Publications

Pharmacological research

Daraxonrasib (RMC-6236) pharmacokinetics: impact of transporters and drug-metabolizing enzymes on a first-in-class pan-RAS molecular glue.

01-07-2026

Acta pharmaceutica Sinica. B

Resistance mutations and the blood-brain barrier: Key challenges in targeted treatment of brain metastatic non-small cell lung cancer.

01-08-2025

Acta pharmacologica Sinica

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

01-03-2025

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

Investigational new drugs

Extrahepatic metabolism of ibrutinib.

01-02-2021

Key Publication

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

Daraxonrasib (RMC-6236) pharmacokinetics: impact of transporters and drug-metabolizing enzymes on a first-in-class pan-RAS molecular glue.

Resistance mutations and the blood-brain barrier: Key challenges in targeted treatment of brain metastatic non-small cell lung cancer.

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

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

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

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

ABCB1 attenuates brain exposure to the KRASG12C inhibitor opnurasib whereas binding to mouse carboxylesterase 1c influences its plasma exposure.

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

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

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

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

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

Development and validation of an LC-MS/MS method for the quantification of KRASG12C inhibitor opnurasib in several mouse matrices and its application in a pharmacokinetic mouse study.

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

Validated LC-MS/MS method for simultaneous quantification of KRASG12C inhibitor sotorasib and its major circulating metabolite (M24) in mouse matrices and its application in a mouse pharmacokinetic study.

Pharmacokinetics of the KRASG12C inhibitor adagrasib is limited by CYP3A and ABCB1, and influenced by binding to mouse plasma carboxylesterase 1c.

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

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

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

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

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

Carboxylesterase 1 family knockout alters drug disposition and lipid metabolism.

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.

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

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

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

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

ABCB1 limits brain exposure of the KRASG12C inhibitor sotorasib, whereas ABCB1, CYP3A, and possibly OATP1a/1b restrict its oral availability.

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

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

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

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

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

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

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

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.

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

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

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

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

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

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

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.

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.

Extrahepatic metabolism of ibrutinib.

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

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.

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

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

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

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

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.

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.

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

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