Publications
Publication in Diabetes Research and Clinical Practice: MASLD/MASH and type 2 diabetes: Two sides of the same coin? From single PPAR to pan-PPAR agonists
Publication in Nature Communications: The pan-PPAR agonist lanifibranor improves cardiometabolic health in patients with metabolic dysfunction-associated steatohepatitis
EASL 2024: The pan-PPAR agonist lanifibranor improved altered liver vascular biology in MASH, associated with improved liver histology
EASL 2024: Improvements in MACK-3, a diagnostic test for active metabolic dysfunction-associated steatohepatitis, parallel response to lanifibranor therapy
AASLD 2023: Lanifibranor Reverses Insulin Resistance and Improves Glucose and Lipid Metabolism in Patients with Type 2 Diabetes and Metabolic Dysfunction-Associated Steatotic Liver Disease (MASLD)
AASLD 2023: Lanifibranor improves liver histology and markers of cardiometabolic health in patients with NASH independent of PNPLA3 genotype: a retrospective analysis of the NATIVE study
AASLD 2023: Lanifibranor-associated adiponectin increase correlates with improvement of histological and serum markers of NASH severity both in terms of activity and fibrosis
EASL 2023: The pan-PPAR agonist lanifibranor decreases portal pressure in models of both hepatic and prehepatic portal hypertension
EASL 2023: Unraveling the individual contributions of the PPAR isotypes to the pan-PPAR agonist Lanifibranor-induced improvements of the vascular alterations and liver histology in a rat model of early NAFLD
EASL 2023: The pan-PPAR agonist Lanifibranor improves increased portal pressure, endothelial dysfunction and liver histology in a rat model of early NAFLD
ADA 2023: Lanifibranor Improves Markers of Cardiometabolic Health in Patients with NASH and Type 2 Diabetes, Correlated with Responses in Adiponectin Levels
Lanifibranor-induced improvement of liver and cardiometabolic markers of NASH is associated with an increase in adiponectin
Lanifibranor therapy reduces the FAST score
Identification of biomarkers of histological response in patients with non-cirrhotic NASH treated with lanifibranor
Lanifibranor improves markers of cardio-metabolic health in NASH patients independent of weight change
The pan-PPAR agonist lanifibranor improves NonAlcoholic SteatoHepatitis (NASH) and glycemic control
AASLD 2021: Lanifibranor improves NASH, fibrosis and diastolic dysfunction in a hamster preclinical model of diet induced NASH
AASLD 2021: Liver Sinusoidal Endothelial Cell (LSEC) capillarization in NASH and its evolution following lanifibranor treatment: an exploratory study of the NATIVE clinical trial
AASLD 2021: Treatment response to the PAN-PPAR agonist lanifibranor in the NATIVE study: NASH resolution and fibrosis improvement are correlated
AASLD 2021: Lanifibranor treatment improves hepatic steatosis in patients with NASH, evaluated by histological grading and Controlled Attenuation Parameter (CAP)
AASLD 2021: Lanifibranor reverses fasting glucose levels to normoglycemia in prediabetic patients with nonalcoholic steatohepatitis (NASH)
Treatment of Mucopolysaccharidosis type VI patients with odiparcil alone or in addition to enzyme replacement therapy: a phase IIa study WORDSymposium 2020
Differential effects of selective- and pan-PPAR agonists on experimental steatohepatitis and hepatic macrophages Journal of Hepatology Sander Lefere, Tobias Puengel, Jana Hundertmark, ., Lindsey Devisscher, Guillaume Wettstein, Frank Tacke
AASLD 2020 : Selection based on SAF Activity score instead of NASH CRN NAFLD Activity Score leads to selection of a more severe NASH with more advanced fibrosis patient cohort in the NATIVE phase 2b study of the panPPAR agonist Lanifibranor
AASLD 2020: Effect of the panPPAR agonist lanifibranor on plasma biomarkers of liver necro‐inflammation and fibrosis in non‐cirrhotic NASH patients: additional results of the NA11 12TIVE Phase 2b trial.13
AASLD 2020: Efficacy of the panPPAR agonist lanifibranor on the histological endpoints NASH resolution and fibrosis regression is similar in type‐2 diabetic and non‐diabetic patients: additional results of the NATIVE Phase 2b trial in non‐cirrhotic NASH
Odiparcil, a potential glycosaminoglycans clearance therapy in mucopolysaccharidosis VI—Evidence from in vitro and in vivo models
Eugeni Entchev , Ingrid Jantzen, Philippe Masson, Stephanie Bocart, Bruno Bournique, Jean-Michel Luccarini, Andre Bouchot,Olivier Lacombe, Jean-Louis Junien, Pierre Broqua, Mireille Tallandier
Discovery of YAP-TEAD Protein-Protein interaction inhibitors for treating Malignant Pleural Mesothelioma
Discovery of YAP-TEAD Protein-Protein interaction inhibitors for treating Malignant Pleural Mesothelioma
AACR San Diego, Sep. 2019
A Soude, M. Barth, JM Luccarini, S. Delaporte, F. Chirade, G. Cheret, A. Boulay, C.Valaire, M. Dorchie, C. Estivalet, P. Tuya-Boustugue, C. Montalbetti, R. Tranchant*, D. Jean*, L. Quetel*, JB. Assié,*
I. Konstantinova, JL. Junien & P. Broqua
Discovery of promising anti-cancer drug combination using YAP-TEAD inhibitors with standard of care treatment in mesothelioma and NSCLC cells
EORTC, Nov 2018
Anne Soude, Martine Barth, Séverine Delaporte, Florence Chirade, Geneviève Cheret, Sylvie Contal, Aude Boulay, Christelle Valaire, Christian Montalbetti, Irena Konstantinova, Jean-Louis Junien & Pierre Broqua.
Evidence for Altered Peroxisome Proliferator Activated Receptor (PPAR) Pathway Activity in a Transgenic Mouse Model of Scleroderma (TbetaRIIgammak-fib): Analysis of Mouse Skin, Lung and Explanted Cells
ACR, Oct 2018
Emma Derrett-Smith, Rachel Hoyles, Xu Shi-Wen, Olivier Lacombe, Pierre Broqua, Jean-Louis Junien, Irena Konstantinova, Christopher P Denton
In vivo assessment of lung fibrosis’ prevention using the pan-PPAR agonist lanifibranor in the TbetaRIIgammak-fib (Transgenic Mouse Model of Scleroderma) mouse model of systemic sclerosis
ACR, Oct 2018
Emma C. Derrett-Smith, Shiwen Xu, David Abraham, Olivier Lacombe,Pierre Broqua, Jean-Louis Junien, Irena Konstantinova and Christopher P. Denton
Intracellular GAG Level in Leukocytes is a Promising Pharmacodynamic Biomarker for MPS VI
MPS Symposium, Aug 2018
Paul Harmatz, Laura Pollard, Nick Cantley, JoAnn Johnson, Olivier Lacombe, Jean-Louis Junien, Jean-Louis Abitbol, Mireille Tallandier
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate
the Journal of Medicinal Chemistry, June 2018
Benaïssa Boubia, Olivia Poupardin, Martine Barth, Jean Binet, Philippe Peralba, Laurent Mounier, Elise Jacquier, Emilie Gauthier, Valérie Lepais, Maryline Chatar, Stéphanie Ferry, Anne Thourigny, Fabrice Guillier, Jonathan Llacer, Jérome Amaudrut, Pierre Dodey, Olivier Lacombe, Philippe Masson, Christian Montalbetti, Guillaume Wettstein, Jean-Michel Luccarini, Christiane Legendre, Jean-Louis Junien, and Pierre Broqua
The New-Generation Pan-Peroxisome Proliferator-Activated Receptor Agonist IVA337 Protects the Liver From Metabolic Disorders and Fibrosis
Hepatology Communications, June 2017
Guillaume Wettstein, Jean-Michel Luccarini, Laurence Poekes, Patrick Faye, Francine Kupkowski, Vanessa Adarbes, Evelyne Defrêne, Céline Estivalet, Xavier Gawronski, Ingrid Jantzen, Alain Philippot, Julien Tessier, Pascale Tuyaa-Boustugue, Fiona Oakley, Dereck A. Mann, Isabelle Leclercq, Sven Francque, Irena Konstantinova, Pierre Broqua, and Jean-Louis Junien
IVA337, a PAN-PPAR agonist, reduces NASH features and inhibits the inflammasome in murin models of NASH
EASL, The International Liver Congress, Amsterdam, September 19-23
Guillaume Wettstein, Laurence Poekes, Fiona Oakley, Patrick Faye, Jean-Michel Luccarini, Pierre Broqua, Jean-Louis Junien, Derek Mann, Isabelle Leclercq, Irena Konstantinova
A rational approach for the discovery of NSD2 inhibitors for the treatment of multiple myeloma
2nd Annual Epigenetics Discovery Congress, London, September 8-9
Xavier Espanel, Séverine Estevez, Vanessa Adarbes, Stéphanie Bocart, Bruno Loillier, Séverine Delaporte, Elina Mandry
IVA336 a Potential Substrate Reduction Therapy for Mucopolysaccharidose type-VI, -I, and -II Diseases
MPS 2016, Bonn, July 13-14
Mireille Tallandier ,Philippe Masson, Eugeni Entchev, Sebastien Jacquet, Ingrid Jantzen, Olivier Lacombe, Véronique Douet
A rational approach for the discovery of inhibitors of NSD2 for the treatment of cancer
AACR 2016, New Orleans, April 16-20
Claudia Fromond, Xavier Espanel, Séverine Estevez, Vanessa Adarbes, Stéphanie Bocart, Bruno Loillier
The pan-PPAR agonist IVA337 has anti-fibrotic effects in multiple in vitro and in vivo fibrosis models
4th Systemic Sclerosis World Congress, Lisbon, February 18-20
Irena Konstantinova, Jean-Michel Luccarini, Evelyne Defrêne, Céline Estivalet, Ingrid Jantzen, Julien Tessier.
