Recently, CDE official website showed that the clinical trial application of Betta Pharmaceuticals for BPI-23314 tablets, a type 1 new drug, has been given the implied license. This new drug is used to treat malignant hematological tumors (including but not limited to myeloproliferative tumors, such as myelofibrosis and myelodysplastic syndrome. This is the third clinical trial license for the drug.
According to the announcement issued by Betta Pharmaceuticals, BPI-23314 is a new molecular chemical entity independently developed by it. It is a new, powerful and selective oral small molecule inhibitor of bromine structural domain and extra terminal domain (BET) protein family, which has a brand-new mechanism of degrading target protein and is intended to be used for the treatment of hematologic tumor, breast cancer and lung cancer.
Upon inquiry, drugs with the same target at home and abroad are in the clinical trial stage, and haven't yet been listed.
At present, BET family proteins have become one of the new targets for scientists to develop innovative anti-cancer therapies. BET protein family consists of BRD2, BRD3, BRD4 and BRDT. Studies have shown that BET protein is widely expressed in human tissues and regulate gene transcription. Among them, bromine structural domain protein 4 (BRD4) is the most important functional protein in BET family, which can regulate DNA replication and gene expression through histone acetylation, thus affecting the cell cycle procession. In recent years, it has been found that the dysfunction of BET family is also closely related to the occurrence, invasion and metastasis of tumors.
As a new anti-cancer drug, BET inhibitor is promising in treating blood cancers, such as leukemia and lymphoma. BET inhibitors can inhibit growth of tumor by blocking the function of BET protein. R&D of BET protein selective inhibitors is a new target at present. At present, many pharmaceutical companies and hospital supply companies have engaged in the R&D of this selective inhibitor.
Wenda Pharma-NHWD-870
NHWD-870 is a novel and powerful BET inhibitor, which is intended to be developed for the treatment of various solid tumors. This is the first innovative antitumor drug of Wenda Pharma entering into the clinical development stage.
NHWD-870 can inhibit BRD4 structural domain by targeting, and induce apoptosis of tumor cells, thus achieving anti-tumor effect. According to public data, the drug was initially developed by Professor Chen Xiang and Professor Yin Mingzhu from the R&D team of Xiangya Hospital Central South University. And now, the subsequent R&D is carried out by Wenda Pharma and Hengya Pharm.
Researchers found that NHWD-870 can not only down-regulate c-MYC and directly inhibit the proliferation of tumor cells, but also block the proliferation of tumor-related macrophages through a variety of mechanisms, some of which are to stimulate the expression and secretion of factor CSF1 by reducing the macrophage colony of tumor cells.
Preclinical studies indicate that NHWD-870 shows strong anti-tumor activity in nine different mouse tumor models. Moreover, the inhibitory activity of NHWD-870 is 5-50 times higher than that of similar compounds. According to the result of pharmacokinetic study, oral NHWD-870 shows good tumor penetration.
Mechanism of NHWD-870 (Source: Reference 1)
Jacobio -- JAB-8263
JAB-8263 is a BET inhibitor of Jacobio. JAB-8263 is intended to be used in the treatment of various cancer types associated with increased MYC expression, including various solid tumors and blood cancers. According to the preclinical studies, JAB-8263 shows good anti-tumor effect in various solid tumors and hematologic tumors, and has higher activity than similar drugs. JAB-8263 has obtained the IND approval for the treatment of solid tumors in China and the United States. In July 2020, it was approved for IND by FDA ...
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