oral Akt inhibitor
Ph. I in advanced solid tumors
scaffold hopping and PK opt.
J. Med. Chem.
Nanjing Chia-Tai Tianqing Pharmaceutical Co., Ltd., Nanjing, CN
Context. NTQ1062 (Nanjing Chia-Tai Tianqing; CTTQ) is an oral ATP-competitive Akt inhibitor being developed for cancer. Because the PI3K/Akt/mTOR pathway is one of the most commonly disrupted pathways in cancer, inhibitors targeting one or more of the three kinases have been hotly pursued. To date, five PI3K and three mTOR inhibitors have been approved, but favorable PK and safety data have hindered the approval of an Akt inhibitor for cancer. The compound, which is currently being evaluated in a Ph. I study in China (CTR20211999), joins a select list of Akt inhibitors being evaluated in various stages of clinical development. It remains to be seen whether the promising preclinical data will translate into decent efficacy and safety in patients. Editor…