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Handling cytotoxic drugs such as antibody–drug conjugates (ADCs) in a biopharmaceutical environment represents a challenge based on the potency of the compounds. These derivatives are dangerous to humans if they accidentally get in contact with the skin, are inhaled, or are ingested, ei ...

Pharmacokinetic and absorption, distribution, metabolism, and excretion (ADME) characterization of antibody–drug conjugates (ADCs) reflects the dynamic interactions between the biological system and ADC, and provides critical assessments in lead selection, optimiz ...

Antibody-drug conjugates (ADCs) are promising biotherapeutics designed to selectively deliver highly cytotoxic drugs to tumor cells while sparing normal tissues. They can be viewed as prodrugs, stable in the bloodstream in order to minimize drug release in circulation and efficie ...

Antibody–drug conjugates (ADCs), which combine the specificity, favorable pharmacokinetics, and biodistribution of a monoclonal antibody (mAb) with the cytotoxic potency of a drug, are promising new therapies for cancer. Along with the development of monoclonal antibodies (mA ...

Toxin payloads, or drugs, are the crucial components of therapeutic antibody–drug conjugates (ADCs). This review will give an introduction on the requirements that make a toxic compound suitable to be used in an antitumoral ADC and will summarize the structural and mechanistic features of ...

Antibody–drug conjugates (ADCs) combine the selectivity of a monoclonal antibody with the killing potency of a cytotoxic drug. For an antibody to function as a successful component of an ADC, it needs to bind to the target antigen on the surface of tumor cells and then be internalized by the cell. Follo ...

ADC success requires that all three components of the agent function in a near-flawless manner. Equally important is that the target be selected with stringent consideration as the target is the one factor in ADC development that is immutable and beyond the reach of the developer to refine/mani ...

Recent developments in biopharmaceutical processes twined with a desire to remove cleaning and cross-contamination issues from drug production have led to the widespread introduction of single-use technologies and systems within operations. One key area that end users need to ad ...

Biological therapies play an increasing role in cancer treatment, although the number of naked antibodies showing clinical efficacy as single agent remains limited. One way to enhance therapeutic potential of antibodies is to conjugate them to small molecule drugs. This combination ...

Imaged capillary isoelectric focusing (icIEF) is capable of monitoring the charge heterogeneity profile of conjugated antibodies. The electropherogram from icIEF can be integrated to quantitate the amount of unconjugated antibody present in a conjugate sample. This chapter d ...

This chapter describes an LC-ESI-MS method for the DAR and drug load distribution analysis that is suitable for lysine-linked ADCs. The ADC sample is desalted using a reversed-phase LC column with an acetonitrile gradient prior to online MS analysis. The MS spectrum is processed (deconvolut ...

Hydrophobic interaction chromatography (HIC) is the method of choice for determination of the drug-to-antibody ratio (DAR) and drug load distribution for cysteine (Cys)-linked antibody–drug conjugates (ADCs). The drug-loaded species are resolved based on the increasing hydro ...

UV/Vis spectroscopy is a simple and convenient method to determine protein concentrations as well as the average number of drugs that are conjugated to the antibody in an antibody–drug conjugate (ADC). Using the measured absorbances of the ADC and the extinction coefficients of the antibody ...

Antibodies are one of the most commonly used targeting ligands for nanocarriers, mainly because they are specific, have a strong binding affinity, and are available for a number of disease biomarkers. The bioconjugation chemistry can be a crucial factor in determining the targeting effic ...

Manufacturing highly potent antibody–drug conjugates (ADCs) is a demanding task—combining conventional organic synthesis with biotechnological manufacturing. Hence a series of new and unique engineering and chemistry challenges have to be addressed to support clinical t ...

Formulation development of an ADC resembles that of a conventional antibody, but the conjugated form introduces new molecular attributes such as drug-to-antibody ratio and stability of the drug itself that need to be considered. An extended set of analytical tools, coupled with underst ...

Enzymatic posttranslational modification of proteins permits more precise control over conjugation site than chemical modification of reactive amino acid side chains. Ideally, protein modification by an enzyme yields completely homogeneous conjugates with improved pr ...

Antibody conjugates are used in many therapeutic and research applications and are generated by chemically linking a cysteine or lysine residue to potent chemotherapeutic drugs or other functional groups through a flexible linker. Recently, we have engineered THIOMABs (antibod ...

Currently, the most widely used chemical methodology for the conjugation of drugs to monoclonal antibodies involves either lysine or cysteine residues. In this chapter, several methods for the preparation of antibody–drug conjugates (ADCs) through conjugation of drugs to solvent ...

Genotoxicity tests are designed to detect the genetic damage by various mechanisms. Several guidelines have provided various tests to be conducted for testing the genotoxicity and each of the regulatory agencies around the world have developed their own requirements for mutagenic ...