ポマリドマイド

外観

白色～黄色～緑色粉末～結晶

用途

ポマリドミド（Pomalidomide）は、サリドマイドの誘導体であり、血管新生阻害作用と免疫調節作用を有する医薬品である。ボルテゾミブ?レナリドミド治療抵抗性または治療後に再発した多発性骨髄腫の治療に用いられる。 ポマリドミドは直接的に血管新生を阻害すると共に骨髄腫細胞の成長を阻害する。この二重効果が作用の本質であり、ロリプラムやペントキシフィリン（英語版）などのTNF-α阻害薬が骨髄腫細胞の阻害も血管新生の阻害もしないことに比べて効果的である。

効能

抗悪性腫瘍薬, 免疫調節薬

商品名

ポマリスト (セルジーン)

説明

In February 2013, the US FDA approved pomalidomide (also known as CC4047) for the treatment of multiple myeloma (MM) in patients with disease progression after receiving other cancer therapeutics. Pomalidomide is a 4-amino analog of thalidomide with enhanced potency and an improved toxicity profile. Pomalidomide and thalidomide exert their effects by modulation of immunity, inhibition of angiogenesis, interference with the bone/tumor microenvironment, and inhibition of the cereblon protein. Pomalidomide potently inhibited in vitro proliferation in a variety of human MM cell lines, IC₅₀～10 nM, while thalidomide showed almost no inhibition up to 100 μM. In mouse MM tumor models, 50 mg/kg daily doses of pomalidomide resulted in marked inhibition of tumor growth after 15 days of treatment and complete regression in 3–6 weeks versus thalidomide-treated controls at the same dose. Pomalidomide is prepared by condensation of 4-nitrophthalic anhydride with 3-aminopiperidine-2,6-dione followed by catalytic hydrogenation of the nitro group.

化学的特性

Yellow Solid

使用

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM

定義

ChEBI: An aromatic amine that is thalidomide substituted at position 4 on the isoindole ring system by an amino group. Used for the treatment of multiple myeloma in patients who failed to respond to previous therapies.