Publications

Investigational new drugs

Extrahepatic metabolism of ibrutinib.

01-02-2021

Key

Cancer research

A mutation hot spot in the Bcrp1 (Abcg2) multidrug transporter in mouse cell lines selected for Doxorubicin resistance.

15-04-2002

Key

Acta pharmacologica Sinica

Intestinal human carboxylesterase 2 (CES2) expression rescues drug metabolism and most metabolic syndrome phenotypes in global Ces2 cluster knockout mice.

04-11-2024

Molecular pharmaceutics

Brain Exposure to the Macrocyclic ALK Inhibitor Zotizalkib is Restricted by ABCB1, and Its Plasma Disposition is Affected by Mouse Carboxylesterase 1c.

07-10-2024

Toxicology and applied pharmacology

The role of drug efflux and uptake transporters in the plasma pharmacokinetics and tissue disposition of morphine and its main metabolites.

01-09-2024

Cancer chemotherapy and pharmacology

Impact of loperamide on the pharmacokinetics and tissue disposition of ritonavir-boosted oral docetaxel therapy; a preclinical assessment.

01-07-2024

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

ABCB1 attenuates brain exposure to the KRAS^G12C inhibitor opnurasib whereas binding to mouse carboxylesterase 1c influences its plasma exposure.

01-06-2024

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

Interplay of OATP1A/1B/2B1 uptake transporters and ABCB1 and ABCG2 efflux transporters in the handling of bilirubin and drugs.

01-06-2024

Molecular pharmaceutics

Interplay of Ritonavir-Boosted Oral Cabazitaxel with the Organic Anion-Transporting Polypeptide (OATP) Uptake Transporters and Carboxylesterase 1 in Mice.

01-04-2024

Toxicology and applied pharmacology

The ABCB1 and ABCG2 efflux transporters limit brain disposition of the SYK inhibitors entospletinib and lanraplenib.

01-04-2024

International journal of pharmaceutics

Coadministration of ABCB1/P-glycoprotein inhibitor elacridar improves tissue distribution of ritonavir-boosted oral cabazitaxel in mice.

25-01-2024

Clinical and translational science

Predictability of human exposure by human-CYP3A4-transgenic mouse models: A meta-analysis.

01-01-2024

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences

Development and validation of an LC-MS/MS method for the quantification of KRAS^G12C inhibitor opnurasib in several mouse matrices and its application in a pharmacokinetic mouse study.

01-01-2024

Biomedical chromatography : BMC

Development and validation of an HPLC-MS/MS method to quantify the KRAS inhibitor adagrasib in mouse plasma and tissue-related matrices.

01-11-2023

Journal of pharmaceutical and biomedical analysis

Validated LC-MS/MS method for simultaneous quantification of KRAS^G12C inhibitor sotorasib and its major circulating metabolite (M24) in mouse matrices and its application in a mouse pharmacokinetic study.

25-10-2023

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

Pharmacokinetics of the KRAS^G12C inhibitor adagrasib is limited by CYP3A and ABCB1, and influenced by binding to mouse plasma carboxylesterase 1c.

01-10-2023

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

Natural deletion of mouse carboxylesterases Ces1c/d/e impacts drug metabolism and metabolic syndrome development.

01-08-2023

Pharmaceutical research

P-glycoprotein (MDR1/ABCB1) Restricts Brain Penetration of the Main Active Heroin Metabolites 6-monoacetylmorphine (6-MAM) and Morphine in Mice.

01-08-2023

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

The inhibitory and inducing effects of ritonavir on hepatic and intestinal CYP3A and other drug-handling proteins.

01-06-2023

Molecular pharmaceutics

Enhancement of the Oral Availability of Cabazitaxel Using the Cytochrome P450 3A (CYP3A) Inhibitor Ritonavir in Mice.

01-05-2023

Pharmacological research

Organic anion-transporting polypeptide 2B1 knockout and humanized mice; insights into the handling of bilirubin and drugs.

01-04-2023

Acta pharmaceutica Sinica. B

Carboxylesterase 1 family knockout alters drug disposition and lipid metabolism.

01-02-2023

Biomedical chromatography : BMC

Bioanalytical assay for the quantification of the tyrosine kinase inhibitor EAI045 and its major metabolite PIA in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry.

01-11-2022

Pharmaceuticals (Basel, Switzerland)

P-Glycoprotein (MDR1/ABCB1) Restricts Brain Accumulation of the Novel EGFR Inhibitor EAI045 and Oral Elacridar Coadministration Enhances Its Brain Accumulation and Oral Exposure.

08-09-2022

International journal of molecular sciences

The Mechanism-Based Inactivation of CYP3A4 by Ritonavir: What Mechanism?

30-08-2022

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

ABCB1 restricts brain accumulation of the novel RORγ agonist cintirorgon, while OATP1A/1B and CYP3A limit its oral availability.

