ビスモデギブ
Material name by the IUPAC glossology | |
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2-chloro-N-(4-chloro-3-pyridin-2-ylphenyl) -4-methylsulfonylbenzamide | |
Clinical data | |
Legal regulation |
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Dosage method | Oral |
Identification | |
ATC cord | none |
PubChem | CID: 24776445 |
UNII | 25X868M3DS |
Another name | GDC-0449, RG-3616 |
Chemical data | |
Chemical formula | C19H14Cl2N2O3S |
Molecular weight | 421.30 g/mol |
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ビスモデギブ (British: Vismodegib) is a kind of the inhibitors for the hedgehog signal transmission course. I am expected as the molecular target medicine which is usable for various types of tumors with pharmaceutical products studying now. The development name is RG3616 or GDC-0449. As of June, 2011, I finish the second aspect examination for the metastatic basal cell carcinoma in the United States [1], and a second aspect examination is going for metastatic colon cancer, a pulmonary small cell cancer, progressive stomach cancer, pancreatic cancer, medulloblastoma [2]. Chugai Pharmaceutical wins a license in Japan, and a clinical trial becomes going to be carried out [3].
Action mechanism
ビスモデギブ acts as an antagonist inhibiting Smoothened(SMO) constituting a hedgehog signal course. It is known that this signal course is activated for more than 90% of basal cell carcinomas [1]. Is a neoplastic cell with the variation to aspartic acid (D473) of the 473rd of SMO; for ビスモデギブ indicating the tolerance [4].
Allied item
- Cyclopamine: The nature compound which inhibits Smoothened.
Source
- ^ a b H. Spreitzer (4 July 2011). " Neue Wirkstoffe – Vismodegib "(German). Österreichische Apothekerzeitung (14/2011): 10.
- ^ Molecule of the Month. (June 2011) .
- It is Chugai Pharmaceutical February 19, 2010 about the licensing agreement conclusion of ^ hedgehog course repressor "RG3616"
- ^ Robert L. Yauch et al (2 September 2009). "Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma." (English). Science (23 October 2009.vol.326): 572-574.
This article is taken from the Japanese Wikipedia ビスモデギブ
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