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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.

Pharmacology. --- Prodrugs. --- Drug effects --- Medical pharmacology --- Medical sciences --- Chemicals --- Chemotherapy --- Drugs --- Pharmacy --- Physiological effect --- Antibody-directed enzyme prodrug therapy

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Biotransformation --- Prodrugs --- Drug Carriers --- Pharmaceutical Preparations --- Drug carriers (Pharmacy) --- metabolism --- Biopharmaceutics. --- #Lilly --- Drugs --- Antibody-directed enzyme prodrug therapy --- Carriers, Drug (Pharmacy) --- Drug carrier systems (Pharmacy) --- Drug vehicles (Pharmacy) --- Vehicles, Drug (Pharmacy) --- Drug delivery systems --- Chemistry, Pharmaceutical --- Carriers --- Vehicles --- Prodrugs. --- Drug carriers (Pharmacy). --- Biopharmaceutics --- Pharmaceutics --- Pharmaceutic

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Albumin is playing an increasing role as a versatile, biodegradable drug carrier in clinical theranostics. By applying different techniques, smart drug-delivery systems can be developed from albumin in order to improve drug delivery of different active pharmaceutical ingredients, even small-molecule drugs, peptides or enzymes. Principally, three drug delivery technologies can be distinguished for binding small-molecule or peptide drugs through the charged amino acids, carboxyl, and amino groups of albumin: physical or covalent binding of the drug to albumin through a ligand- or protein-binding group, the fusion of drug with albumin or the encapsulation of drugs into albumin nanoparticles. The accumulation of albumin in inflamed tissues and solid tumours forms the rationale for developing albumin-based drug delivery systems for targeted drug delivery. Besides tumour therapy, albumin-based drug delivery systems can be successfully applied as anti-inflammatory and anti-thrombotic coating for medical devices. The development and optimization of albumin nanoparticles may also be a rational and promising tool for conventional or alternative administration routes in order to improve therapy. This collection provides an overview of the significant scientific research works in this field, which may inspire researchers towards further development and utilization of these smart drug delivery systems.

Medicine. --- plasma half-life extension --- albumin conjugation --- in vivo glucose-lowering activity --- glucagon-like peptide-1 --- quality by design --- rapid equilibrium dialysis --- muco-adhesion --- brain PAMPA --- RPMI 2650 nasal epithelial cell --- human serum albumin --- dimerization --- doxorubicin --- enhanced permeability and retention effect --- antitumor --- Arthrobacter globiformis --- gout --- half-life extension --- inverse electron demand Diels-Alder reaction --- site-specific albumin conjugation --- thermostability --- urate oxidase --- albumin --- anti-thrombotic --- CD39 --- coating of medical devices --- stent coating --- therapeutic fusion protein --- conjugates --- vanadium --- cancer --- prodrug --- hydrogels --- EPR/ESR spectroscopy --- release behavior --- disulfide --- glioma --- conjugate --- albumin binding moieties --- peptides --- Evans blue --- 4-(p-iodophenyl)butyric acid --- integrin αvβ6 --- integrin αvβ6 binding peptide --- improved pharmacokinetics --- PET imaging

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Patient outcomes remain poor for many cancers despite improvements in treatments and new molecular-targeted biomedicines for certain cancer types or subtypes. Dose-limiting toxicity, a narrow therapeutic index, and the development of resistance to traditional anti-cancer agents are well-established. It is apparent that inherent and acquired drug resistance are major challenges with molecular-targeted agents and that on- as well as off-target side effects can still occur. Other issues include drug metabolism by the body and safely supplying a sufficient amount of active drug to the tumor cells. There is a clear and urgent need for new molecular targets and drugs that specifically target cancer cells in different ways to existing approved drugs. This book, through a collection of eight research articles and two review articles from the Biomedicines themed Special Issue ‘Novel Anti-Cancer Agents and Cellular Targets and Their Mechanism(s) of Action’, provides a snapshot of some of the diverse and exciting research approaches being taken by the cancer research community in trying to address some of these therapeutic challenges.

Technology: general issues --- History of engineering & technology --- microtubule acetylation --- triple-negative breast cancer --- anti-cancer agent --- apoptosis --- K562 --- 8-hydroxydaidzein --- autophagy --- BCR-ABL --- MAPK --- NF-κB --- c-myc --- RNA interference --- siRNA --- oncogene --- gene silencing --- expression --- nanosystems --- Cytochrome P450 --- CYP1A1 --- CYP1B1 --- CYP2W1 --- breast cancer --- prodrug --- bioprecursor --- duocarmycin --- phortress --- AQ4N --- 5-FU resistance --- colorectal cancer --- drug repurposing --- Genomics of Drug Sensitivity in Cancer --- Connectivity Map --- anticancer drug --- B-lactam steroid alkylators --- synthetic lethality --- poly (ADP-ribose) polymerase inhibitors --- ovarian cancer --- hybrid steroidal alkylating agents --- migration --- invasion --- glioblastoma --- CCN1 --- mesenchymal–amoeboid transition --- biomarker --- HepG2 --- Huh7 --- isatin sulfonamides --- angiogenesis --- cancer hallmarks --- molecular docking --- EGFR tyrosine kinase inhibitor --- photon upconversion --- triplet-triplet annihilation --- in vivo imaging --- PLGA --- nanoparticles --- affibody molecule --- human epidermal growth factor receptor 3 (HER3) --- BxPC-3 --- emtansine --- DM1 --- albumin binding domain --- affibody drug conjugate (AffiDC) --- n/a --- mesenchymal-amoeboid transition

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This book focuses on how nanoscale systems can be used to deliver molecules to help with cancer management. It provides a broad overview of some of the key strategies for nanocarrier design. These strategies are brought together by the wide compositional variety of these systems and the diversity of molecules that may be carried. Additionally, functionalization strategies, codelivery, and combination with other treatment modalities highlight a very active research field.

Medicine --- Pharmacology --- nanostructured lipid carriers --- doxorubicin --- mucositis --- cell internalization --- albumin --- BSA --- CPP --- gold nanorods --- gold nanoprisms --- arginine-rich peptide --- glutathione --- nanoparticles --- oxidative stress --- breast cancer --- gastric cancer --- nanoparticle --- fucoidan --- d-alpha-tocopherylpoly (ethylene glycol) succinate --- combination chemotherapy --- G-quadruplex --- nucleolin --- DNA nanocages --- intracellular localization --- cancer targeting --- molecular dynamics simulations --- mesoporous silica nanoparticles --- radiotherapy --- immunotherapy --- tumor microenvironment --- abscopal effect --- magnetofection in vivo --- magnetic nanoparticles --- iron oxide --- gene delivery --- gene vectors --- codelivery nanocarriers --- photodynamic therapy --- anticancer therapies --- combination therapy --- phthalocyanine --- uterine cervical neoplasms --- photochemotherapy --- in vitro --- in vivo --- nanocarrier --- polyplexes --- siRNA delivery --- glioblastoma therapy --- amphiphilic poly(α)glutamate --- P-selectin --- prodrug --- drug delivery --- targeted therapy --- chemotherapy --- prostate cancer --- prostate-specific membrane antigen --- targeted delivery --- encapsulation --- cabazitaxel --- nanocarriers --- nanosystems --- radiosensitizer --- hypoxia --- synergism --- cancer --- photothermal therapy --- combined antitumor effect --- oxygenation --- hydrogel --- hypoxic tumor --- n/a