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Last Updated: 01/25/17

Information below provided by the Pharmaceutical Company.

Vismodegib (GDC-0449, RO5450815, ERIVEDGE®)

Agent Description

Vismodegib (GDC 0449) is 2-chloro-N-(4-chloro-3-[pyridin-2-yl] phenyl)-4-(methylsulfonyl)benzamide. The molecular formula is C19H14Cl2N2O3S. The molecular weight is 421.30 g/mol. It is a crystalline free base with a pKa (pyridinium cation) of 3.8, appearing as a white to tan powder. The solubility of vismodegib is pH dependent with 0.1 μg/mL at pH 7 and 0.99 mg/mL at pH 1. The partition coefficient (log P) is 2.7. Solid-state stability studies showed that vismodegib is very stable against heat and light. In solution, vismodegib is very stable over a wide pH range and under oxidative conditions. Stability studies indicate that vismodegib API is stable in the recommended storage conditions of “Do not store above 30°C”. Each capsule for oral administration contains 150mg of vismodegib and the following inactive ingredients: microcrystalline cellulose, lactose monohydrate, sodium lauryl sulfate, povidone, sodium starch glycolate, talc, and magnesium stearate (non-bovine). The capsule shell contains gelatin, titanium dioxide, red iron oxide, and black iron oxide. The black printing ink contains shellac and black iron oxide.

Mechanism of Action

Vismodegib is an inhibitor of the Hedgehog pathway. Vismodegib binds to and inhibits Smoothened, a transmembrane protein involved in Hedgehog signal transduction

Classification

Hedgehog Inhibitor

Molecular Targets

Smoothened, a transmembrane protein in the hedgehog signaling pathway

Monograph

Approved Indication:

Vismogegib is indicated for the treatment of adults with metastatic basal cell carcinoma, or with locally advanced basal cell carcinoma that has recurred following surgery or who are not candidates for surgery, and who are not candidates for radiation.

Package insert: https://www.gene.com/download/pdf/erivedge_prescribing.pdf External Link

Studies of Interest

Supported Proposals:

  • Unique Neoadjuvant; Combination Treatment (not duplicative of any ongoing studies)
  • AE Management
  • Assessment by Histology and Staging
  • Assessment for other Hedgehog pathway dependent diseases

Not Supported Proposals:

  • Assessment for Hedgehog dependent diseases with demonstrated lack of efficacy (i.e. Prostate Cancer, AML)

Information collaborator would like included in investigator proposals

N/A

Genentech supports non-clinical research proposals through a separate mechanism. Please visit https://www.gene.com/gene/reagents-program/reagents-program.jsp External Link if you wish to submit a request for a Genentech agent for non-clinical work.