2017년 2월 15일 수요일

ビスモデギブ

ビスモデギブ

ビスモデギブ
Vismodegib.svg
Vismodegib spacefill.png
Material name by the IUPAC glossology
Clinical data
Legal regulation
  • Investigational
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

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

  1. ^ a b H. Spreitzer (4 July 2011). " Neue Wirkstoffe – Vismodegib "(German). Österreichische Apothekerzeitung (14/2011): 10. 
  2. ^ Molecule of the Month. (June 2011). http://www.prous.com/molecules/default.asp?ID=210. 
  3. It is Chugai Pharmaceutical February 19, 2010 about the licensing agreement conclusion of ^ hedgehog course repressor "RG3616"
  4. ^ 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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