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Article ; Online: A method to assess the robustness of complex mathematical models used for quantitative interpretation of experimental data by nonlinear regression analysis: application to high-affinity binding models.

Vanhove, Marc

2021 Volume 50, Issue 7, Page(s) 1045–1054

Abstract: Nonlinear regression is widely used to fit experimental data to a specific mathematical model to extract numerical values for parameters representing the studied process. However, assessing the degree of precision that can be expected from such an ... ...

Abstract	Nonlinear regression is widely used to fit experimental data to a specific mathematical model to extract numerical values for parameters representing the studied process. However, assessing the degree of precision that can be expected from such an analysis for a given parameter can be quite challenging for complex mathematical models. To address this issue, we propose here a method based on the analysis of a large number of data sets generated in such a way to mimic specific experimental conditions. Applying this methodology to high-affinity binding models, we report here a quantitative analysis of the robustness of such models, and how the precision on the fitting parameters can be expected to vary based on, e.g., the initial experimental conditions, the number or distribution of experimental points, or the experimental variability. We also show that these models, although widely used, are intrinsically limited by the fact that the two main fitting parameters, one representing the concentration of the studied species and the other its affinity, are inversely correlated, but demonstrate that this limitation can be overcome by global analysis of multiple data series generated at different concentrations of the titrated species.
MeSH term(s)	Models, Biological
Language	English
Publishing date	2021-06-17
Publishing country	Germany
Document type	Journal Article
ZDB-ID	283671-3
ISSN	1432-1017 ; 0175-7571
ISSN (online)	1432-1017
ISSN	0175-7571
DOI	10.1007/s00249-021-01556-y
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Article ; Online: K

Spiegelberg, Diana / Stenberg, Jonas / Richalet, Pascale / Vanhove, Marc

European biophysics journal : EBJ

2021 Volume 50, Issue 7, Page(s) 979–991

Abstract: Design of next-generation therapeutics comes with new challenges and emulates technology and methods to meet them. Characterizing the binding of either natural ligands or therapeutic proteins to cell-surface receptors, for which relevant recombinant ... ...

Abstract	Design of next-generation therapeutics comes with new challenges and emulates technology and methods to meet them. Characterizing the binding of either natural ligands or therapeutic proteins to cell-surface receptors, for which relevant recombinant versions may not exist, represents one of these challenges. Here we report the characterization of the interaction of five different antibody therapeutics (Trastuzumab, Rituximab, Panitumumab, Pertuzumab, and Cetuximab) with their cognate target receptors using LigandTracer. The method offers the advantage of being performed on live cells, alleviating the need for a recombinant source of the receptor. Furthermore, time-resolved measurements, in addition to allowing the determination of the affinity of the studied drug to its target, give access to the binding kinetics thereby providing a full characterization of the system. In this study, we also compared time-resolved LigandTracer data with end-point K
MeSH term(s)	Cetuximab ; Flow Cytometry ; Kinetics ; Ligands ; Receptors, Cell Surface
Chemical Substances	Ligands ; Receptors, Cell Surface ; Cetuximab (PQX0D8J21J)
Language	English
Publishing date	2021-07-24
Publishing country	Germany
Document type	Journal Article
ZDB-ID	283671-3
ISSN	1432-1017 ; 0175-7571
ISSN (online)	1432-1017
ISSN	0175-7571
DOI	10.1007/s00249-021-01560-2
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Article ; Online: Affinity determination of biomolecules: a kinetic model for the analysis of pre-equilibrium titration curves.

Vanhove, Emilie / Vanhove, Marc

European biophysics journal : EBJ

2018 Volume 47, Issue 8, Page(s) 961–966

Abstract: Equilibrium titration curves have been used to determine the affinity of biomolecules using a variety of platforms and technologies. Such measurements, however, are experimentally limited by the time that is needed for the system to reach the equilibrium, ...

Abstract	Equilibrium titration curves have been used to determine the affinity of biomolecules using a variety of platforms and technologies. Such measurements, however, are experimentally limited by the time that is needed for the system to reach the equilibrium, which may exceed the time during which the studied biomolecules are stable. We propose here a kinetic model to analyze titration curves obtained prior to full equilibration of the system.
MeSH term(s)	Kinetics ; Models, Chemical
Language	English
Publishing date	2018-07-10
Publishing country	Germany
Document type	Journal Article
ZDB-ID	283671-3
ISSN	1432-1017 ; 0175-7571
ISSN (online)	1432-1017
ISSN	0175-7571
DOI	10.1007/s00249-018-1318-y
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Article ; Online: A novel assay based on pre-equilibrium titration curves for the determination of enzyme inhibitor binding kinetics.

