CAS NO: | 1354690-24-6 |
规格: | 98% |
分子量: | 450.46 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Background:
Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.
Expression of APDS mutant p110δ in cell lines and patient-derived lymphocytes lead to increased pathway activity, measured as phosphorylation of AKT or S6, which is suppressed by leniolisib in a concentration dependent way[1].
Oral leniolisib lead to a dose-dependent reduction in PI3K/AKT pathway activity and resolve the immune dysregulation with normalization of circulating transitional and na?ve B cells and reduction in PD-1+CD4+ and senescent CD57+CD8+ T cells. After 12 weeks of treatment, all patients show amelioration of lymphoproliferation with lymph node sizes and spleen volumes reduced by 39% (mean, range 26-57%) and 40% (mean, range: 13-65%), respectively[1].
Reference:
[1]. Rao V, et al. Effective 'Activated PI3Kd Syndrome' -targeted therapy with PI3Kd inhibitor leniolisib. The New England journal of medicine: NEJM. ISSN 0028-4793; 1533-4406