Discovery of YAP-TEAD Protein-Protein interaction (PPI) inhibitors for the treatment of cancer
AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, Boston, MA, November 5-9
Anne Soude, Martine Barth, Stéphanie Bocart, Frédéric Thoreau, Elina Mandry, Sylvie Contal
A Rational Approach for the Discovery of NSD2 Inhibitors for the Treatment of Cancer
Miptec 2015, Basel, Sept 19-23
13th annual Discovery On Target, Boston, MA, September 22-23
Xavier Espanel, Séverine Estevez, Vanessa Adarbes, Stéphanie Bocart, Bruno Loillier, and Christian Montalbetti
Inhibition of two NADPH-independent enzymatic activities: Aldehyde oxidase and Xanthine oxidase inhibition
18th International Conference on Drug-Drug Interactions ,Washington, June 29- July 1st
Didier Bressac, Rachel Dechaume, Aurélie Péraire, Emmanuel Hardillier, Christelle Gondran, Eric Lecocq, Olivier Lacombe
Rodent Pharmacokinetics and in vitro ADME Properties of IV3086: An orally available and brain penetrant NURR1/RXR Activator
ISSX – 13th European Meeting, Glasgow, June 22-25
Bruno Bournique, Didier Bressac, Emmanuel Hardillier, Olivier Lacombe
A rational approach for the discovery of inhibitors of the YAP-TEAD interaction
Drug Discovery Chemistry , San Diego , April 21-23
Christian Montalbetti, Claudia Fromond, Laurent Chene, Anne Soude, Martine Barth, Sylvie Contal and Pierre Broqua
Identification of G9a inhibitors by AlphaLisa™ technology and hit confirmation using MT-Glo™
AACR, Philadelphia, April 18-22
Claudia Fromond, Xavier Espanel, Laurent Chene, Philippe Masson, BenaïssaBoubia, Christian Montalbetti, Pierre Broqua
A rational approach for the discovery of inhibitors of NSD2 for the treatment of cancer
AACR, Philadelphia, April 18-22
Claudia Fromond, Xavier Espanel, Anne Soudé, Laurent Chene, Philippe Masson, BenaïssaBoubia, Christian Montalbetti and Pierre Broqua
A rational approach for discovery of inhibitors of YAP-TEAD interaction
AACR, Philadelphia, April 18-22
Claudia Fromond, Laurent Chene, Anne Soude, Martine Barth, Christian Montalbetti and Pierre Broqua
Identification of G9a inhibitors by Alphalisa™ and hit confirmation using MT-Glo™
SLAS 2015, Washington DC, February 7-11.
Philippe Masson, Vanessa Adarbes, Stéphanie Bocart , Séverine Estevez , Bruno Loillier, Laurent Chêne, Christian Montalbetti, Claudia Fromond, Benaissa Boubia and Xavier Espanel.
Ultrafast LC-UV-ELSD-MS confirming the high quality of Inventiva’s screening collection
SLAS 2015, Washington DC, February 7-11.
Frédéric Bell, Clément Gaiffe, Amandine Vessot Jérôme Amaudrut, Sylvaine Marie, Philippe Masson.
A rational approach for the discovery of inhibitors of NSD2 for the treatment of cancer
Epigenetics and Cancer , Keystone Colorado , January 25-30.
Xavier Espanel, Séverine Estevez, Vanessa Adarbes, Stéphanie Bocart, Bruno Loillier, Séverine Delaporte, Elina Mandry, Anne Soudé, Laurent Chene, Philippe Masson, Benaïssa Boubia, Christian Montalbetti, Pierre Broqua and Claudia Fromond.
