ASPET

SEPTEMBER 16, 2024

GBM has a poor prognosis despite aggressive treatment, in part due to lack of adequate drug permeability at the BBB. CNS distribution of elimusertib is partially limited by P-gp efflux at the BBB, and high binding to CNS tissues leads to low levels of pharmacologically active (unbound) drug in the brain.

Pharmacogenetics 100

Pharmacogenetics DNA Pharmacokinetics Treatment 100

ASPET

JUNE 10, 2024

Radiation therapy, a standard treatment option for many cancer patients, induces DNA double strand breaks (DSBs), leading to cell death. Efficacy of radiosensitizers for brain tumors may be influenced by a lack of effective drug delivery across the blood-brain barrier (BBB).

Pharmacokinetics 100

Pharmacokinetics Pharmacogenetics Treatment DNA 100

ASPET

FEBRUARY 26, 2024

Panobinostat is a potent pan-HDAC inhibitor that has been tested in multiple studies for the treatment of brain tumors. There have been contrasting views surrounding its efficacy for the treatment of tumors in the CNS following systemic administration when examined in different models or species.

Metabolic Stability 100

Metabolic Stability Pharmacokinetics Pharmacogenetics Treatment 100

ASPET

MARCH 6, 2024

A first pharmacological phenotyping with the OATP2B1 substrate-drug atorvastatin revealed reduced hepatic content and increased expression of rCYP3A1 in the humanized animals. The contrary was observed, when microsomes isolated from treatment naive animals were assessed for the OSI-420 formation after erlotinib exposure.

Protein Expression 100

Protein Expression Pharmacogenetics Treatment Drugs 100

The Open Targets Blog

NOVEMBER 30, 2023

Target prioritisation A major new feature of this release is the Target Prioritisation view, which provides an assessment of target-specific properties of interest when evaluating the suitability of a target for a drug discovery programme. It is presented here with an additional layer of analysis with a drug discovery focus.

Pharmacogenetics 59

Pharmacogenetics Small Molecule Disease Drugs 59