Vismodegib
Hedgehog Inhibitor
DB08828
Approved Indication
Vismodegib is used for treating locally advanced or metastatic basal cell carcinoma in patients whose carcinoma has recurred after surgery, and in patients who are not candidates for surgery or radiation.
1
Targets
10
Resistance Mutations
50
References
5L7I
Structure Loaded
Protein Targets
Mechanism of Action
Mutations of the Hedgehog pathway may results in uncontrolled proliferation of skin basal cells. Vismodegib binds to and inhibits the transmembrane protein Smoothened homologue (SMO) to inhibit the Hedgehog signalling pathway.
Resistance Mutations
— 16 resistance samples observed in COSMIC
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SMO
p.A459V
5
p.C469Y
5
p.D473G
5
p.D473H
5
p.D473Y
5
p.Q477E
5
p.S533N
5
p.T241M
5
p.V321M
5
p.W281L
3
Resistance mutations sourced from COSMIC Drug Resistance database. Cyan = on-target · Amber = off-target · numbered badge = PubMed references for that mutation
Details
DrugBank ID
DB08828 ↗
Approval Date
2012-01-30
Molecular Weight
421.297 g/mol
Drug Class
Hedgehog Inhibitor
ATC Codes
L01XX43
Synonyms
Hedgehog Antagonist GDC-0449, Vismodegibum
PubChem
CID: 24776445 ↗
ChEMBL
CHEMBL473417 ↗
SMILES
CS(=O)(=O)C1=CC(Cl)=C(C=C1)C(=O)NC1=CC=C(Cl)C(=C1)C1=CC=CC=N1
ADMET Profile
Computing properties…
Drug References (DrugBank)