efatutazone and Neoplasm-Metastasis

Efatutazone is a highly selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ), a therapeutic target for carcinogenesis.. In this phase I dose-escalation study, we assessed the safety, efficacy, and pharmacokinetics of efatutazone and the recommended dose (RD) was determined in Japanese patients with metastatic solid tumors using a 3+3 design.. A total of 13 patients were enrolled and received efatutazone at doses of 0.25 mg, 0.50 mg, and 0.75 mg bid for multiple 3-week cycles. No dose-limiting toxicities were observed, and the maximum tolerated dose was not reached. Partial response was confirmed in one patient and stable disease in three. Efatutazone exposure was almost dose-proportional. RD was determined to be 0.50 mg bid, corresponding to the RD in previous global phase I studies.. Efatutazone demonstrated acceptable toxicity and gave evidence of disease control in Japanese patients with metastatic solid tumors.

Topics: Administration, Oral; Aged; Antineoplastic Agents; Biomarkers; Female; Humans; Male; Middle Aged; Neoplasm Metastasis; Neoplasms; PPAR gamma; Thiazolidinediones; Treatment Outcome

AIB1Δ4 is an N-terminally truncated isoform of the oncogene amplified in breast cancer 1 (AIB1) with increased expression in high-grade human ductal carcinoma

Topics: Animals; Cell Culture Techniques, Three Dimensional; Cell Line, Tumor; CRISPR-Cas Systems; Dexamethasone; Disease Progression; Electric Impedance; Enhancer Elements, Genetic; Female; Humans; Lung Neoplasms; Mice; Mice, SCID; Neoplasm Invasiveness; Neoplasm Metastasis; Neoplasm Transplantation; Nuclear Receptor Coactivator 3; Phenotype; Protein Isoforms; Receptors, Glucocorticoid; RNA Splicing; Signal Transduction; Thiazolidinediones; Triple Negative Breast Neoplasms; Zebrafish