duvelisib

Duvelisib (INK1197) 是 p100δ的选择性抑制剂，能够作用于 p110δ (IC50:2.5 nM)、p110γ (IC50:27.4 nM)、p110β (IC50:85 nM) 和 p110α (IC50:1602 nM)。

Duvelisib (R enantiomer) hydrochloride (INK1197 R enantiomer HCl) 是 PI3K 抑制剂。Duvelisib (R enantiomer) hydrochloride 是 Duvelisib 的活性较低的对映体。

Duvelisib R enantiomer (IPI-145 R enantiomer) 是一种 Duvelisib 的对映异构体，活性较低。 它是一种 PI3K 抑制剂。

Duvelisib, also known as IPI-145 and INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Upon administration, PI3K delta gamma inhibitor IPI 145 prevents the activation of the PI3K delta gamma-mediated signaling pathways which may lead to a reduction in cellular proliferation in PI3K delta gamma-expressing tumor cells. Unlike other isoforms of PI3K, the delta and gamma isoforms are overexpressed primarily in hematologic malignancies and inflammatory and autoimmune diseases.

Elenbecestat,also known as E2609 is a BACE1 inhibitor. By inhibiting BACE, a key enzyme in the production of Aβ peptides, E2609 decreases the formation of these peptides which can aggregate into toxic oligomers and protofibrils and eventually form amyloid plaques in the brain. Elenbecestat has been shown to reduce Aβ levels in cerebrospinal fluid, was investigated in two global phase 3 studies in early AD.