Vismodegib

CAS No.: 879085-55-9




Molecular formula: C19H14Cl2N2O3S




Molecular weight: 421.3




Overview: Vismodegib, trade name: Erivedge; It is one of the first new anti-tumor drugs applied by Genentech Co., Ltd. and approved by the US Food and Drug Administration (FDA) for the treatment of advanced skin basal cell carcinoma (BCC) on January 30, 2012.




Purpose: It is used for the treatment of locally progressive or metastatic basal cell carcinoma in adults with recurrent or discomfort after surgery or radiotherapy; Basal cell carcinoma (BCC) is one of the most common skin cancers. It originates from the surface of the skin, and the patient will not feel pain. For skin diseases that are often exposed to sunlight or ultraviolet radiation, the probability of occurrence is the highest. The R&D and listing of Vimodge has brought good news to BCC patients. Its clinical role is important and its target market is huge. It will grow into a "giant bomb" drug (>US $1 billion) in the future.




Mechanism of action: Vimodoge has a new mechanism of action and is a hedgehog pathway inhibitor of selective Hedgehog signal transduction. Although Hedgehog signal transduction pathway is active in early life and plays an important role in regulating human growth and development, it is not active in adults. The vast majority of patients with basal cell carcinoma (>90%) have excessive activity of Hedgehog signal transduction pathway, which is considered as the basic molecular driver of basal cell carcinoma. As a competitive cyclopamine antagonist, it acts on the transmembrane G protein-coupled receptor protein (Smoothened) in the Hedgehog signal pathway. It keeps the transcription factors GLT-1 and GLT-2 inactive by inhibiting the SMO receptor, and can block the expression of tumor regulatory genes related to the Hedgehog signal pathway.


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