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mAbs Have Distinct Characteristics, Including High Specificity for a Single Target


mAbs Function Through Two Different Mechanisms

Indirect Mechanism (Activates Host Immune System)1,2

mAbs mediate immune response via cell-mediated cytotoxicity (in which a mAb binds a target cell and recruits effector immune cells, such as macrophages or natural killer cells) or complement-dependent cytotoxicity (in which a mAb activates the complement cascade in the target cell, which disrupts cell membrane integrity).1

Direct Mechanism (Independent of Host Immune System)1-3

mAbs can bind to target ligands and prevent their interaction with target cells. The therapeutic effect of the mAb may be affected by the local concentration of the target ligand. mAbs can also bind to target receptors, preventing ligand-receptor interactions.

mAb, monoclonal antibody.1. Foltz IN, et al. Circulation. 2013;127:2222-2230. 2. Silberstein S, et al. Headache. 2015;55:1171-1182. 3. Goel G, et al. J Hematol Oncol. 2015;8:92.
mAbs &
small molecules
Antibody-based
therapeutics

Summary of Differences Between mAbs and Small Molecules1

PropertySmall molecule mAb
Size~500 daltons~150,000 daltons
SpecificityLowerHigh
MetabolismHepatic/RenalReticuloendothelial system,
target-mediated disposition
ToxicityBroken down into chemical metabolites;
often cleared by liver or kidneys
On-target (depends on the target of the mAb)
and off-target toxicities (eg, immunogenicity)
Drug-drug interactionsMore likelyLess likely
Crossing blood-brain barrier2Potentially yes*Minimal
AdministrationUsually oralIntramuscular, subcutaneous,
or intravenous
Half-life3~HoursDays to weeks
DosingUsually dailyTypically less frequent (eg, monthly)
Production4,5Chemical synthesis; relatively easy
to make and reproduce reliably
Produced inside unique line of modified living
cells; difficult to make and reproduce precisely

*Depending on degree of lipid solubility.

mAb, monoclonal antibody.
1. Foltz IN, et al. Circulation. 2013;127:2222-2230. 2. Tabrizi M, et al. AAPS J. 2010;12:33-43. 3. Silberstein S, et al. Headache. 2015;55:1171-1182. 4. Kleinberg M, et al. Am J Health
Syst Pharm. 2004;61:695-710. 5. Committee on Methods of Producing Monoclonal Antibodies. Monoclonal Antibody Production. 1999.

Antibody-Based Therapeutics

Research and Development of mAbs Is Rapidly Evolving

The First mAb Was Produced in 1975; Since Then1

mAb, monoclonal antibody.
1. Silberstein S, et al. Headache. 2015;55:1171-1182. 2. Cai HH. MOJ Immunology. 2017;5:145. 3. Foltz IN, et al. Circulation. 2013;127:2222-2230.