クリニカルKRAS ((G12C) 阻害剤AMG510は抗腫瘍免疫を誘発する
Jude Canon1, Karen Rex2, Anne Y Saiki2
1Amgen Research, Amgen Inc, Thousand Oaks, CA, USA. jcanon@amgen.com.
Nature
|November 1, 2019
まとめ
研究者は,前臨床モデルと初期の臨床試験で有意な抗腫瘍活性を示す新しいKRAS ((G12C)) 阻害剤であるAMG 510を開発しました. この標的治療は KRAS変異を患っているがん患者にとって 新しい希望をもたらします
科学分野:
- 腫瘍学
- 分子生物学
- 薬物の発見
背景:
- KRASはがんで頻繁に変異する腫瘍遺伝子で 腫瘍の成長を促します
- KRAS ((G12C)) 変異は,阻害剤開発のための標的となるシステイン残留物を提示する.
研究 の 目的:
- KRAS (G12C) を標的とする共性阻害剤の最適化により,効能と選択性が向上する.
- 新薬のAMG510の治療可能性を臨床前および臨床環境で評価する.
主な方法:
- 阻害剤の結合相互作用を最適化するための構造ベースの薬剤設計.
- KRAS (G12C) 腫瘍モデルでの臨床前試験 (in vitroおよびin vivo).
- AMG510の安全性と有効性を評価する臨床試験
主要な成果:
- 臨床開発中の最初のKRAS (G12C) 阻害剤であるAMG510の発見
- AMG510は腫瘍の有意な回帰と,化学療法と標的治療薬による有効性の向上を示した.
- AMG510は炎症を誘発する腫瘍の微小環境を誘発し,マウスの耐久的な治癒と適応免疫をもたらした.
結論:
- AMG510はKRAS ((G12C) の有力かつ選択的阻害を示している.
- AMG510は有望な抗腫瘍活性を示し,KRAS (G12C) がんの変容療法としての可能性を示しています.
- AMG510の開発は,標的がん治療における重要な進歩です.
さらに関連する動画
09:29Development and Maintenance of a Preclinical Patient Derived Tumor Xenograft Model for the Investigation of Novel Anti-Cancer Therapies
Published on: September 30, 2016
14.3K
12:55Generation of CAR T Cells for Adoptive Therapy in the Context of Glioblastoma Standard of Care
Published on: February 16, 2015
22.0K
関連する概念動画
01:27Tumor Immunotherapy
1.7K
Immunotherapy is a treatment that boosts or manipulates the immune system to fight diseases, including cancer. For instance, by stimulating an immune response through vaccinations against viruses that cause cancers, like hepatitis B virus and human papillomavirus, these diseases can be prevented. Nonetheless, some cancer cells can avoid the immune system due to their rapid mutation and division. The immune response to many cancers involves three phases: elimination, equilibrium, and escape.
1.7K
02:57Targeted Cancer Therapies
8.6K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
8.6K
02:34Inhibition of Cdk Activity
5.5K
The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
5.5K
02:50Combination Therapies and Personalized Medicine
5.8K
Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
5.8K