Search Results - "Lebre, Maria C."

ABCB1 attenuates brain exposure to the KRASG12C inhibitor opnurasib whereas binding to mouse carboxylesterase 1c influences its plasma exposure by Rijmers, Jamie, Retmana, Irene A., Bui, Viët, Arguedas, Davinia, Lebre, Maria C., Sparidans, Rolf W., Beijnen, Jos H., Schinkel, Alfred H.

“…Opnurasib (JDQ443) is a newly developed oral KRASG12C inhibitor, with a binding mechanism distinct from the registered KRASG12C inhibitors sotorasib and…”
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Brain accumulation of tivozanib is restricted by ABCB1 (P-glycoprotein) and ABCG2 (breast cancer resistance protein) in mice by Wang, Jing, Bruin, Maaike A.C., Gan, Changpei, Lebre, Maria C., Rosing, Hilde, Beijnen, Jos H., Schinkel, Alfred H.

“…[Display omitted] Tivozanib is a potent and selective inhibitor of VEGFR1-3, recently approved by the EMA for first-line treatment of renal cell carcinoma. We…”
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Pharmacokinetics of the KRASG12C inhibitor adagrasib is limited by CYP3A and ABCB1, and influenced by binding to mouse plasma carboxylesterase 1c by Loos, Nancy H.C., Retmana, Irene A., Rijmers, Jamie, Wang, Yaogeng, Gan, Changpei, Lebre, Maria C., Sparidans, Rolf W., Beijnen, Jos H., Schinkel, Alfred H.

“…Adagrasib (Krazati™) is the second FDA-approved specific KRASG12C inhibitor for non-small cell lung cancer (NSCLC) patients harboring this mutation. The impact…”
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Organic anion-transporting polypeptide 2B1 knockout and humanized mice; insights into the handling of bilirubin and drugs by Li, Wenlong, Iusuf, Dilek, Sparidans, Rolf W., Wagenaar, Els, Wang, Yaogeng, de Waart, Dirk R., Martins, Margarida L.F., van Hoppe, Stéphanie, Lebre, Maria C., van Tellingen, Olaf, Beijnen, Jos H., Schinkel, Alfred H.

“…Organic anion transporting polypeptide 2B1 (OATP2B1/SLCO2B1) facilitates uptake transport of structurally diverse endogenous and exogenous compounds. To…”
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Anti-TNF therapy reduces serum levels of chemerin in rheumatoid arthritis: a new mechanism by which anti-TNF might reduce inflammation by Herenius, Marieke M J, Oliveira, Ana S F, Wijbrandts, Carla A, Gerlag, Daniëlle M, Tak, Paul P, Lebre, Maria C

“…Chemerin is a specific chemoattractant for macrophages and dendritic cells (DC). In addition, it can rapidly stimulate macrophage adhesion to extracellular…”
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Human Keratinocytes Express Functional Toll-Like Receptor 3, 4, 5, and 9 by Lebre, Maria C., van der Aar, Angelic M.G., van Baarsen, Lisa, van Capel, Toni M.M., Schuitemaker, Joost H.N., Kapsenberg, Martien L., de Jong, Esther C.

“…Keratinocytes are continuously in contact with external stimuli and have the capacity to produce several soluble mediators. Pathogen-associated molecular…”
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Interplay of OATP1A/1B/2B1 uptake transporters and ABCB1 and ABCG2 efflux transporters in the handling of bilirubin and drugs by Li, Wenlong, Sparidans, Rolf W., Wang, Yaogeng, Martins, Margarida L.F., de Waart, Dirk R., van Tellingen, Olaf, Song, Ji-Ying, Lebre, Maria C., van Hoppe, Stéphanie, Wagenaar, Els, Beijnen, Jos H., Schinkel, Alfred H.

“…Transmembrane drug transporters can be important determinants of the pharmacokinetics, efficacy, and safety profiles of drugs. To investigate the potential…”
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P-glycoprotein (MDR1/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2) limit brain accumulation of the FLT3 inhibitor quizartinib in mice by Wang, Jing, Gan, Changpei, Retmana, Irene A., Sparidans, Rolf W., Li, Wenlong, Lebre, Maria C., Beijnen, Jos H., Schinkel, Alfred H.

“…[Display omitted] Quizartinib, a second-generation FLT3 inhibitor, is in clinical development for the treatment of acute myeloid leukemia. We studied its…”
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Natural deletion of mouse carboxylesterases Ces1c/d/e impacts drug metabolism and metabolic syndrome development by Gan, Changpei, Wang, Jing, Wang, Yaogeng, Martínez-Chávez, Alejandra, Hillebrand, Michel, de Vries, Niels, Beukers, Joke, Lebre, Maria C., Wagenaar, Els, Rosing, Hilde, Klarenbeek, Sjoerd, Bleijerveld, Onno B., Song, Ji-Ying, Altelaar, Maarten, Beijnen, Jos H., Schinkel, Alfred H.

“…Mammalian carboxylesterase 1 enzymes can hydrolyze many xenobiotic chemicals and endogenous lipids. We here identified and characterized a mouse strain…”
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ABCB1 and ABCG2 Control Brain Accumulation and Intestinal Disposition of the Novel ROS1/TRK/ALK Inhibitor Repotrectinib, While OATP1A/1B, ABCG2, and CYP3A Limit Its Oral Availability by Li, Wenlong, Sparidans, Rolf W., Lebre, Maria C., Beijnen, Jos H., Schinkel, Alfred H.

