Absolute Bioavailability, Mass Balance, and Metabolic Profiling Assessment of [14 C]-Belumosudil in Healthy Men: A Phase 1, Open-Label, 2-Part Study.
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DOI: 10.1002/cpdd.1085
Abstract: Belumosudil is a selective Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor. ROCK2 has been shown to drive proinflammatory response and fibrosis that occurs with chronic graft-versus-host disease; therefore, inhibition of ROCK2 has emerged as… read more here.
Keywords: balance metabolic; absolute bioavailability; part study; belumosudil ... See more keywords
A Phase 1 Study to Evaluate Absolute Bioavailability and Absorption, Distribution, Metabolism, and Excretion of Savolitinib in Healthy Male Volunteers
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DOI: 10.1002/cpdd.1224
Abstract: Savolitinib is an oral MET (hepatocyte growth factor receptor) tyrosine kinase inhibitor, with demonstrated preliminary efficacy in several cancer types. Previous pharmacokinetics assessments showed that savolitinib is rapidly absorbed but there are limited data on… read more here.
Keywords: metabolism; bioavailability; savolitinib; bioavailability absorption ... See more keywords
Absolute Bioavailability of Vemurafenib in Patients With BRAFV600 Mutation–Positive Malignancies
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DOI: 10.1002/cpdd.773
Abstract: Vemurafenib is a BRAF kinase inhibitor indicated for the treatment of patients with BRAFV600 mutation–positive unresectable or metastatic melanoma and Erdheim‐Chester disease. This phase 1, open‐label, single‐arm study was designed to estimate absolute bioavailability of… read more here.
Keywords: mutation positive; bioavailability; absolute bioavailability; patients brafv600 ... See more keywords
Absolute Bioavailability of Microdosed Midazolam After Buccal Administration Is Dependent on Buccal Exposure Time.
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DOI: 10.1002/jcph.1751
Abstract: Midazolam is an established probe drug to assess cytochrome P450 3A activity (phenotyping). Microdosed midazolam is increasingly used for this purpose; a buccal formulation might be of advantage, but buccal absorption might occur. We therefore… read more here.
Keywords: buccal exposure; exposure time; absolute bioavailability; bioavailability ... See more keywords
Determination of the absolute bioavailability of oral imatinib using a stable isotopically labeled intravenous imatinib-d8 microdose
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DOI: 10.1007/s00228-020-02888-y
Abstract: Purpose The aim of this study was to ascertain whether the absolute bioavailability of oral imatinib (Glivec®) during steady state plasma pharmacokinetics in cancer patients could be determined through a concomitant intravenous administration of a… read more here.
Keywords: stable isotopically; absolute bioavailability; bioavailability oral; imatinib ... See more keywords
Absolute Bioavailability of Esaxerenone and Food Effects on its Pharmacokinetics After a Single Oral Dose in Healthy Japanese Subjects: An Open-Label Crossover Study
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DOI: 10.1007/s12325-019-00956-z
Abstract: IntroductionTo investigate the absolute bioavailability of esaxerenone and the effects of food on its pharmacokinetics (PK) after a single oral dose in healthy Japanese subjects.MethodsTwenty-four Japanese males aged 20–45 years were randomised to six groups (each… read more here.
Keywords: esaxerenone; oral dose; absolute bioavailability; single oral ... See more keywords
Rilzabrutinib, a reversible covalent Bruton's tyrosine kinase inhibitor: Absorption, metabolism, excretion and absolute bioavailability in healthy participants.
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DOI: 10.1111/cts.13524
Abstract: This single-center, open-label, non-randomized, two-part, phase I study was conducted 1) to evaluate the absolute oral bioavailability of rilzabrutinib 400 mg tablet following an IV microtracer dose of ~100 μg [14C]-rilzabrutinib (~1 μCi) and single… read more here.
Keywords: rilzabrutinib; excretion; oral dose; absolute bioavailability ... See more keywords