Absorption of the orally active multikinase inhibitor axitinib as a therapeutic index to guide dose titration in metastatic renal cell carcinoma
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DOI: 10.1007/s10637-020-01023-z
Abstract: Purpose Axitinib is an orally active multikinase inhibitor currently used to treat patients with metastatic renal cell carcinoma (RCC). This study examined the pharmacokinetics of axitinib and the relationship between peak drug concentration (C max… read more here.
Keywords: renal cell; orally active; cell carcinoma; metastatic renal ... See more keywords
Phase II study of selumetinib, an orally active inhibitor of MEK1 and MEK2 kinases, in KRASG12R-mutant pancreatic ductal adenocarcinoma
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DOI: 10.1007/s10637-020-01044-8
Abstract: Background Preclinical evidence has suggested that a subset of pancreatic cancers with the G12R mutational isoform of the KRAS oncogene is more sensitive to MAPK pathway blockade than pancreatic tumors with other KRAS isoforms. We… read more here.
Keywords: inhibitor; orally active; study; selumetinib orally ... See more keywords
Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00789
Abstract: Targeting the menin-MLL protein-protein interaction is being pursued as a new therapeutic strategy for the treatment of acute leukemia carrying MLL-rearrangements (MLLr leukemia). Herein, we report M-1121, a covalent and orally active inhibitor of the… read more here.
Keywords: orally active; menin; covalent; interaction ... See more keywords
Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01006
Abstract: Colony-stimulating factor-1 receptor (CSF1R) is implicated in tumor-associated macrophage (TAM) repolarization and has emerged as a promising target for cancer immunotherapy. Herein, we describe the discovery of orally active and selective CSF1R inhibitors by property-driven… read more here.
Keywords: selective csf1r; murine colon; csf1r; orally active ... See more keywords
Mangostanin Derivatives as Novel and Orally Active Phosphodiesterase 4 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis with Improved Safety.
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DOI: 10.1021/acs.jmedchem.1c01085
Abstract: Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease, and its incidence rate is rapidly rising. However, effective therapies for the treatment of IPF are still lacking. Phosphodiesterase 4 (PDE4) inhibitors were reported to be… read more here.
Keywords: improved safety; fibrosis; idiopathic pulmonary; novel orally ... See more keywords
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02026
Abstract: On the basis of the synergism of topoisomerase (Top) and histone deacetylase (HDAC) inhibitors in antitumor therapy, a series of novel Top/HDAC dual inhibitors were designed and synthesized by the pharmacophore fusion strategy. After systematic… read more here.
Keywords: histone deacetylase; orally active; antitumor; dual inhibitors ... See more keywords
Discovery of 3-Quinazolin-4(3H)-on-3-yl-2,N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00239
Abstract: Phosphoinositide 3-kinases (PI3Ks) mediate a series of events related to cell growth, proliferation, survival, and differentiation. Overexpression of PI3Ks can lead to the dysregulation of cell homeostasis and cause tumorigenesis. In this study, rationally designed… read more here.
Keywords: pi3k; discovery quinazolin; orally active; active selective ... See more keywords
Rational Design of an Orally Active Anticancer Fluoropyrimidine, Pencitabine, a Hybrid of Capecitabine and Gemcitabine.
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DOI: 10.1021/acsmedchemlett.1c00565
Abstract: The structure of the anticancer drug capecitabine was redesigned to prevent metabolic conversion to 5-fluorouracil and its associated potentially fatal toxicities. The resulting cytidine analogue, pencitabine, is a hybrid of capecitabine and gemcitabine, another anticancer… read more here.
Keywords: orally active; capecitabine gemcitabine; pencitabine hybrid; pencitabine ... See more keywords
Orally Active Epoxyeicosatrienoic Acid Analogs.
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DOI: 10.1097/fjc.0000000000000523
Abstract: Biologically active epoxyeicosatrienoic acid (EET) regioisomers are synthesized from arachidonic acid by cytochrome P450 epoxygenases of endothelial, myocardial, and renal tubular cells. EETs relax vascular smooth muscle and decrease inflammatory cell adhesion and cytokine release.… read more here.
Keywords: active epoxyeicosatrienoic; eet; orally active; epoxyeicosatrienoic acid ... See more keywords
L-4, a Well-Tolerated and Orally Active Inhibitor of Hedgehog Pathway, Exhibited Potent Anti-tumor Effects Against Medulloblastoma in vitro and in vivo
Sign Up to like & getrecommendations! Published in 2019 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2019.00089
Abstract: Inhibition of aberrant Hedgehog (Hh) pathway had been proved to be a promising therapeutic intervention in cancers like basal cell carcinoma (BCC), medulloblastoma (MB), and so on. Two drugs (Vismodegib, Sonidegib) were approved to treat… read more here.
Keywords: orally active; hedgehog pathway; anti tumor; tolerated orally ... See more keywords
Erratum: Discovery and Preclinical Development of Orally Active Small Molecules That Exhibit Highly Selective Follicle Stimulating Hormone Receptor Agonism
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DOI: 10.3389/fphar.2021.672778
Abstract: [This corrects the article DOI: 10.3389/fphar.2020.602593.]. read more here.
Keywords: development orally; preclinical development; orally active; active small ... See more keywords