Noppen, Bernard / Vanbelle, Anouk / Stitt, Alan W / Vanhove, Marc

European biophysics journal : EBJ

2021 Volume 50, Issue 7, Page(s) 1037–1043

Abstract: Selection of pharmacological agents based on potency measurements performed at equilibrium fail to incorporate the kinetic aspects of the drug-target interaction. Here we describe a method for screening or characterization of enzyme inhibitors that ... ...

Abstract	Selection of pharmacological agents based on potency measurements performed at equilibrium fail to incorporate the kinetic aspects of the drug-target interaction. Here we describe a method for screening or characterization of enzyme inhibitors that allows the concomitant determination of the equilibrium inhibition constant in unison with rates of complex formation and dissociation. The assay is distinct from conventional enzymatic assays and is based on the analysis of inhibition curves recorded prior to full equilibration of the system. The methodology is illustrated using bicyclic peptide inhibitors of the serine protease plasma kallikrein.
MeSH term(s)	Enzyme Inhibitors/pharmacology ; Kinetics ; Protein Binding ; Serine Endopeptidases
Chemical Substances	Enzyme Inhibitors ; Serine Endopeptidases (EC 3.4.21.-)
Language	English
Publishing date	2021-06-22
Publishing country	Germany
Document type	Journal Article
ZDB-ID	283671-3
ISSN	1432-1017 ; 0175-7571
ISSN (online)	1432-1017
ISSN	0175-7571
DOI	10.1007/s00249-021-01554-0
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Article ; Online: Systemic exposure following intravitreal administration of therapeutic agents: an integrated pharmacokinetic approach. 2. THR-687.

Vanhove, Marc / Wagner, Jean-Marc / Noppen, Bernard / Jonckx, Bart / Vermassen, Elke / Stitt, Alan W

Journal of pharmacokinetics and pharmacodynamics

2021 Volume 48, Issue 6, Page(s) 837–849

Abstract: Intravitreal (IVT) injection remains the preferred administration route of pharmacological agents intended for the treatment of back of the eye diseases such as diabetic macular edema (DME) and neovascular age-related macular degeneration (nvAMD). The ... ...

Abstract	Intravitreal (IVT) injection remains the preferred administration route of pharmacological agents intended for the treatment of back of the eye diseases such as diabetic macular edema (DME) and neovascular age-related macular degeneration (nvAMD). The procedure enables drugs to be delivered locally at high concentrations whilst limiting whole body exposure and associated risk of systemic adverse events. Nevertheless, intravitreally-delivered drugs do enter the general circulation and achieving an accurate understanding of systemic exposure is pivotal for the evaluation and development of drugs administered in the eye. We report here the full pharmacokinetic properties of THR-687, a pan RGD integrin antagonist currently in clinical development for the treatment of DME, in both rabbit and minipig. Pharmacokinetic characterization included description of vitreal elimination, of systemic pharmacokinetics, and of systemic exposure following IVT administration. For the latter, we present a novel pharmacokinetic model that assumes clear partition between the vitreous humor compartment itself where the drug is administered and the central systemic compartment. We also propose an analytical solution to the system of differential equations that represent the pharmacokinetic model, thereby allowing data analysis with standard nonlinear regression analysis. The model accurately describes circulating levels of THR-687 following IVT administration in relevant animal models, and we suggest that this approach is relevant to a range of drugs and analysis of subsequent systemic exposure.
MeSH term(s)	Animals ; Diabetic Retinopathy/drug therapy ; Intravitreal Injections ; Macular Edema/drug therapy ; Rabbits ; Swine ; Swine, Miniature ; Vitreous Body
Language	English
Publishing date	2021-07-23
Publishing country	United States
Document type	Journal Article
ZDB-ID	2041601-5
ISSN	1573-8744 ; 1567-567X
ISSN (online)	1573-8744
ISSN	1567-567X
DOI	10.1007/s10928-021-09774-9
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Article ; Online: Systemic exposure following intravitreal administration of therapeutic agents: an integrated pharmacokinetic approach. 1. THR-149.

