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Preclinical systemic pharmacokinetics, dose-proportionality, and CNS distribution of the ATM inhibitor WSD0628, a novel radiosensitizer for the treatment of brain tumors [Metabolism, Transport, and Pharmacogenetics]

ASPET

Radiation therapy, a standard treatment option for many cancer patients, induces DNA double strand breaks (DSBs), leading to cell death. This approach will provide critical insights for the clinical translation of WSD0628 for the treatment of primary and secondary brain tumors.

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Factors influencing the Central Nervous System (CNS) distribution of the ATR inhibitor elimusertib (BAY1895344): Implications for the treatment of CNS tumors [Metabolism, Transport, and Pharmacogenetics]

ASPET

GBM has a poor prognosis despite aggressive treatment, in part due to lack of adequate drug permeability at the BBB. Acknowledging the potential for inter-species differences in pharmacokinetics, these data suggest that clinical translation of elimusertib in combination with temozolomide for treatment of GBM may be limited.

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Pharmacokinetics of panobinostat: Inter-species difference in metabolic stability [Metabolism, Transport, and Pharmacogenetics]

ASPET

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.

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CNS distribution of panobinostat in preclinical models to guide dosing for pediatric brain tumors [Metabolism, Transport, and Pharmacogenetics]

ASPET

Panobinostat is a nonselective pan-HDAC inhibitor that is being tested in pre-clinical and clinical studies, including for the treatment of pediatric medulloblastoma, which has a propensity for leptomeningeal spread, and diffuse midline glioma (DMG), which can infiltrate into supratentorial brain regions.

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Humanization of SLCO2B1 in rats increases rCYP3A1 protein expression but not the metabolism of erlotinib to OSI-420 [Metabolism, Transport, and Pharmacogenetics]

ASPET

The contrary was observed, when microsomes isolated from treatment naive animals were assessed for the OSI-420 formation after erlotinib exposure. Microsomes isolated from the treated animals were characterized for CYP3A activity using testosterone, showing higher activity in the knock-in rats.

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Open Targets Platform 23.12 has been released!

The Open Targets Blog

Introducing pharmacogenetics data to the Platform This release introduces a new datasource to the Platform: the pharmacogenetics widget will incorporate data about the impact of human genetic variation on drug responses. You can find this data on the target and drug profile pages.

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Diaceutics Launches World’s First Diagnostic Network for Precision Medicine to Solve Global Cancer Testing Issues

The Pharma Data

Collaborators today include Synlab, PathGroup (US), SRL Diagnostics (Asia), Fundación Jimenez Díaz, The Royal Marsden NHS Foundation Trust, Istituto Nazionale Tumori Regina Elena Roma and Diatech Pharmacogenetics (EU). There is a better way to get every patient the treatment they deserve. We believe that DXRX is that way.