BeBetter Med filed Two Patent Applications in More than 40 Countries
   Guangzhou BeBetter Medical Technology Co., Ltd. announced two invention patents of the company (CN105130986B, CN106117185B) have been issued by the China National Patent Bureau, and the corresponding PCT international patents (WO 2017/054484, WO 2017/036263) recently filed for patent application in more than 40 countries, including the United States, the EU, Canada, Australia and Japan etc.The WO 2017/054484 invention discloses a pyrimidine or pyridopyridone compound and an application thereof relating to the technical field of medicament preparation. The compound can selectively suppress cyclin-dependent kinases (CDK) 4 and 6. Thus, the compound can be used for various diseases caused by cell cycle control disorders involving CDK4 and CDK6, and particularly in the treatment of malignant tumors.  The WO 2017/036263 invention discloses a 2, 4-di-(nitrogen containing group) substituted pyrimidine compound, a pharmaceutically acceptable salt and a stereoisomer thereof, a preparation method thereof, and a use thereof in preparation of anti-tumor drugs. The compound can selectively suppress activity of mutant epidermal growth factor receptors (EGFR), including T790M and gain-of-function mutant EGFR L858R and ex19del as well. The compound has a weak suppression effect on wild-type EFGR, and thus it has a potential to be used for treating EGFR mutant tumors, especially non-small cell lung cancer (NSCLC) carrying a T790M EGFR mutation.After obtaining invention patents issued within China and internationally, BeBetter Med will possess global rights for both BEBT-209 and BEBT-109, two First-of-Class new drug candidates.

    BEBT-209 is a more selective CDK4 inhibitor as compared to palbociclib, which is an equally potent CDK4 and CDK6 inhibitor. Neutropenia and lymphopenia are the most frequently reported adverse reaction with palbociclib.  CDK6 has a unique role in the hematopoietic system. CDK6 is mainly expressed in hematopoietic cells. Loss of CDK6 in mice causes thymic atrophy and reduction in neutrophils, lymphocytes and platelets. By reducing CDK6 inhibitory activities, and BEBT-209 may have the potential to significantly reduce toxicities against immunoeffector cells and other normal hematopoietic cells while retaining strong anti-cancer activities of palbociclib. The incidence of breast cancer in China is about 550,000 every year. About 60% of breast cancer patients with estrogen receptor positive /HER2 negative are being treated with CDK4 and CDK6 inhibitors.

      BEBT-109 is a third generation EGFR inhibitor discovered on the basis of osimertinib (AZD9291). Its inhibitory activity against EGFR T790M mutation is stronger than AZD9291. In addition, its potency against mutant EGFR is over 1000-fold stronger comparing to the wild type EGFR. Furthermore, as a covalent irreversible EGFR inhibitor, as compared to osimertinib, it has improved pharmacokinetics and has better safety profiles. Its potent anti-tumor activity has been demonstrated in various tumor models with EGFR mutations. Therefore, BEBT-109 has the potential to be a best-in-class 3rd generation EGFR inhibitor.

     The IND-Enabling studies of BEBT-209 and BEBT-109 were initiated in 2017. The company plans to submit INDs in the fourth quarter of the year and commence phase I clinical trial in the first quarter of 2019.