Vanhove, Marc / Noppen, Bernard / Wagner, Jean-Marc / Van Bergen, Tine / Barbeaux, Philippe / Stitt, Alan W

Journal of pharmacokinetics and pharmacodynamics

2021 Volume 48, Issue 6, Page(s) 825–836

Abstract: Intravitreal (IVT) injection of pharmacological agents is an established and widely used procedure for the treatment of many posterior segment of the eye diseases. IVT injections permit drugs to reach high concentrations in the retina whilst limiting ... ...

Abstract	Intravitreal (IVT) injection of pharmacological agents is an established and widely used procedure for the treatment of many posterior segment of the eye diseases. IVT injections permit drugs to reach high concentrations in the retina whilst limiting systemic exposure. Beyond the risk of secondary complications such as intraocular infection, the potential of systemic adverse events cannot be neglected. Therefore, a detailed understanding of the rules governing systemic exposure following IVT drug administration remains a prerequisite for the evaluation and development of new pharmacological agents intended for eye delivery. We present here a novel mathematical model to describe and predict circulating drug levels following IVT in the rabbit eye, a species which is widely used for drug delivery, pharmacokinetic, and pharmacodynamic studies. The mathematical expression was derived from a pharmacokinetic model that assumes the existence of a compartment between the vitreous humor compartment itself and the systemic compartment. We show that the model accurately describes circulating levels of THR-149, a plasma kallikrein inhibitor in development for the treatment of diabetic macular edema. We hypothesize that the model based on the rabbit eye has broader relevance to the human eye and can be used to analyze systemic exposure of a variety of drugs delivered in the eye.
MeSH term(s)	Animals ; Diabetic Retinopathy/drug therapy ; Macular Edema/drug therapy ; Macular Edema/metabolism ; Pharmaceutical Preparations/metabolism ; Rabbits ; Retina/metabolism ; Vitreous Body/metabolism
Chemical Substances	Pharmaceutical Preparations
Language	English
Publishing date	2021-07-23
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2041601-5
ISSN	1573-8744 ; 1567-567X
ISSN (online)	1573-8744
ISSN	1567-567X
DOI	10.1007/s10928-021-09773-w
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Article ; Online: A novel, label-free, pre-equilibrium assay to determine the association and dissociation rate constants of therapeutic antibodies on living cells.

Janezic, Eric M / Doan, Alexander / Mai, Elaine / Bravo, Daniel D / Wang, Jianyong / Kim, Hok Seon / Spiess, Christoph / Bewley, Kathryn / ElSohly, Adel / Liang, Wei-Ching / Koerber, James T / Richalet, Pascale / Vanhove, Marc / Comps-Agrar, Laetitia

British journal of pharmacology

2023

Abstract: Background and purpose: Monoclonal antibodies (Ab) represent the fastest growing drug class. Knowledge of the biophysical parameters (k: Experimental approach: We developed a pre-equilibrium kinetic exclusion assay using recent mathematical advances ... ...

Abstract	Background and purpose: Monoclonal antibodies (Ab) represent the fastest growing drug class. Knowledge of the biophysical parameters (k Experimental approach: We developed a pre-equilibrium kinetic exclusion assay using recent mathematical advances to determine the k Key results: Using our novel assay, we demonstrated for several monoclonal Ab:receptor pairs that the calculated kinetic rate constants were comparable with orthogonal methods that were lower throughput or more resource consuming. We ran simulations to predict the critical conditions to improve the performance of the assays. We further showed that this method could successfully be applied to both suspension and adherent cells. Finally, we demonstrated that k Conclusions and implications: Our novel assay has the potential to systematically probe binding kinetics of monoclonal Abs to cells and can be incorporated in a screening cascade to identify new therapeutic candidates. Wide-spread adoption of pre-equilibrium assays using physiologically relevant systems will lead to a more holistic understanding of how Ab binding kinetics influence their potency.
Language	English
Publishing date	2023-10-02
Publishing country	England
Document type	Journal Article
ZDB-ID	80081-8
ISSN	1476-5381 ; 0007-1188
ISSN (online)	1476-5381
ISSN	0007-1188
DOI	10.1111/bph.16258
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Article ; Online: Intravitreally Injected Fluid Dispersion: Importance of Injection Technique.

Willekens, Koen / Reyns, Geert / Diricx, Marjan / Vanhove, Marc / Noppen, Bernard / Coudyzer, Walter / Ni, Yicheng / Feyen, Jean H M / Stalmans, Peter

Investigative ophthalmology & visual science

2017 Volume 58, Issue 3, Page(s) 1434–1441

Abstract: Purpose: The purpose of this study was to evaluate the dispersion of intravitreally injected solutions and investigate the influence of varying injection techniques.: Methods: This was a prospective study using enucleated porcine eyes and ultra-high- ... ...

