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Ruxolitinib

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Information about Ruxolitinib

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

Liver safety of Ruxolitinib

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 Ruxolitinib

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 Ruxolitinib

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 Ruxolitinib

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 Ruxolitinib

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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