イミキモド 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
効能
抗ウイルス薬, 免疫調節薬, Toll様受容体作動薬
商品名
ベセルナ (持田製薬)
説明
Aldara was launched in the US for the topical treatment of genital warts
caused by human papillomavirus (HPV). It can be prepared in a six step approach
beginning with the nucleophilic substitution of 4-chloro-3-nitroquinolone with
isobutylamine or via a thermal electrocyclic ring closure of 1 - and 2-azahexatriene
systems. Aldara has antiviral and antitumor properties, with the former activity arising
from the induction of cytokines, in particular, INF-α. Aldara also induces TNF-γ, IL-1α, IL-1β, IL-1ra, IL-6, IL-8, IL-10, GM-CSF, G-CSF and MID-la formation 1-4 hr after
stimuli. The exact cells responsible for the response have not been determined,
however, it is not activating T lymphocytes, NK cells, B lymphocytes, or dendritic stem
cells but monocytes (CD14
+, CD36
+, HLA-DR
+, HLA-DQ
±, CD19
-, CD16
- and CD23
-) are
partly responsible. The speculation is that Aldara may interact with a kinase
modulating the transduction pathway leading to cytokine genes. There is no direct
antiviral activity (induction of IFN does not follow true dose response) and it is not mutagenic. The hydroxylated metabolite also induces IFN-α.
化学的特性
White to off white crystalline powder
使用
Imiquimod is a caspase 3 activator which acts as an immunomodulator and displays antiviral and anti-tumor activity. It is a patient-applied cream used for the treatment of genital warts and basal cell carcinoma. It is also used to cure actinic keratosis on the face and scalp. It belongs to a group of drugs called immune response modifiers, which work by activating the immune system to fight abnormal skin growth.
適応症
Imiquimod (Aldara) is a topical immune response modifier
approved for the treatment of anogenital warts
(condylomata acuminata). The exact mechanism of action
is unknown; it has no direct antiviral activity in
vitro. It is thought to work in vivo by inducing the production
of tumor necrosis factor (TNF α ), interferons
(IFN)α and γ , and other cytokines with antiviral activity.
It may also be useful for treatment of other types of
warts, molluscum contagiosum, and certain forms of
skin cancer. Local irritant reactions related to the frequency
of application are common.
応用例（製薬）
An imidazoquinoline used for the treatment of genital and
perianal warts. While the mechanism of action is not precisely
known, it is thought to induce interferon. It has no direct antiviral
activity. The 5% cream applied three times a week for
up to 16 weeks resulted in total wart clearance in 50% of
patients, with a better response in women than in men. Local
reactions are common and include erythema, erosion, excoriation
and edema.
生物活性
Immunomodulator that displays antiviral and antitumor activity. Acts as a Toll-like receptor 7 (TLR-7) agonist; stimulates proinflammatory cytokine production and activates NF- κ B.
作用機序
Imiquimod (Aldara) is an imidazoquinolone amine that is an immune responsemodifier.
Its exact mechanism is unknown in the topical treatment of HPV and molluscum
contagiosum but may be related to the immunomodulating effect of the drug. It is also
effective in the treatment of actinic keratoses and superficial basal cell carcinoma.
It induces production of a variety of cytokines and can enhance cell-mediated
cytolytic antiviral activity. It is a rapid and potent inducer of interferon-α,
interleukin?1 α and β, interleukin 6, interleukin 8, tumor necrosis factor-α,
granulocyte-macrophage colony-stimulating factor, and granulocyte colonystimulating
factor. Systemic absorption is minimal. It is generally well tolerated.
Adverse local reactions include erythema, erosion, excoriation, flaking, and edema
of the treatment sites.
イミキモド 上流と下流の製品情報
原材料
準備製品