“…Repotrectinib shows high activity against ROS1/TRK/ALK fusion-positive cancers in preclinical studies. We explored the roles of multidrug efflux transporters…”
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Drug Transporters ABCB1 (P-gp) and OATP, but not Drug-Metabolizing Enzyme CYP3A4, Affect the Pharmacokinetics of the Psychoactive Alkaloid Ibogaine and its Metabolites by F Martins, Margarida L, Heydari, Paniz, Li, Wenlong, Martínez-Chávez, Alejandra, Venekamp, Nikkie, Lebre, Maria C, Lucas, Luc, Beijnen, Jos H, Schinkel, Alfred H

“…The psychedelic alkaloid ibogaine is increasingly used as an oral treatment for substance use disorders, despite being unlicensed in most countries and having…”
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Why CCR2 and CCR5 blockade failed and why CCR1 blockade might still be effective in the treatment of rheumatoid arthritis by Lebre, Maria C, Vergunst, Clarissa E, Choi, Ivy Y K, Aarrass, Saïda, Oliveira, Ana S F, Wyant, Tim, Horuk, Richard, Reedquist, Kris A, Tak, Paul P

“…The aim of this study was to provide more insight into the question as to why blockade of CCR1, CCR2, and CCR5 may have failed in clinical trials in rheumatoid…”
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P-Glycoprotein (MDR1/ABCB1) Restricts Brain Accumulation of the Novel EGFR Inhibitor EAI045 and Oral Elacridar Coadministration Enhances Its Brain Accumulation and Oral Exposure by Wang, Jing, Susam, M. Merve, Gan, Changpei, Sparidans, Rolf W, Lebre, Maria C, Beijnen, Jos H, Schinkel, Alfred H

“…EAI045 is a fourth-generation allosteric tyrosine kinase inhibitor (TKI) of the epidermal growth factor receptor (EGFR). It targets T790M and C797S EGFR…”
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P-Glycoprotein (ABCB1/MDR1) and BCRP (ABCG2) Limit Brain Accumulation and Cytochrome P450-3A (CYP3A) Restricts Oral Exposure of the RET Inhibitor Selpercatinib (RETEVMO) by Wang, Yaogeng, Sparidans, Rolf W., Potters, Sander, Şentürk, Rahime, Lebre, Maria C., Beijnen, Jos H., Schinkel, Alfred H.

“…Selpercatinib is a targeted, FDA-approved, oral, small-molecule inhibitor for the treatment of rearranged during transfection (RET) proto-oncogene…”
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Carboxylesterase 1 family knockout alters drug disposition and lipid metabolism by Gan, Changpei, Wang, Jing, Martínez-Chávez, Alejandra, Hillebrand, Michel, de Vries, Niels, Beukers, Joke, Wagenaar, Els, Wang, Yaogeng, Lebre, Maria C., Rosing, Hilde, Klarenbeek, Sjoerd, Ali, Rahmen Bin, Pritchard, Colin, Huijbers, Ivo, Beijnen, Jos H., Schinkel, Alfred H.

“…The mammalian carboxylesterase 1 (Ces1/CES1) family comprises several enzymes that hydrolyze many xenobiotic chemicals and endogenous lipids. To investigate…”
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Impact of Adalimumab Treatment on Interleukin-17 and Interleukin-17 Receptor Expression in Skin and Synovium of Psoriatic Arthritis Patients with Mild Psoriasis by Bolt, Janne W, van Kuijk, Arno W, Teunissen, Marcel B M, van der Coelen, Dennis, Aarrass, Saïda, Gerlag, Daniëlle M, Tak, Paul P, van de Sande, Marleen G, Lebre, Maria C, van Baarsen, Lisa G M

“…Interleukin (IL)-17 and tumor necrosis factor-alpha (TNF)-α are key players in psoriatic arthritis (PsA) pathogenesis. While both cytokines can be…”
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Human organic anion transporting polypeptide (OATP) 1B3 and mouse OATP1A/1B affect liver accumulation of Ochratoxin A in mice by Wang, Jing, Gan, Changpei, Qi, Xiaozhe, Lebre, Maria C., Schinkel, Alfred H.

“…Ochratoxin A (OTA) is a dietary mycotoxin that can cause nephrotoxicity, hepatotoxicity, neurotoxicity and carcinogenicity. We found that in mice OTA is…”
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OATP1A/1B, CYP3A, ABCB1, and ABCG2 limit oral availability of the NTRK inhibitor larotrectinib, while ABCB1 and ABCG2 also restrict its brain accumulation by Wang, Yaogeng, Sparidans, Rolf W., Li, Wenlong, Lebre, Maria C., Beijnen, Jos H., Schinkel, Alfred H.

“…Background and Purpose Larotrectinib is a FDA‐approved oral small‐molecule inhibitor for treatment of neurotrophic tropomyosin receptor kinase fusion‐positive…”
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P-glycoprotein and breast cancer resistance protein restrict brigatinib brain accumulation and toxicity, and, alongside CYP3A, limit its oral availability by Li, Wenlong, Sparidans, Rolf W., Wang, Yaogeng, Lebre, Maria C., Beijnen, Jos H., Schinkel, Alfred H.

“…[Display omitted] Brigatinib is an FDA-approved oral anaplastic lymphoma kinase (ALK) inhibitor for treatment of metastatic non-small cell lung cancer (NSCLC)…”
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ABCB1 and ABCG2, but not CYP3A4 limit oral availability and brain accumulation of the RET inhibitor pralsetinib by Wang, Yaogeng, Sparidans, Rolf W., Potters, Sander, Lebre, Maria C., Beijnen, Jos H., Schinkel, Alfred H.

“…Pralsetinib is an FDA-approved oral small-molecule inhibitor for treatment of rearranged during transfection (RET) proto-oncogene fusion-positive non-small…”
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