Analysis of the pharmacodynamic activity of the mTOR inhibitor ridaforolimus (AP23573, MK-8669) in a phase 1 clinical trial

Purpose As part of a phase 1 dose-escalation trial, the pharmacodynamic activity of the mammalian target of rapamycin (mTOR) inhibitor ridaforolimus was assessed in multiple tissues by measuring levels of phosphorylated 4E binding protein-1 (p-4E-BP1) or S6, two downstream markers of mTOR activity....

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Veröffentlicht in:	Cancer chemotherapy and pharmacology 2012-05, Vol.69 (5), p.1369-1377
Hauptverfasser:	Berk, Lori, Mita, Monica M., Kreisberg, Jeff, Bedrosian, Camille L., Tolcher, Anthony W., Clackson, Tim, Rivera, Victor M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Adaptor Proteins, Signal Transducing - drug effects Adaptor Proteins, Signal Transducing - metabolism Animals Antineoplastic agents Antineoplastic Agents - administration & dosage Antineoplastic Agents - pharmacology Biological and medical sciences Cancer Research Cell Line, Tumor Clinical Trial Report Dose-Response Relationship, Drug Female Humans Leukocytes, Mononuclear - metabolism Medical sciences Medicine Medicine & Public Health Mice Mice, SCID Neoplasms - drug therapy Neoplasms - pathology Oncology Pharmacology. Drug treatments Pharmacology/Toxicology Phosphoproteins - drug effects Phosphoproteins - metabolism Phosphorylation - drug effects Ribosomal Protein S6 - drug effects Ribosomal Protein S6 - metabolism Sirolimus - administration & dosage Sirolimus - analogs & derivatives Sirolimus - pharmacology Skin - metabolism Time Factors TOR Serine-Threonine Kinases - antagonists & inhibitors Xenograft Model Antitumor Assays
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