Alpha 2.0
Login Register
» Authors » Maria C Lebre

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
1.
Intestinal human carboxylesterase 2 (CES2) expression rescues drug metabolism and most metabolic syndrome phenotypes in global Ces2 cluster knockout mice
Wang Y, Gan C, Beukers-Korver J, Rosing H, Li W, Wagenaar E, et al.
Acta Pharmacol Sin . 2024 Nov; 46(3):777-793. PMID: 39496863
Carboxylesterase 2 (CES2) is expressed mainly in liver and intestine, but most abundantly in intestine. It hydrolyzes carboxylester, thioester, and amide bonds in many exogenous and endogenous compounds, including lipids....
2.
Brain Exposure to the Macrocyclic ALK Inhibitor Zotizalkib is Restricted by ABCB1, and Its Plasma Disposition is Affected by Mouse Carboxylesterase 1c
Rijmers J, Sparidans R, Acda M, Loos N, Epeslidou E, Bui V, et al.
Mol Pharm . 2024 Sep; 21(10):5159-5170. PMID: 39312722
Zotizalkib (TPX-0131), a fourth-generation macrocyclic anaplastic lymphoma kinase (ALK) inhibitor, is designed to overcome resistance due to secondary ALK mutations in non-small cell lung cancer (NSCLC). We here evaluated the...
3.
The role of drug efflux and uptake transporters in the plasma pharmacokinetics and tissue disposition of morphine and its main metabolites
F Martins M, Heydari P, Li W, Martinez-Chavez A, El Yattouti M, Lebre M, et al.
Toxicol Appl Pharmacol . 2024 Jul; 490:117040. PMID: 39032800
Morphine is a widely used opioid for the treatment of pain. Differences in drug transporter expression and activity may contribute to variability in morphine pharmacokinetics and response. Using appropriate mouse...
4.
ABCB1 attenuates brain exposure to the KRAS inhibitor opnurasib whereas binding to mouse carboxylesterase 1c influences its plasma exposure
Rijmers J, Retmana I, Bui V, Arguedas D, Lebre M, Sparidans R, et al.
Biomed Pharmacother . 2024 May; 175:116720. PMID: 38733773
Opnurasib (JDQ443) is a newly developed oral KRAS inhibitor, with a binding mechanism distinct from the registered KRAS inhibitors sotorasib and adagrasib. Phase I and II clinical trials for opnurasib...
5.
Interplay of OATP1A/1B/2B1 uptake transporters and ABCB1 and ABCG2 efflux transporters in the handling of bilirubin and drugs
Li W, Sparidans R, Wang Y, F Martins M, de Waart D, van Tellingen O, et al.
Biomed Pharmacother . 2024 May; 175:116644. PMID: 38692057
Transmembrane drug transporters can be important determinants of the pharmacokinetics, efficacy, and safety profiles of drugs. To investigate the potential cooperative and/or counteracting interplay of OATP1A/1B/2B1 uptake transporters and ABCB1...
6.
The ABCB1 and ABCG2 efflux transporters limit brain disposition of the SYK inhibitors entospletinib and lanraplenib
Loos N, Sparidans R, Heydari P, Bui V, Lebre M, Beijnen J, et al.
Toxicol Appl Pharmacol . 2024 Mar; 485:116911. PMID: 38527694
The highly selective Spleen Tyrosine Kinase (SYK) inhibitors entospletinib and lanraplenib disrupt kinase activity and inhibit immune cell functions. They are developed for treatment of B-cell malignancies and autoimmunity diseases....
7.
Impact of loperamide on the pharmacokinetics and tissue disposition of ritonavir-boosted oral docetaxel therapy; a preclinical assessment
Loos N, Bui V, de Jong D, Lebre M, Rosing H, Beijnen J, et al.
Cancer Chemother Pharmacol . 2024 Mar; 94(1):79-87. PMID: 38456955
Purpose: An oral docetaxel formulation boosted by the Cytochrome P450 (CYP) 3 A inhibitor ritonavir, ModraDoc006/r, is currently under clinical investigation. Based on clinical data, the incidence of grade 1-2...
8.
Interplay of Ritonavir-Boosted Oral Cabazitaxel with the Organic Anion-Transporting Polypeptide (OATP) Uptake Transporters and Carboxylesterase 1 in Mice
Loos N, Ferreira Martins M, Rijmers J, de Jong D, Lebre M, Tibben M, et al.
Mol Pharm . 2024 Feb; 21(4):1952-1964. PMID: 38423793
Intravenously administered chemotherapeutic cabazitaxel is used for palliative treatment of prostate cancer. An oral formulation would be more patient-friendly and reduce the need for hospitalization. We therefore study determinants of...
9.
Coadministration of ABCB1/P-glycoprotein inhibitor elacridar improves tissue distribution of ritonavir-boosted oral cabazitaxel in mice
Loos N, F Martins M, de Jong D, Lebre M, Tibben M, Beijnen J, et al.
Int J Pharm . 2023 Dec; 650:123708. PMID: 38135258
Developing an oral formulation for the chemotherapeutic cabazitaxel might improve its patient-friendliness, costs, and potentially exposure profile. Cabazitaxel oral availability is restricted by CYP3A-mediated first-pass metabolism, but can be substantially...
10.
Pharmacokinetics of the KRAS inhibitor adagrasib is limited by CYP3A and ABCB1, and influenced by binding to mouse plasma carboxylesterase 1c
Loos N, Retmana I, Rijmers J, Wang Y, Gan C, Lebre M, et al.
Biomed Pharmacother . 2023 Aug; 166:115304. PMID: 37586117
Adagrasib (Krazati™) is the second FDA-approved specific KRAS inhibitor for non-small cell lung cancer (NSCLC) patients harboring this mutation. The impact of the drug efflux transporters ABCB1 and ABCG2, and...