophenolate Mofetil 1318
Case Study: Olmesartan Medoxomil: A Prodrug of Olmesartan 1324
Case Study: Omeprazole (Prilosec®) 1332
Case Study: Oseltamivir: An Orally Bioavailable Ester Prodrug of Oseltamivir Carboxylate 1341
Case Study: Parecoxib: A Prodrug of Valdecoxib 1353
Case Study: Tenofovir Disoproxil Fumarate: An Oral Prodrug of Tenofovir 1365
Case Study: Travoprost: A Potent PGF2 Analog 1376
Case Study: Valacyclovir: A Prodrug of Acyclovir 1386
Case Study: Valganciclovir: A Prodrug of Ganciclovir 1394
Case Study: Vantin: A Prodrug of Cefpodoxime 1404
Case Study: Ximelagatran: A Double Prodrug of Melagatran 1412
Index 1420
| Erscheint lt. Verlag | 26.8.2007 |
|---|---|
| Reihe/Serie | Biotechnology: Pharmaceutical Aspects | Biotechnology: Pharmaceutical Aspects |
| Zusatzinfo | XVIII, 1464 p. |
| Verlagsort | New York |
| Sprache | englisch |
| Themenwelt | Medizin / Pharmazie ► Medizinische Fachgebiete ► Pharmakologie / Pharmakotherapie |
| Medizin / Pharmazie ► Pharmazie | |
| Studium ► 1. Studienabschnitt (Vorklinik) ► Biochemie / Molekularbiologie | |
| Technik ► Umwelttechnik / Biotechnologie | |
| Wirtschaft | |
| Schlagworte | challenges • Dynamics • Metabolism • Prodrugs • Rewards • Stella |
| ISBN-10 | 0-387-49785-4 / 0387497854 |
| ISBN-13 | 978-0-387-49785-3 / 9780387497853 |
| Haben Sie eine Frage zum Produkt? |
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