Abstract	Purpose: The purpose of this study was to evaluate the dispersion of intravitreally injected solutions and investigate the influence of varying injection techniques. Methods: This was a prospective study using enucleated porcine eyes and ultra-high-resolution computed tomography (UHRCT) scanning to visualize iomeprol intravitreal dispersion. Sixty eyes were divided over 12 different groups according to the injection procedure: fast (2 seconds) or slow (10 seconds) injection speed and needle tip location (6- and 12-mm needle shaft insertion or premacular tip placement verified by indirect ophthalmoscopy). For each of these combinations, eyes were either injected with the combination of V20I (which is an analogue of ocriplasmin) and iomeprol or iomeprol alone. Distance to the macula and volume measurements were performed at 1, 2, 3, and 5 hours after injection. Results: The measured contrast bolus volume increases slowly over time to an average of 0.70 (P = 0.03), 1.04 (P = 0.006), and 0.79 (P = 0.0001) cm3 5 hours after the injection for the 6-mm needle shaft insertion, 12-mm needle shaft insertion, and premacular needle tip placement, respectively. The distance to the macular marker was significantly lower for premacular needle tip placement injections compared with 6- and 12-mm needle shaft insertion depths. Conclusions: Ultra-high-resolution computed tomography with three-dimensional reconstruction offers the possibility to study the dispersion of intravitreally injected solutions in a noninvasive manner. Intravitreal premacular solution delivery is possible with an indirect ophthalmoscope-guided injection technique and significantly reduces the time to reach the posterior pole in respect to 6- and 12-mm needle insertion depths. The speed of injection does not influence dispersion significantly.
MeSH term(s)	Animals ; Contrast Media/administration & dosage ; Drug Combinations ; Electroretinography ; Equipment Design ; Fibrinolysin/administration & dosage ; Fibrinolysin/pharmacokinetics ; Follow-Up Studies ; Imaging, Three-Dimensional ; Intravitreal Injections/instrumentation ; Iopamidol/administration & dosage ; Iopamidol/analogs & derivatives ; Iopamidol/pharmacokinetics ; Models, Animal ; Ophthalmoscopy ; Peptide Fragments/administration & dosage ; Peptide Fragments/pharmacokinetics ; Pilot Projects ; Prospective Studies ; Swine ; Tomography, X-Ray Computed ; Vitreous Body/diagnostic imaging ; Vitreous Body/metabolism
Chemical Substances	Contrast Media ; Drug Combinations ; Peptide Fragments ; iomeprol (17E17JBP8L) ; microplasmin (7V6HE3DM5A) ; Fibrinolysin (EC 3.4.21.7) ; Iopamidol (JR13W81H44)
Language	English
Publishing date	2017-03-01
Publishing country	United States
Document type	Journal Article
ZDB-ID	391794-0
ISSN	1552-5783 ; 0146-0404
ISSN (online)	1552-5783
ISSN	0146-0404
DOI	10.1167/iovs.16-20543
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Article ; Online: The potent small molecule integrin antagonist THR-687 is a promising next-generation therapy for retinal vascular disorders.

Hu, Tjing-Tjing / Vanhove, Marc / Porcu, Michaël / Van Hove, Inge / Van Bergen, Tine / Jonckx, Bart / Barbeaux, Philippe / Vermassen, Elke / Feyen, Jean H M

Experimental eye research

2018 Volume 180, Page(s) 43–52

Abstract: Integrins are associated with various eye diseases such as diabetic retinopathy (DR) and wet age-related macular degeneration (AMD) and implicated in main pathologic disease hallmarks like neovascularization, inflammation, fibrosis and vascular leakage. ... ...

