1237 Bioanalysis (2015) 7(10), 1237–1251 ISSN 1757-6180
Research Article
part of
10.4155/BIO.15.56 © 2015 Future Science Ltd
Background: In preclinical studies, monoclonal antibodies (mAbs) are traditionally
assayed by ligand-binding-assays. Recently, quantitative liquid chromatography
mass spectrometry (MS)-based assays have emerged which circumvent a number of
challenges. These assays may also be multiplex, making them potentially compatible with
pharmacokinetic assays for combined antibody therapies. Materials & Methods: We
combined a quantitative MS-based approach with the protein standard for absolute
quantification (PSAQ™) strategy to simultaneously quantify three mAb variants
presenting minor sequence differences. Stable isotopically labeled mAbs were
produced and used as quantification standards. Titration curves were performed to
assess the analytical performances of the method. LC-MS/MS and ELISA data were
cross-compared. Results: The approach presented provides similar accuracy and
precision than ELISA, while being multiplex and faster to develop. It has applications
at all stages of the pharmaceutical development.
Background
Monoclonal antibodies (mAbs) and related
derivatives have become a major class of
therapeutic compounds used to treat can-
cers, infectious diseases, allergies, inflam-
mation, and autoimmune diseases due to
their high specificity and efficacy. There
are currently more than 50 approved mAb-
based products available on the market [1] .
Since the first approval of a therapeutic mAb
drug in the late nineties [2] , over 400 thera-
peutic monoclonal antibodies (mAbs) have
been tested in clinical trials. As a result, the
clinical development of this type of bio-
therapeutics is increasingly competitive.
Newly developed therapeutic mAbs should
have optimized physicochemical and phar-
maceutical properties, such as high affinity
and avidity for the target, controlled biodis-
tribution, known effector functions and an
optimized half-life [3,4] . Indeed, suboptimal
pharmacokinetic (PK) properties are among
the reasons that a compound may fail to
reach the market. To avoid discovering
these properties late in the selection process,
multiple structural and sequence variants of
mAb candidates are selected and tested in
early preclinical studies. One of the chal-
lenges for pharmaceutical companies lies
in identifying the candidates with the best
pharmaceutical and clinically relevant fea-
tures as early as possible. These candidates
will have a greater probability of success
(OptimAbs project, which was launched on
26 November 2010, aimed at transforming
therapeutic ‘research leads’ into drug can-
didates by including ‘developability’ crite-
ria beforehand). Meanwhile, R&D strate-
gies have to be developed to limit costs, to
save time and to reduce the risks related
to developing lead candidates. As part of
this, one approach consists in co-injecting
several variant compounds and comparing
their PK properties in a rodent-based tri-
age study, with the objective to limit the
number of later monkey triaging studies.
To do this, robust and rapid bioanalyti-
cal methods are being developed to select
candidates that demonstrate suitable clini-
cal potential based on PK properties. Cur-
rently, ligand-binding-assays (LBAs), such
as ELISA, remain the most common and
Absolute and multiplex quantification
of antibodies in serum using PSAQ™
standards and LC-MS/MS
Dorothee Lebert*
,1
,
Guillaume Picard
1
,
Charlotte Beau-Larvor
2
,
Lysiane Troncy
2
,
Christine Lacheny
2
,
Bernadette Maynadier
3
,
Walter Low
4
, Nicolas
Mouz
1
, Virginie Brun
5,6,7
,
Christine Klinguer-Hamour
2
,
Michel Jaquinod
5,6,7
& Alain Beck
2
1
PROMISE Advanced Proteomics,
Grenoble, F-38040, France
2
Centre d’Immunologie Pierre
Fabre (CIPF), 5 Av. Napoléon III,
BP 60497, 74164 Saint-Julien-en-
Genevois, France
3
Centre d’Etudes Pré-Cliniques Pierre
Fabre, Campans, France
4
PX-Therapeutics, Grenoble,
F-38040, France
5
Université Grenoble Alpes, iRTSV-BGE,
F-38000 Grenoble, France
6
CEA, iRTSV-BGE, F-38000 Grenoble,
France
7
INSERM, BGE, F-38000 Grenoble,
France
*Author for correspondence:
Tel.: +33 438 023 650
dorothee.lebert@
promise-proteomics.com
For reprint orders, please contact reprints@future-science.com