On December 28 of 2021, a new generation of oral selective estrogen receptor degrading agent (SERD) SCR-6852 capsule (R&D code: SIM0270) independently developed by Simcere for the treatment of ER+/HER2-type breast cancer which was applied for clinical trial (IND) was approved by NMPA. As the only molecule that can effectively penetrate the blood-brain barrier among similar SERD drugs in the world, SIM0270 is expected to provide a new treatment option for breast cancer patients with brain metastases.
SIM0270 is a brand-new oral SERD compound with independent intellectual property rights developed by Simcere. Compared with the first-generation intramuscular injection of SERD drugs, this oral dosage form can not only avoid injection-induced pain and related side effects, but also has good in vivo and in vitro activities and cross-species pharmacokinetic properties. At the same time, SIM0270 shows a higher brain penetration rate in preclinical in vivo models (cerebral blood ratio is 4-10 times higher than that of similar compounds under investigation), and it has a wide range of inhibitory effects on ER-positive cells in vitro. Tumor tissues and brain tissues are exposed to a high level. Single agent or combined with piperacillil can significantly inhibit tumor growth in ER-positive breast cancer mouse models, and significantly improve the survival time of ER-positive breast cancer brain orthotopic model mice. Related data has been announced at the 2021 American Association for Cancer Research Annual Meeting (AACR).
About ER+/HER2-type breast cancer
Estrogen receptor (ER) positive/human epidermal growth factor receptor (HER-2) negative type is the most important subtype of breast cancer, accounting for 65% of patients aged <50 years and 75% of elderly patients. This type of population is sensitive to endocrine therapy, but relapsed or metastatic disease is still difficult to cure, and the 5-year overall survival rate is only 25%.
Female breast cancer has replaced lung cancer as the world's largest new cancer. Due to advances in imaging technology and prolonged survival, the incidence of breast cancer brain metastasis is increasing. The current treatments for breast cancer patients with ER-positive/HER-2 negative brain metastases are mainly surgery and local radiotherapy. For patients who are not suitable for surgery and local radiotherapy, or for patients with brain metastases who relapse after surgery or after radiotherapy, drug treatments are scarce.