Prodrugs: Challenges and Rewards(Biotechnology: Pharmaceutical Aspects)

Front Matter....Pages i-xvii
Front Matter....Pages 1-1
A Case for Prodrugs....Pages 3-33
Front Matter....Pages 35-35
Controlled Release — Small Molecules....Pages 357-377
Controlled Release - Macromolecular Prodrugs....Pages 379-416
Controlled Release - Proenzymes....Pages 417-428
Targeting - Theoretical and Computational Models....Pages 429-445
Targeting - Cancer — Small Molecules....Pages 447-506
Monoclonal Antibody Drug Conjugates for Cancer Therapy....Pages 507-524
Antibody-Directed Enzyme Prodrug Therapy....Pages 525-540
Prodrugs for Liver-targeted Drug Delivery....Pages 541-572
Prodrug Approaches for Drug Delivery to the Brain....Pages 573-651
Lymphatic Absorption of Orally Administered Prodrugs....Pages 653-682
Colonic Delivery....Pages 683-699
Prodrug Approaches to Enhancing the Oral Delivery of Poorly Permeable Drugs....Pages 37-82
Topical Delivery Using Prodrugs....Pages 83-123
Prodrug approaches to ophthalmic drug delivery....Pages 125-155
Overcoming Poor Aqueous Solubility of Drugs for Oral Delivery....Pages 157-215
Prodrugs and Parenteral Drug Delivery....Pages 217-281
Poly (ethylene glycol) Prodrugs: Altered Pharmacokinetics and Pharmacodynamics....Pages 283-338
Prodrugs to Reduce Presystemic Metabolism....Pages 339-355
Front Matter....Pages 701-701
Prodrugs of Carboxylic Acids....Pages 703-729
Front Matter....Pages 701-701
Prodrugs of Alcohols and Phenols....Pages 731-799
Prodrugs of Amines....Pages 801-831
Prodrugs of Amides, Imides and Other NH-acidic Compounds....Pages 833-887
Prodrugs of Benzamidines....Pages 889-922
Prodrugs of Phosphonates, Phosphinates, and Phosphates....Pages 923-964
Functional Group Approaches to Prodrugs: Functional Groups in Peptides....Pages 965-988
Macromolecular Prodrugs of Small Molecules....Pages 989-1021
Miscellaneous Functional Groups....Pages 1023-1039
Front Matter....Pages 1041-1041
Prodrugs: Absorption, Distribution, Metabolism, Excretion (ADME) Issues....Pages 1043-1081
Formulation Challenges of Prodrugs....Pages 1083-1110
Safety Assessment of Prodrugs....Pages 1111-1124
Toxicological Issues with Pivalate Prodrugs....Pages 1125-1148
Front Matter....Pages 1149-1149
Case Study: Adefovir Dipivoxil: An Oral Prodrug of Adefovir....Pages 1151-1161
Case Study: Amifostine: (Ethyol®)....Pages 1163-1171
Case Study: Capecitabine: A Prodrug of 5-Fluorouracil....Pages 1173-1183
Case Study: Cefditoren Pivoxil: An Oral Prodrug of Cefditoren....Pages 1185-1194
Case Study: Cefuroxime Axetil: An Oral Prodrug of Cefuroxime....Pages 1195-1205
Case Study: Clindamycin 2-Phosphate, A Prodrug of Clindamycin....Pages 1207-1219
Case Study: Enalapril: A Prodrug of Enalaprilat....Pages 1221-1229
Case Study: Famciclovir: A Prodrug of Penciclovir....Pages 1231-1239
Front Matter....Pages 1149-1149
Case Study: Fosamprenavir: A Prodrug of Amprenavir....Pages 1241-1249
Case Study: Fosinopril....Pages 1251-1258
Case Study: Fosphenytoin: A Prodrug of Phenytoin....Pages 1259-1267
Case Study: Irinotecan (CPT-11), A Water-soluble Prodrug of SN-38....Pages 1269-1279
Case Study: Latanoprost: Isopropylester of a Prostaglandin F2α Analog....Pages 1281-1288
Case Study: Moexipril Hydrochloride: A Prodrug of Moexiprilat....Pages 1289-1297
Case Study: Mycophenolate Mofetil....Pages 1299-1304
Case Study: Olmesartan Medoxomil: A Prodrug of Olmesartan....Pages 1305-1312
Case Study: Omeprazole (Prilosec ® )....Pages 1313-1321
Case Study: Oseltamivir: An Orally Bioavailable Ester Prodrug of Oseltamivir Carboxylate....Pages 1323-1334
Case Study: Parecoxib: A Prodrug of Valdecoxib....Pages 1335-1346
Case Study: Tenofovir Disoproxil Fumarate: An Oral Prodrug of Tenofovir....Pages 1347-1357
Case Study: Travoprost: A Potent PGF2α Analog....Pages 1359-1368
Case Study: Valacyclovir: A Prodrug of Acyclovir....Pages 1369-1376
Case Study: Valganciclovir: A Prodrug of Ganciclovir....Pages 1377-1386
Case Study: Vantin: A Prodrug of Cefpodoxime....Pages 1387-1394
Case Study: Ximelagatran: A Double Prodrug of Melagatran....Pages 1395-1402
Back Matter....Pages 1403-1465