Vismodegib

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vismodegib (VIS-moh-DEH-gib) is a drug used to treat advanced basal cell carcinoma that has spread to other parts of the body or has come back after surgery. It is also used in patients who cannot be treated with surgery or radiation therapy. It is also being studied in the treatment of other types of cancer. Vismodegib blocks a type of protein involved in tissue growth and repair and may block the growth of cancer cells. It is a type of Hedgehog signaling pathway antagonist. Also called Erivedge and GDC-0449.

Information about Vismodegib

Vismodegib is a kinase inhibitor active used in the therapy of unresectable or metastatic basal cell carcinoma.

Liver safety of Vismodegib

Vismodegib therapy is associated with a low rate or transient elevations in serum aminotransferase during therapy and has been linked to rare cases of clinically apparent acute liver injury

Mechanism of action of Vismodegib

Vismodegib (vis” moe deg’ ib) is an orally available, kinase inhibitor with specific activity against a key step (activation of smoothened: SMO) in the hedgehog signaling pathway.  Hedgehog is a key regulator of embryonic development, cell growth and differentiation.  Mutations in this pathway have been identified in several malignant diseases including basal cell carcinoma.  Clinical trials of vismodegib in patients with metastatic or locally advanced basal cell carcinoma reported at least partial responses in up to half of patients. 

FDA approval information for Vismodegib

Vismodegib, the first hedgehog pathway inhibitor, was approved for use in the United States in 2012.  Current indications include metastatic or locally advanced, recurrent or unresectable basal cell carcinoma. 

Dosage and administration for Vismodegib

Vismodegib is available in capsules of 150 mg under the brand name Erivedge.  The typical dose is 150 mg once daily until disease progression or unacceptable toxicity occurs. 

Side effects of Vismodegib

Side effects are common and often dose limiting, although rarely life threatening.  Common side effects include muscle spasms, alopecia, anorexia, dysguesia, weight loss, nausea, diarrhea, fatigue and arthralgias.  Potential serious adverse events include severe weight loss, squamous cell skin cancer and embryo-fetal toxicity.


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