Effects of Hepatic Impairment on the Pharmacokinetic Profile and Safety of Lobeglitazone
Sign Up to like & getrecommendations! Published in 2022 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.1045
Abstract: In this open‐label, single‐dose, parallel‐group study, we compared the pharmacokinetic profile and safety of lobeglitazone, a thiazolidinedione acting as an agonist for peroxisome proliferator‐activated receptors, in patients with hepatic impairment (HI) and healthy matched controls… read more here.
Keywords: profile safety; safety lobeglitazone; lobeglitazone; pharmacokinetic profile ... See more keywords
Pharmacokinetic Interactions Between Gemigliptin and Metformin, and Potential Differences in the Pharmacokinetic Profile of Gemigliptin Between the Mexican and Korean Populations: A Randomized, Open-label Study in Healthy Mexican Volunteers.
Sign Up to like & getrecommendations! Published in 2018 at "Clinical therapeutics"
DOI: 10.1016/j.clinthera.2018.08.015
Abstract: PURPOSE The aim of this study was to assess the pharmacokinetic interactions between a newly developed dipeptidyl peptidase (DPP)-4 inhibitor, gemigliptin, and metformin in healthy Mexican male volunteers, and the differences in the pharmacokinetic profile… read more here.
Keywords: gemigliptin metformin; pharmacokinetic profile; gemigliptin; profile gemigliptin ... See more keywords
Pharmacokinetic profile and oral bioavailability of Kaurenoic acid from Copaifera spp. in rats.
Sign Up to like & getrecommendations! Published in 2018 at "Fitoterapia"
DOI: 10.1016/j.fitote.2018.05.013
Abstract: Kaurenoic acid (KA) is a kaurane diterpene found in several medicinal plants that displays biological activities, such as anti-inflammatory, smooth muscle relaxant and hypotensive response. However, there are no pharmacokinetic data available about this molecule.… read more here.
Keywords: oral bioavailability; bioavailability; pharmacokinetic profile; profile oral ... See more keywords
Pharmacokinetic Profile of Twice- and Once-daily Tacrolimus in Pediatric Kidney Transplant Recipients.
Sign Up to like & getrecommendations! Published in 2017 at "Transplantation proceedings"
DOI: 10.1016/j.transproceed.2016.11.022
Abstract: BACKGROUND The aim of this study was to assess the differences in pharmacokinetic (PK) profiles after the 1:1 ratio-based conversion from a twice-daily to a once-daily tacrolimus formulation (TD-TAC and OD-TAC, respectively) in pediatric recipients… read more here.
Keywords: tac; daily tacrolimus; tac tac; twice daily ... See more keywords
2-Deoxyglycoside conjugates of lupane triterpenoids with high cytotoxic activity - synthesis, activity, and pharmacokinetic profile.
Sign Up to like & getrecommendations! Published in 2019 at "Bioconjugate chemistry"
DOI: 10.1021/acs.bioconjchem.9b00565
Abstract: A set of 41 glycosidic conjugates of pentacyclic triterpenes was synthesized in order to improve the solubility of highly cytotoxic parent compounds. Their in vitro cytotoxic activity was evaluated in 25 cancer cell lines and… read more here.
Keywords: ccrf cem; pharmacokinetic profile; compound; activity ... See more keywords
Discovery of a Potent and Selective PI3Kδ Inhibitor (S)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01264
Abstract: PI3Kδ inhibitors have been approved for B-cell malignancies like CLL, small lymphocytic lymphoma, and so forth. However, currently available PI3Kδ inhibitors are nonoptimal, showing weakness against at least one of the several important properties: potency,… read more here.
Keywords: pharmacokinetic profile; pi3k inhibitor; profile; efficacy ... See more keywords
Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01349
Abstract: In this study, we have designed and synthesized pyrazoline analogues that partially mimic the structure of mycobactin, to address the requirement of novel therapeutics to tackle the emerging global challenge of antimicrobial resistance (AMR). Our… read more here.
Keywords: pump inhibition; pharmacokinetic profile; efflux pump; mycobactin ... See more keywords
Discovery of a Small Molecule TREM2 Agonist with Improved In Vitro Pharmacokinetic Profile and Validated Target Engagement.
Sign Up to like & getrecommendations! Published in 2025 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.5c00299
Abstract: The microglial lipid-sensing receptor TREM2 is a promising therapeutic target for Alzheimer's disease. We report the discovery of C1, a racemic structural analog of the clinical-stage TREM2 agonist VG-3927. Synthesized via a concise, modular, and… read more here.
Keywords: vitro pharmacokinetic; pharmacokinetic profile; target; validated target ... See more keywords
Cremophor EL Alters the Plasma Protein Binding and Pharmacokinetic Profile of Valspodar in Rats.
Sign Up to like & getrecommendations! Published in 2017 at "Drug research"
DOI: 10.1055/s-0043-111411
Abstract: Cremophor EL is a nonionic surfactant widely used in pharmaceutical formulations. Nonetheless, there are several reports on the influence of this excipient on the protein binding, pharmacokinetics, and pharmacodynamics of drugs. Valspodar is an investigational… read more here.
Keywords: valspodar; protein binding; plasma protein; formulation ... See more keywords
Polyethylene glycol-mediated functionalization of nanodelivery systems for improving their pharmacokinetic profile and anticancer efficacy
Sign Up to like & getrecommendations! Published in 2024 at "International Journal of Polymeric Materials and Polymeric Biomaterials"
DOI: 10.1080/00914037.2024.2383413
Abstract: Abstract PEGylation has emerged as a promising adaptation in the architecture of nanodelivery systems to improve their physicochemical properties, stability, circulation time, passive targeting to tumor tissues, and anticancer efficacy. Owing to its heterogeneity, metastatic… read more here.
Keywords: anticancer efficacy; polyethylene glycol; nanodelivery systems; efficacy ... See more keywords
Pharmacokinetic profile and in vivo anticancer efficacy of anagrelide administered subcutaneously in rodents
Sign Up to like & getrecommendations! Published in 2025 at "Drug Delivery"
DOI: 10.1080/10717544.2025.2463433
Abstract: Abstract Anagrelide (ANA) is a phosphodiesterase 3A (PDE3A) inhibitor, commonly prescribed for essential thrombocythemia. It also functions as a molecular glue, inducing complex formation between PDE3A and Schlafen 12. This association either triggers apoptosis or… read more here.
Keywords: profile vivo; vivo anticancer; efficacy; tumor ... See more keywords