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Abt-199 is a new type of cancer drug, a Bcl-2 inhibitor, developed by AbbVi, an American pharmaceutical company. It is effective in fighting cancer and has fewer side effects than current drugs. The study was conducted by researchers in the United States and Australia. Related research results were published in the international journal NatureMedicine. Unlike common cancer drugs, the drug, abT-199, works by attacking an important protein called Bcl-2. Bcl-2 is one of the first members of the bcl-2 family of proteins that regulate cell death. It has been linked to many types of cancer, as well as some mental disorders and autoimmune diseases. In cancer, it is thought to act as a suppressor that helps cancer cells resist cancer treatment drugs. In cancer treatment, the pro-survival protein Bcl-2 can be used by cancer cells to suppress the therapeutic effects of conventional chemotherapy, which is often a headache for clinicians. Because cancer cells can use the pro-survival protein Bcl-2 to suppress the therapeutic effects of traditional chemotherapy, clinicians have to repeatedly increase the dose, resulting in side effects such as nausea, hair loss and Chemicalbook. The emergence of ABT-199 as a drug that can eliminate and reduce bcl-2 in cancer cells has led many clinicians to see the dawn of cancer treatment. Abt-199 is a novel anticancer drug that inhibits bcl-2 growth without affecting Bcl-XL, a protein essential for platelet formation. Overcoming this problem, in the history of cancer treatment is nothing short of jubilant. [Clinical trial evaluation] : A phase I clinical trial (NCT01328626) enrolled 84 patients with recurrent/refractory type.
Abt-199 showed low sensitivity to Bcl-XL, McL-1 and Bcl-W with Ki of 48nM,>444nM and 245nM, respectively. Abt-199 effectively inhibited FL5.12-Bcl-2 cells,RS4; 11 cells, EC50 of 4nM and 8nM, respectively, showed low activity on FL5.12-Bcl-XL cells, EC50 of 261nM. Abt-199 chemicalbook induced RS4; 11 cells exhibited rapid apoptosis, cytochrome C release, caspase activation, phosphatidylserine externalization, and sub-G0/G1DNA accumulation. Quantitative western blotting showed that the sensitivity of ABT-199 to NHL, DLBCL, MCL, AML and ALL cell lines was strongly correlated with bcl-2 expression. Abt-199 also induced CLL apoptosis with an average EC50 of 3.0nM.Abt-199 (100mg/kg) treated RS4; The maximum tumor growth inhibition rate was 95% and the tumor growth was delayed by 152%. Chemicalbookabt-199, either alone or in combination with SDX-105 and other agents, also inhibited tumor growth in DoHH2 and Granta 519 grafts.
Venetoclax (ABT-199, GDC-0199) is a bcl-2 selective inhibitor with Ki <0.01 nM in cell-free assay, which is more than 4800 times more selective than bcl-XL and Bcl-W, and has no inhibitory activity against McL-1. Venetoclax has been shown to induce cell growth inhibition, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.
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