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Oncology
Lili Mao, Jun Guo, Lingjun Zhu, Yu Jiang, Wangjun Yan, Jian Zhang, Ai-Min Hui, Yuchen Yang, Lei Diao, Yan Tan, Han Zhao, Yiqian Jiang, Zhuli Wu, Lu Si
Summary: The study evaluated the safety, tolerability, and antitumor activity of the oral MEK1/2 inhibitor FCN-159 in Chinese patients with advanced, NRAS-mutant melanoma. The results showed that FCN-159 demonstrated promising antitumor activity at doses >6 mg once daily and was well tolerated.
EUROPEAN JOURNAL OF CANCER
(2022)
Article
Pharmacology & Pharmacy
Akihito Ogasawara, Kei Ogawa, Ryosuke Ide, Yuka Ikenaga, Chie Fukunaga, Satoshi Nakayama, Minoru Tsuda
Summary: This study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of dersimelagon in healthy participants. Dersimelagon was generally well tolerated and showed consistent pharmacokinetic profile. However, multiple doses of dersimelagon may lead to increased melanin density, which requires further investigation.
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
(2023)
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Oncology
Qian Jiang, Zongru Li, Yazhen Qin, Weiming Li, Na Xu, Bingcheng Liu, Yanli Zhang, Li Meng, Huanling Zhu, Xin Du, Suning Chen, Yang Liang, Yu Hu, Xiaoli Liu, Yongping Song, Lichuang Men, Zi Chen, Qian Niu, Hengbang Wang, Ming Lu, Dajun Yang, Yifan Zhai, Xiaojun Huang
Summary: This study evaluated the safety and efficacy of Olverembatinib in Chinese adults with TKI-resistant CML, and found significant antileukemic activity in patients in the chronic phase and accelerated phase.
JOURNAL OF HEMATOLOGY & ONCOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Mahmut Gozelle, Selen Gozde Kaya, Ahmet Bugra Aksel, Erva Ozkan, Filiz Bakar-Ates, Yesim Ozkan, Gokcen Eren
Summary: SIRT2, a member of the sirtuin family, regulates various cellular processes and is associated with inflammation, neurodegenerative diseases, and cancer. In this study, a series of compounds were synthesized and evaluated for their inhibitory activity against SIRT2 and cell activity. Two compounds with excellent selectivity against SIRT2 were identified, and molecular docking and molecular dynamics simulations were performed to rationalize their inhibitory activity.
BIOORGANIC CHEMISTRY
(2022)
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Pharmacology & Pharmacy
Xiaofei Zhou, Paul Matthias Diderichsen, Neeraj Gupta
Summary: This article investigates the effects of the novel anticancer drug TAK-931 on electrocardiogram QT intervals and heart rate. The study finds that at the recommended dose, TAK-931 does not significantly affect the QT intervals.
CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT
(2022)
Article
Pharmacology & Pharmacy
Khalid Abd-Elaziz, Christine Voors-Pette, Kang-Ling Wang, Sandy Pan, Yisheng Lee, John Mao, Yuhua Li, Benjamin Chien, David Lau, Zuzana Diamant
Summary: The study evaluated the safety, tolerability, and pharmacokinetics of FP-025, a novel and highly selective matrix metalloproteinase-12 inhibitor, in healthy subjects. Results showed that FP-025 was well tolerated and demonstrated a favorable pharmacokinetic profile. Further efficacy studies in patient populations with diseases like asthma, COPD, and pulmonary fibrosis are warranted.
CLINICAL DRUG INVESTIGATION
(2021)
