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Maria C Lebre

Explore the profile of Maria C Lebre including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 48
Citations 654
Followers 0
Related Specialties
Pharmacology
Chemistry
General Medicine
Top 10 Co-Authors
Alfred H Schinkel
Jos H Beijnen
Rolf W Sparidans
Wenlong Li
Yaogeng Wang
Nancy H C Loos
Margarida L F Martins
Hilde Rosing
Paul P Tak
Jing Wang
Published In
Pharmacol Res
Mol Pharm
Int J Pharm
Biomed Pharmacother
Arthritis Res Ther
Affiliations
Soon will be listed here.
Recent Articles
11.
P-glycoprotein (MDR1/ABCB1) Restricts Brain Penetration of the Main Active Heroin Metabolites 6-monoacetylmorphine (6-MAM) and Morphine in Mice
F Martins M, Loos N, El Yattouti M, Offeringa L, Heydari P, Hillebrand M, et al.
Pharm Res . 2023 Jun; 40(8):1885-1899. PMID: 37344602
Background & Purpose: Heroin (diacetylmorphine; diamorphine) is a highly addictive opioid prodrug. Heroin prescription is possible in some countries for chronic, treatment-refractory opioid-dependent patients and as a potent analgesic for...
12.
Natural deletion of mouse carboxylesterases Ces1c/d/e impacts drug metabolism and metabolic syndrome development
Gan C, Wang J, Wang Y, Martinez-Chavez A, Hillebrand M, de Vries N, et al.
Biomed Pharmacother . 2023 Jun; 164:114956. PMID: 37267638
Mammalian carboxylesterase 1 enzymes can hydrolyze many xenobiotic chemicals and endogenous lipids. We here identified and characterized a mouse strain (FVB/NKI) in which three of the eight Ces1 genes were...
13.
Enhancement of the Oral Availability of Cabazitaxel Using the Cytochrome P450 3A (CYP3A) Inhibitor Ritonavir in Mice
Loos N, F Martins M, de Jong D, Lebre M, Tibben M, Beijnen J, et al.
Mol Pharm . 2023 Mar; 20(5):2477-2489. PMID: 36976574
There is currently great interest in developing oral taxanes due to their lower costs and greater patient friendliness. We here wanted to test whether oral ritonavir, a cytochrome P450 3A...
14.
Organic anion-transporting polypeptide 2B1 knockout and humanized mice; insights into the handling of bilirubin and drugs
Li W, Iusuf D, Sparidans R, Wagenaar E, Wang Y, de Waart D, et al.
Pharmacol Res . 2023 Mar; 190:106724. PMID: 36907287
Organic anion transporting polypeptide 2B1 (OATP2B1/SLCO2B1) facilitates uptake transport of structurally diverse endogenous and exogenous compounds. To investigate the roles of OATP2B1 in physiology and pharmacology, we established and characterized...
15.
Carboxylesterase 1 family knockout alters drug disposition and lipid metabolism
Gan C, Wang J, Martinez-Chavez A, Hillebrand M, de Vries N, Beukers J, et al.
Acta Pharm Sin B . 2023 Mar; 13(2):618-631. PMID: 36873183
The mammalian carboxylesterase 1 (Ces1/CES1) family comprises several enzymes that hydrolyze many xenobiotic chemicals and endogenous lipids. To investigate the pharmacological and physiological roles of Ces1/CES1, we generated cluster knockout...
16.
P-Glycoprotein (MDR1/ABCB1) Restricts Brain Accumulation of the Novel EGFR Inhibitor EAI045 and Oral Elacridar Coadministration Enhances Its Brain Accumulation and Oral Exposure
Wang J, Susam M, Gan C, Sparidans R, Lebre M, Beijnen J, et al.
Pharmaceuticals (Basel) . 2022 Sep; 15(9). PMID: 36145346
EAI045 is a fourth-generation allosteric tyrosine kinase inhibitor (TKI) of the epidermal growth factor receptor (EGFR). It targets T790M and C797S EGFR mutants in the treatment of non-small cell lung...
17.
ABCB1 restricts brain accumulation of the novel RORγ agonist cintirorgon, while OATP1A/1B and CYP3A limit its oral availability
Li W, Lehutova D, Sparidans R, Heydari P, Wang J, Lebre M, et al.
Eur J Pharm Biopharm . 2022 Jun; 177:135-146. PMID: 35772614
Cintirorgon (LYC-55716), a first-in-class, small-molecule, oral selective RORγ agonist, has been developed as a new immuno-oncology drug for solid tumors. We here studied the functions of the ABCB1 and ABCG2...
18.
Drug Transporters ABCB1 (P-gp) and OATP, but not Drug-Metabolizing Enzyme CYP3A4, Affect the Pharmacokinetics of the Psychoactive Alkaloid Ibogaine and its Metabolites
F Martins M, Heydari P, Li W, Martinez-Chavez A, Venekamp N, Lebre M, et al.
Front Pharmacol . 2022 Mar; 13:855000. PMID: 35308219
The psychedelic alkaloid ibogaine is increasingly used as an oral treatment for substance use disorders, despite being unlicensed in most countries and having reported adverse events. Using wild-type and genetically...
19.
Impact of Adalimumab Treatment on Interleukin-17 and Interleukin-17 Receptor Expression in Skin and Synovium of Psoriatic Arthritis Patients with Mild Psoriasis
Bolt J, van Kuijk A, Teunissen M, van der Coelen D, Aarrass S, Gerlag D, et al.
Biomedicines . 2022 Feb; 10(2). PMID: 35203534
Interleukin (IL)-17 and tumor necrosis factor-alpha (TNF)-α are key players in psoriatic arthritis (PsA) pathogenesis. While both cytokines can be therapeutically targeted with beneficial clinical outcome, it is unclear whether...
20.
ABCB1 limits brain exposure of the KRAS inhibitor sotorasib, whereas ABCB1, CYP3A, and possibly OATP1a/1b restrict its oral availability
Loos N, Retmana I, Li W, F Martins M, Lebre M, Sparidans R, et al.
Pharmacol Res . 2022 Feb; 178:106137. PMID: 35192958
Sotorasib (Lumakras™) is the first FDA-approved KRAS inhibitor for treatment of patients with non-small cell lung cancer (NSCLC) carrying this mutation. Using genetically modified mouse models, we studied the influence...