First-in-human Phase 1 open label study of the BET inhibitor ODM-207 in patients with selected solid tumours

• Published in: British journal of cancer Vol. 123; no. 12; pp. 1730 - 1736
• Main Authors: Ameratunga, Malaka, Braña, Irene, Bono, Petri, Postel-Vinay, Sophie, Plummer, Ruth, Aspegren, John, Korjamo, Timo, Snapir, Amir, de Bono, Johann S
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 08.12.2020; Nature Publishing Group
• Subjects: 631/154/433; 631/67/1059/153; 631/67/1347; 631/67/1813/1634; 631/67/589/466; Administration, Oral; Adolescent; Adult; Aged; Anorexia; Antineoplastic Agents - administration & dosage; Antineoplastic Agents - adverse effects; Antineoplastic Agents - pharmacokinetics; Asthenia; Biological Availability; Biomedical and Life Sciences; Biomedicine; Blood Platelets - drug effects; Breast Neoplasms - drug therapy; Breast Neoplasms - metabolism; Cancer Research; Carcinoma, Non-Small-Cell Lung - drug therapy; Carcinoma, Non-Small-Cell Lung - metabolism; Clinical trials; Diarrhea; Drug Administration Schedule; Drug Resistance; Epidemiology; Epigenetics; Fatigue; Fatigue - chemically induced; Female; Humans; Lung Neoplasms - drug therapy; Lung Neoplasms - metabolism; Lymphoma, Non-Hodgkin - drug therapy; Lymphoma, Non-Hodgkin - metabolism; Male; Maximum Tolerated Dose; Melanoma - drug therapy; Melanoma - metabolism; Middle Aged; Molecular Medicine; Nausea; Neoplasms - drug therapy; Neoplasms - metabolism; Oncology; Oral administration; Ovarian Neoplasms - drug therapy; Ovarian Neoplasms - metabolism; Oxazoles - administration & dosage; Oxazoles - adverse effects; Oxazoles - pharmacokinetics; Patients; Pharmacokinetics; Prostate cancer; Prostatic Neoplasms, Castration-Resistant - drug therapy; Proteins - antagonists & inhibitors; Pyridines - administration & dosage; Pyridines - adverse effects; Pyridines - pharmacokinetics; Quinolines - administration & dosage; Quinolines - adverse effects; Quinolines - pharmacokinetics; Sarcoma - drug therapy; Sarcoma - metabolism; Small Cell Lung Carcinoma - drug therapy; Small Cell Lung Carcinoma - metabolism; Solid tumors; Therapeutic targets; Thrombocytopenia; Titration; Toxicity; Tumors; Vomiting; Young Adult

Background Bromodomain and extra-terminal domain (BET) proteins are reported to be epigenetic anti-cancer drug targets. This first-in-human study evaluated the safety, pharmacokinetics and preliminary anti-tumour activity of the BET inhibitor ODM-207 in patients with selected solid tumours. Methods...