Erivedge

— THERAPEUTIC CATEGORIES —
  • Melanoma and other skin cancers

Erivedge Generic Name & Formulations

General Description

Vismodegib 150mg; caps.

Pharmacological Class

Hedgehog pathway inhibitor.

How Supplied

Caps—28

Manufacturer

Generic Availability

NO

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.

Erivedge Indications

Indications

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

Erivedge Dosage and Administration

Adult

Swallow whole. 150mg once daily until disease progression or unacceptable toxicity. Withhold for up to 8 weeks for intolerable reactions until improved or resolved.

Children

Not established.

Erivedge Contraindications

Not Applicable

Erivedge Boxed Warnings

Boxed Warning

Embryo-fetal toxicity.

Erivedge Warnings/Precautions

Warnings/Precautions

Risk of embryo-fetal death or severe birth defects in pregnant women. Verify pregnancy status within 7 days prior to initiating therapy. Advise females of reproductive potential to use effective contraception during therapy and for 24 months after final dose; male patients should use condoms (even after a vasectomy) during and for 3 months after final dose. Advise patients not to donate blood or blood products during therapy and for 24 months after final dose. Advise male patients not to donate semen during and for 3 months after final dose. Permanently discontinue if severe cutaneous adverse reactions occur (eg, SJS, TEN, DRESS). Obtain baseline serum CPK and creatinine levels, and as clinically indicated. Based on severity, interrupt dose or discontinue if musculoskeletal adverse reactions occur or serum CPK elevation. Premature fusion of the epiphyses (in pediatrics, if exposed). Pregnancy: avoid. Nursing mothers: not recommended (during and for 24 months after final dose).

Erivedge Pharmacokinetics

Absorption

Single dose absolute bioavailability: 32%.

Distribution

Volume of distribution: ranges from 16.4–26.6 L.

Plasma protein bound: >99%.

Metabolism

Metabolic pathways include oxidation, glucuronidation, and pyridine ring cleavage. 

The two most abundant oxidative metabolites recovered in feces are produced in vitro by recombinant CYP2C9 and CYP3A.

 

Elimination

Fecal (82%), renal (4.4%). 

Half-life: 4 days (after continuous once-daily dosing); 12 days (after a single dose).

Erivedge Interactions

Not Applicable

Erivedge Adverse Reactions

Adverse Reactions

Muscle spasms, alopecia, dysgeusia, weight loss, fatigue, nausea, diarrhea, vomiting, decreased appetite, constipation, arthralgias, ageusia; amenorrhea.

Erivedge Clinical Trials

See Literature

Erivedge Note

Notes

Report immediately exposure to Erivedge during pregnancy by contacting the Genentech Adverse Event Line at (888) 835-2555.

Erivedge Patient Counseling

See Literature

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