Abstract	Integrins are associated with various eye diseases such as diabetic retinopathy (DR) and wet age-related macular degeneration (AMD) and implicated in main pathologic disease hallmarks like neovascularization, inflammation, fibrosis and vascular leakage. Targeting integrins has the potential to attenuate these vision-threatening processes, independent of anti-vascular endothelial growth factor (VEGF) responsiveness. The current investigation characterized THR-687 as a novel pan RGD (arginylglycylaspartic acid) integrin receptor antagonist able to compete for binding with the natural ligand with nanomolar potency (e.g. α
MeSH term(s)	Animals ; Capillary Permeability/drug effects ; Cell Movement/drug effects ; Choroidal Neovascularization/drug therapy ; Diabetic Retinopathy/drug therapy ; Disease Models, Animal ; Enzyme-Linked Immunosorbent Assay ; Fluorescein Angiography ; Human Umbilical Vein Endothelial Cells ; Humans ; Injections, Intraperitoneal ; Intravitreal Injections ; Macaca fascicularis ; Male ; Mice ; Mice, Inbred C57BL ; Organic Chemicals/pharmacology ; Organic Chemicals/therapeutic use ; Rabbits ; Receptors, Immunologic/antagonists & inhibitors ; Receptors, Peptide/antagonists & inhibitors ; Retinal Vessels/drug effects ; Tomography, Optical Coherence ; Vascular Endothelial Growth Factor A/pharmacology ; Wet Macular Degeneration/drug therapy
Chemical Substances	Organic Chemicals ; Receptors, Immunologic ; Receptors, Peptide ; Vascular Endothelial Growth Factor A ; arginyl-glycyl-aspartic acid directed cell adhesion receptor ; integrin receptor antagonist THR-687
Language	English
Publishing date	2018-11-22
Publishing country	England
Document type	Journal Article
ZDB-ID	80122-7
ISSN	1096-0007 ; 0014-4835
ISSN (online)	1096-0007
ISSN	0014-4835
DOI	10.1016/j.exer.2018.11.022
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Article ; Online: Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.

Teufel, Daniel P / Bennett, Gavin / Harrison, Helen / van Rietschoten, Katerine / Pavan, Silvia / Stace, Catherine / Le Floch, François / Van Bergen, Tine / Vermassen, Elke / Barbeaux, Philippe / Hu, Tjing-Tjing / Feyen, Jean H M / Vanhove, Marc

Journal of medicinal chemistry

2018 Volume 61, Issue 7, Page(s) 2823–2836

Abstract: Plasma kallikrein, a member of the kallikrein-kinin system, catalyzes the release of the bioactive peptide bradykinin, which induces inflammation, vasodilation, vessel permeability, and pain. Preclinical evidence implicates the activity of plasma ... ...

Abstract	Plasma kallikrein, a member of the kallikrein-kinin system, catalyzes the release of the bioactive peptide bradykinin, which induces inflammation, vasodilation, vessel permeability, and pain. Preclinical evidence implicates the activity of plasma kallikrein in diabetic retinopathy, which is a leading cause of visual loss in patients suffering from diabetes mellitus. Employing a technology based on phage-display combined with chemical cyclization, we have identified highly selective bicyclic peptide inhibitors with nano- and picomolar potencies toward plasma kallikrein. Stability in biological matrices was either intrinsic to the peptide or engineered via the introduction of non-natural amino acids and nonpeptidic bonds. The peptides prevented bradykinin release in vitro, and in vivo efficacy was demonstrated in both a rat paw edema model and in rodent models of diabetes-induced retinal permeability. With a highly extended half-life of ∼40 h in rabbit eyes following intravitreal administration, the bicyclic peptides are promising novel agents for the treatment of diabetic retinopathy and diabetic macular edema.
MeSH term(s)	Animals ; Bradykinin/metabolism ; Bridged Bicyclo Compounds/chemical synthesis ; Bridged Bicyclo Compounds/pharmacology ; Diabetes Complications/drug therapy ; Diabetic Retinopathy/drug therapy ; Edema/drug therapy ; Eye/metabolism ; Foot/pathology ; Half-Life ; Intravitreal Injections ; Macular Edema/drug therapy ; Macular Edema/etiology ; Male ; Mice ; Mice, Inbred C57BL ; Permeability ; Plasma Kallikrein/antagonists & inhibitors ; Protease Inhibitors/administration & dosage ; Protease Inhibitors/chemical synthesis ; Protease Inhibitors/pharmacology ; Rabbits ; Rats ; Rats, Sprague-Dawley ; Structure-Activity Relationship ; Substrate Specificity ; Vitreous Body/chemistry ; Vitreous Body/metabolism
Chemical Substances	Bridged Bicyclo Compounds ; Protease Inhibitors ; Plasma Kallikrein (EC 3.4.21.34) ; Bradykinin (S8TIM42R2W)
Language	English
Publishing date	2018-03-15
Publishing country	United States
Document type	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.7b01625
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