Rolf Grempler
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View article: Absorption, Metabolism, Distribution and Excretion (ADME) and Absolute Bioavailability Assessment of Zongertinib in Healthy Male Volunteers
Absorption, Metabolism, Distribution and Excretion (ADME) and Absolute Bioavailability Assessment of Zongertinib in Healthy Male Volunteers Open
Registered under identifier NCT05879991 (25 May 2023).
View article: Relative Bioavailability of Zongertinib, an Orally Administered HER2-Selective Tyrosine Kinase Inhibitor, under Fed and Fasted Conditions in Healthy Male Participants: Results from Two Randomized, Open-Label, Crossover Studies
Relative Bioavailability of Zongertinib, an Orally Administered HER2-Selective Tyrosine Kinase Inhibitor, under Fed and Fasted Conditions in Healthy Male Participants: Results from Two Randomized, Open-Label, Crossover Studies Open
Human epidermal growth factor receptor 2 (HER2), also known as ErbB2, is mutated in various solid tumors. Zongertinib (BI 1810631) is a novel, orally administered, HER2-specific tyrosine kinase inhibitor that spares the epidermal growth fa…
View article: The effect of carbamazepine, a strong <scp>CYP3A</scp> inducer, on the pharmacokinetics of zongertinib in healthy male volunteers
The effect of carbamazepine, a strong <span>CYP3A</span> inducer, on the pharmacokinetics of zongertinib in healthy male volunteers Open
Introduction Zongertinib (BI 1810631) is a potent, selective, and epidermal growth factor receptor (EGFR) wild‐type sparing human epidermal growth factor receptor 2 (HER2) inhibitor. Based on in vitro data, the oxidative hepatic metabolism…
View article: Table S6 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S6 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
IC50 in mouse cell lines with different TP53 status.
View article: Table S12 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S12 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Preliminary human PK parameters of brigimadlin.
View article: Table S13 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S13 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Total and unbound brigimadlin in humans and Crl:CD1(ICR) mice.
View article: Table S4 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S4 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
In vitro IC50 (AlphaScreen and CTG cell viability assay) of BI-0252, BI-0282, and brigimadlin
View article: Table S11 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S11 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Brigimadlin PK parameters in SJSA-1 osteosarcoma MDM2-amplified xenograft model.
View article: Data from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Data from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
p53 is known as the guardian of the genome and is one of the most important tumor suppressors. It is inactivated in most tumors, either via tumor protein p53 (TP53) gene mutation or copy number amplification of key negative regulato…
View article: Table S2 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S2 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Antibodies used for Western blot analysis.
View article: Figure S2 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Figure S2 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Dose-dependent regulation of p53 target genes in MDM2-amplified and non-amplified solid tumor cell lines with brigimadlin, alrizomadlin, and milademetan.
View article: Table S3 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S3 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
TaqMan primer and probe sets used for RT-PCR.
View article: Table S10 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S10 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Summary of brigimadlin protein binding in plasma of different species.
View article: Table S9 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S9 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Brigimadlin in vitro activity in normal cell lines.
View article: Supplementary Methods from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Supplementary Methods from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Supplementary Methods and Appendix
View article: Figure S5 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Figure S5 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Modulation of p53 target genes in LU0861 tumor-bearing mice treated with brigimadlin.
View article: Table S7 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S7 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
MDM2 mRNA expression, copy number and brigimadlin in vitro activity in MDM2-amplified cell lines versus MDM2 non-amplified cell lines.
View article: Figure S4 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Figure S4 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
In vitro activity of brigimadlin in normal cells.
View article: Table S8 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S8 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
In vitro activity of MDM2–p53 antagonists brigimadlin, alrizomadlin and milademetan in MDM2-amplified cell lines and MDM2 non-amplified cell lines.
View article: Table S5 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S5 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Permeability and solubility of brigimadlin.
View article: Figure S3 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Figure S3 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Brigimadlin treatment leads to accumulation of p53 in the nucleus.
View article: Figure S1 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Figure S1 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Brigimadlin dose-dependent regulation of p53 target genes and apoptosis in MDM2-amplified and non-amplified solid tumor cell lines.
View article: Figure S6 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Figure S6 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Preliminary mean serum GDF15 absolute change from baseline (pg/mL) vs. planned time [h] after administration of 45 mg on Day 1 in Cycle 1 of a Q3W schedule in patients with cancer (n = 27).
View article: Table S1 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Table S1 from Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
Cell Lines.
View article: Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules
Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2–p53 Antagonist Suitable for Intermittent Dose Schedules Open
p53 is known as the guardian of the genome and is one of the most important tumor suppressors. It is inactivated in most tumors, either via tumor protein p53 (TP53) gene mutation or copy number amplification of key negative regulators, e.g…
View article: Genetic analysis of blood molecular phenotypes reveals common properties in the regulatory networks affecting complex traits
Genetic analysis of blood molecular phenotypes reveals common properties in the regulatory networks affecting complex traits Open
View article: Author Correction: Discovery of drug–omics associations in type 2 diabetes with generative deep-learning models
Author Correction: Discovery of drug–omics associations in type 2 diabetes with generative deep-learning models Open
View article: Trends in industrialization of biotherapeutics: a survey of product characteristics of 89 antibody-based biotherapeutics
Trends in industrialization of biotherapeutics: a survey of product characteristics of 89 antibody-based biotherapeutics Open
There is considerable interest in the pharmaceutical industry toward development of antibody-based biotherapeutics because they can selectively bind diverse receptors and often possess desirable pharmacology. Here, we studied product chara…
View article: 89Zr-immuno-PET using the anti-LAG-3 tracer [89Zr]Zr-BI 754111: demonstrating target specific binding in NSCLC and HNSCC
89Zr-immuno-PET using the anti-LAG-3 tracer [89Zr]Zr-BI 754111: demonstrating target specific binding in NSCLC and HNSCC Open
Purpose Although lymphocyte activation gene-3 (LAG-3) directed therapies demonstrate promising clinical anti-cancer activity, only a subset of patients seems to benefit and predictive biomarkers are lacking. Here, we explored the potential…
View article: Discovery of drug–omics associations in type 2 diabetes with generative deep-learning models
Discovery of drug–omics associations in type 2 diabetes with generative deep-learning models Open
The application of multiple omics technologies in biomedical cohorts has the potential to reveal patient-level disease characteristics and individualized response to treatment. However, the scale and heterogeneous nature of multi-modal dat…