Identification of novel EZH2 inhibitor scaffolds
26th EORTC-NCI-AACR symposium, Barcelona, Nov 18-21.
Xavier Espanel, Laurent Chene, Anne Soude, Séverine Estevez, Vanessa Adarbes, Bruno Loillier, Benaissa Boubia, Philippe Masson, Christian Montalbetti, Pierre Broqua & Claudia Z. A. Fromond.
A rational approach for discovery of inhibitors of YAP-TEAD interaction
26th EORTC-NCI-AACR symposium, Barcelona, Nov 18-21.
Laurent Chene, Anne Soude, Christelle Valaire, Severine Delaporte, Sebastien Jacquet, Yves Cambet, Isabelle Braccini, Martine Barth, Christian Montalbetti, Pierre Broqua & Claudia Z-A Fromond.
One Hour Pre-Infusion followed by Four Hours Co-Infusion of Elacridar as a Tool to Identify the Involvement of P-gp and BCRP in the Brain Penetration of Test Compounds in Rats
19th North American Congress of the International Society for the Study of Xenobiotics, San Francisco, Oct 19-23.
B. Bournique, B. Cautain, V. Douet, C. Eymann, C. Gondran, E. Hardillier, L. Nicolas, O. Lacombe.
A Useful Relationship between In Vivo Rat Kp Brain and In Vitro Caco-2 Cells Efflux Ratio
19th North American Congress of the International Society for the Study of Xenobiotics, San Francisco, Oct 19-23.
B. Bournique, JM. Bony, D.Bressac, B. Cautain, R.Dechaume, V. Douet, C. Eymann, C. Gondran, E.Hardillier, L. Nicolas, O. Lacombe.
A Rapid LC-hrMS Method for Metabolite Identification Simultaneously to Metabolic Stability Assessment on Microsomes at an Early Screening Stage
International Mass Spectrometry,Geneve,August 24-29.
Emmanuel Hardillier, Didier Bressac, Olivier Lacombe
Discovery and optimization of indoline derivatives as new LXR agonists
248TH ACS National Meeting & Exposition, San Francisco, August 10-14.
Dominique Potin, Jérôme Amaudrut
Compound-oriented preparative HPLC purification platform
10th International Symposium on Drug Analysis, Liège, June 23-25.
Nathalie Urban, Frédéric Bell, Cyrielle Couchoux
Solubility toolbox for successful design of drug candidates
10th International Symposium on Drug Analysis, Liège, June 23-25.
Frédéric Bell, Caroline Durand, Nathalie Urban
In Vitro-In Vivo Correlation (IVIVC) for clearance estimation in earlyADME : the importance of unbound fraction assessment in plasma and microsomes
20th International Symposium on Microsomes and Drug Oxidations, Leinfelden, May 18-22.
Didier Bressac, Rachel Dechaume, Jeanne-Marie Bony, Olivier Lacombe
Screening Library Enrichment: Criteria that matter, timely manner
Openeye European User Meeting, Mery sur Oise, May 14-16.
Jérôme Amaudrut, Fabrice Guillier
Development and automation of a fibrotic phenotypic screening using a High Content Screening approach
Keystone Fibrosis, Keystone Colorado, March 23-28.
Laurent Chêne, Anne Soude, Philippe Masson and Xavier Espanel
Identification of novel EZH2 inhibitor scaffolds
Keystone Cancer Epigenetics, Santa Fé, February 4-9.
Xavier Espanel, Christian Montalbetti, Claudia Fromond
A Selective NURR1/RXR activation for treating Parkinson’s disease
Keystone Nuclear Receptors ,Taos , January 10-15.
B.Boubia, O. Lacombe, M. Tallandier
Practical synthesis of N-substituted naphthyridine
18th European Symposium on Organic Chemistry, Marseille, July 7-12.
Laurent Mignon
Synthesis of substituted phenyl acetic acid and 5-membered heterocycles derivatives
18th European Symposium on Organic Chemistry , Marseille, July 7-12.
L. Mounier, M. Barth, B. Boubia
Supporting the Reactivity Assessment of an IVA Acyl-Glucuronide Derivative
HPLC 2013, Amsterdam, June 16-20.
Emmanuel Hardillier, Béatrice Cautain, Olivier Lacombe
Interaction scanning libraries: A general strategy for scaffold functionalization
International Symposium on Advances in Synthetic and Medicinal Chemistry, Moscow, May 5-8.
Fabrice Guillier, Jérôme Amaudrut, Jonathan Llacer, Jérôme Gonzalez