01-08-2022

Pharmaceuticals (Basel, Switzerland)

Predictiveness of the Human-CYP3A4-Transgenic Mouse Model (Cyp3aXAV) for Human Drug Exposure of CYP3A4-Metabolized Drugs.

13-07-2022

Pharmacological research

ABCB1 limits brain exposure of the KRAS^G12C inhibitor sotorasib, whereas ABCB1, CYP3A, and possibly OATP1a/1b restrict its oral availability.

01-04-2022

Pharmacological research

ABCB1 and ABCG2 limit brain penetration and, together with CYP3A4, total plasma exposure of abemaciclib and its active metabolites.

01-04-2022

Frontiers in pharmacology

Drug Transporters ABCB1 (P-gp) and OATP, but not Drug-Metabolizing Enzyme CYP3A4, Affect the Pharmacokinetics of the Psychoactive Alkaloid Ibogaine and its Metabolites.

22-03-2022

Journal of pharmaceutical sciences

Population Pharmacokinetic Modelling to Support the Evaluation of Preclinical Pharmacokinetic Experiments with Lorlatinib.

01-02-2022

Journal of pharmaceutical and biomedical analysis

Development and validation of an LC-MS/MS assay for the quantification of cintirorgon (LYC-55716) in mouse plasma and tissue homogenates.

05-01-2022

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

Rifampin and ritonavir increase oral availability and elacridar enhances overall exposure and brain accumulation of the NTRK inhibitor larotrectinib.

01-01-2022

Molecular pharmaceutics

P-Glycoprotein (ABCB1/MDR1) Controls Brain Penetration and Intestinal Disposition of the PARP1/2 Inhibitor Niraparib.

06-12-2021

Pharmaceuticals (Basel, Switzerland)

P-Glycoprotein (ABCB1/MDR1) and BCRP (ABCG2) Limit Brain Accumulation and Cytochrome P450-3A (CYP3A) Restricts Oral Exposure of the RET Inhibitor Selpercatinib (RETEVMO).

27-10-2021

Pharmaceutics

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.

21-10-2021

Drug and alcohol dependence

The suitability of oral diacetylmorphine in treatment-refractory patients with heroin dependence: A scoping review.

01-10-2021

Pharmacological research

ABCB1 and ABCG2, but not CYP3A4 limit oral availability and brain accumulation of the RET inhibitor pralsetinib.

01-10-2021

Journal of pharmaceutical and biomedical analysis

Simultaneous quantification of abemaciclib and its active metabolites in human and mouse plasma by UHPLC-MS/MS.

05-09-2021

Cancer chemotherapy and pharmacology

Pharmacokinetics of docetaxel and ritonavir after oral administration of ModraDoc006/r in patients with prostate cancer versus patients with other advanced solid tumours.

01-06-2021

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences

Quantification of KRAS inhibitor sotorasib in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry.

01-06-2021

Molecular cancer therapeutics

ABCB1 and ABCG2 Restrict Brain and Testis Accumulation and, Alongside CYP3A, Limit Oral Availability of the Novel TRK Inhibitor Selitrectinib.

01-06-2021

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

The role of drug efflux and uptake transporters ABCB1 (P-gp), ABCG2 (BCRP) and OATP1A/1B and of CYP3A4 in the pharmacokinetics of the CDK inhibitor milciclib.

01-04-2021

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences

Development and validation of a UPLC-MS/MS method with a broad linear dynamic range for the quantification of morphine, morphine-3-glucuronide and morphine-6-glucuronide in mouse plasma and tissue homogenates.

01-03-2021

Clinical pharmacokinetics

Clinical Pharmacokinetics and Pharmacodynamics of the Cyclin-Dependent Kinase 4 and 6 Inhibitors Palbociclib, Ribociclib, and Abemaciclib.

01-12-2020

Journal of pharmaceutical and biomedical analysis

Development and validation of an LC-MS/MS method for the quantitative analysis of milciclib in human and mouse plasma, mouse tissue homogenates and tissue culture medium.

25-10-2020

Toxicology and applied pharmacology

Human organic anion transporting polypeptide (OATP) 1B3 and mouse OATP1A/1B affect liver accumulation of Ochratoxin A in mice.

15-08-2020

Pharmacology research & perspectives

No relation between docetaxel administration route and high-grade diarrhea incidence.

01-08-2020

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences

Bioanalytical method for the simultaneous quantification of irinotecan and its active metabolite SN-38 in mouse plasma and tissue homogenates using HPLC-fluorescence.

15-07-2020

British journal of pharmacology

OATP1A/1B, CYP3A, ABCB1, and ABCG2 limit oral availability of the NTRK inhibitor larotrectinib, while ABCB1 and ABCG2 also restrict its brain accumulation.

01-07-2020