vesicles
Colonel
Chinese scientists develop world's 1st oral HDAC inhibitor
Lu Xianping works in a lab at Shenzhen Chipscreen Biosciences Ltd. in Shenzhen, south China's Guangdong Province, May 20, 2015. Lu Xianping, together with other four returned overseas scientists, spent 14 years to develop Chidamide, the world's first oral HDAC inhibitor, which was given regulatory approval in January. (Xinhua/Mao Siqian)
HBI-8000 (chidamide) is a member of the benzamide class of histone deacetylase (HDAC) inhibitors designed to block the catalytic pocket of Class I HDACs. HBI-8000 is an orally bioavailable, low-nanomolar inhibitor of cancer-associated HDAC enzymes with favorable pharmacology and safety profiles. HBI-8000 inhibits cancer-associated Class I HDAC1, HDAC2, HDAC3, as well as Class IIb HDAC10 at nanomolar concentrations and stimulates accumulation of acetylated histones H3 and H4 in tumor cells. Studies with human-derived tumor cell lines have demonstrated that HBI-8000 inhibits the growth of many tumor cell lines via multiple mechanisms of action, including epigenetic regulation of tumor cell growth and apoptosis, immunomodulatory effects such as activation of NK- and CD8 T-cell-mediated antitumor activity, as well as repression of genes associated with drug resistance. To date, HBI-8000 has been dosed globally in more than 280 patients with various types of hematological and solid tumors in several clinical trials, including a Phase 1 trial completed in the U.S.
Not to rain on everyone's parade, but this kind of new drugs come out almost on a daily basis in publications. We'll have to wait and see how the Phase 1 clinical trial goes. The most critical aspect is the toxicity trial. A patient number of 280 is not enough. And 99.8% of the new drugs fail clinical trials.
A few other things that I've noticed. I've gone over some of their latest publications (2008 and later). To be honest, not very impressive at all. First of all, the best journal of their publication has an impact factor of ~4. Most of their publications have impact factors between 2 and 3, which is simply pathetic. In a decent biology dept, a journal with impact factor below 1.5 is not even considered peer-reviewed. I am sure they have sent their manuscripts to better journals (impact factors of at least 10 or above), but simply got rejected. This means high-impact journals have been less impressed with their work.