| 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 |
