| 应用 |
Proteasomel抑制剂,epoxomicin的类似物 |
| 产品介绍 |
Carfilzomib (PR-171)是一种不可逆proteasome抑制剂，IC50为<5 nM，在体外优先抑制β5亚基的ChT-L活性，对PGPH和T-L活性很弱或没有作用。 |
| 备注 |
Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. |
| 生化机理 |
Carfilzomib, an irreversible proteasome inhibitor, has a favorable safety profile and significant anti-tumor activity in patients with relapsed and refractory multiple myeloma (MM). Here we summarize the clinical pharmacokinetics (PK), metabolism, and drug-drug interaction (DDI) profile of carfilzomib. The PK of carfilzomib, infused over 2-10 min, was evaluated in patients with solid tumors or MM. The proteasome has emerged as an important target for cancer therapy with the approval of bortezomib, a first-in-class, reversible proteasome inhibitor, for relapsed/refractory multiple myeloma (MM). Carfilzomib induced a dose- and time-dependent inhibition of proliferation, ultimately leading to apoptosis. Carfilzomib showed increased efficacy compared with bortezomib and was active against bortezomib-resistant MM cell lines and samples from patients with clinical bortezomib resistance. Carfilzomib has entered in a Phase II clinical trial in the treatment of multiple myeloma |
| 别名 |
Proteasomel抑制剂;卡非佐米; (alphaS)-alpha-[(4-吗啉基乙酰基)氨基]苯丁酰基-L-亮氨酰-N-[(1S)-3-甲基-1-[[(2R)-2-甲基环氧乙烷基]羰基]丁基]-L-苯丙氨酰胺;PR 171;PR171;PR-171; (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide |
