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

ASPET

Panobinostat also showed inter-strain and inter-species differences in the in vitro plasma stability; and was stable in human plasma. Importantly, the plasma stability in various mouse strains was not reflected in the in vivo systemic pharmacokinetic behavior of panobinostat.

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Effect of ophiopogonin D on the pharmacokinetics and transport of cryptotanshinone during their co?administration and the potential mechanism

Chemical Biology and Drug Design

The co-administration of cryptotanshinone with ophiopogonin D induced pharmacokinetic interaction prolonging the systemic exposure and improving metabolic stability of cryptotanshinone. The Caco-2 cells were employed to evaluate the transport of cryptotanshinone, and the metabolic stability was studied in the rat liver microsomes.

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Targeted modification of furan?2?carboxaldehydes into Michael acceptor analogs yielded long?acting hemoglobin modulators with dual antisickling activities

Chemical Biology and Drug Design

However, the aldehyde functional group metabolic instability has severly hampered their development, except for voxelotor, which was approved in 2019 for SCD treatment.

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Evaluation of Systemic and Brain Pharmacokinetic Parameters for Repurposing Metformin Using Intravenous Bolus Administration [Drug Discovery and Translational Medicine]

ASPET

In vitro assays examined brain tissue binding and metabolic stability. The findings highlight metformin's rapid brain entry, minimal binding, and metabolic stability. An LC-MS/MS method to measure metformin levels in plasma, brain, and cerebrospinal fluid (CSF) was developed and validated.

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Covalent Stapling of the Cereblon Sensor Loop Histidine Using Sulfur-Heterocycle Exchange

Covalent Modifiers

Attenuation of intrinsic reactivity through the development of sulfonyl pyrazoles, imidazoles, and nucleobases enhanced plasma stability, and several compounds retained efficient labeling of His353.

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MetID Guided Drug Design

Metabolite Tales Blog

To curb O -glucuronidation at that position, a gem-dimethyl group was incorporated, which not only boosted metabolic stability but also resulted in increased potency of “compound 17” An earlier example of how to manage glucuronidation by steric hindrance is illustrated in “compound 25” in the paper by Zhang et al.,

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Pantothenate kinase activation restores brain coenzyme A in a mouse model of pantothenate kinase associated neurodegeneration [Drug Discovery and Translational Medicine]

ASPET

The metabolic stability, protein binding and membrane permeability of BBP-671 all suggest it has the physical properties required to cross the blood brain barrier. BBP-671 was detected in plasma, liver, cerebrospinal fluid and brain following oral administration in rodents demonstrating the ability of BBP-671 to penetrate the brain.