Pharmacokinetics of monoclonal antibodies


DOI: https://dx.doi.org/10.18565/therapy.2020.2.114-122

Talibov O.B.

A.I. Evdokimov Moscow State University of Medicine and Dentistry of the Ministry of Healthcare of Russia
This is the summary on pharmacokinetics of monoclonal antibodies. Monoclonal antibodies are proteins, and, therefore, have special pharmacokinetics parameters.
After oral administration, not more than 1–2% of the total dose will be absorbed.
Monoclonal antibodies are usually administered by intravenous injections and subcutaneous injections; intramuscular injections are used less frequently. Time to maximum concentration is longer (from 2 to 14 days) after subcutaneous injections.
Drug distribution profile can be described using classic two compartment model, with 2–3L central compartment and 8–20L peripheral compartment.
Elimination is mediated mainly by specific target-based mechanisms. Half-life time may vary from 1 week to 18–21 days. Monoclonal antibodies are eliminated primarily via intracellular lysosomal degradation to short peptides and amino acids.
General immune status, as well as total amount of drug target units may have an impact on elimination; therapeutic response may lead to reduced elimination rate.
Non-linear kinetics was observed for moderate and high doses; this may be explained by saturation of receptors that mediate elimination.
Keywords: pharmacokinetic modeling, non-linear pharmacokinetics, distribution, absorption, elimination, monoclonal antibodies, pharmacokinetics
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About the Autors

Oleg B. Talibov, PhD, associate professor of the Department of therapy, clinical pharmacology and emergency medical care of A.I. Evdokimov Moscow State University of Medicine and Dentistry of the Ministry of Healthcare of Russia. Address: 127473, Moscow, 20/1 Delegatskaya Str. E-mail: oleg.talibov@gmail.com.
ORCID: https://orcid.org/0000-0001-6381-2450.


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