Dosing & Uses
Dosage Forms & Strengths
capsule
- 150mg
Basal Cell Carcinoma
Indicated for 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 or radiation
150 mg PO qDay
Continue until disease progression or unacceptable toxicity
Dosage Modifications
Hepatic and renal impairment: No dosage adjustment necessary
Intolerable adverse reactions
- Withhold treatment for ≤8 weeks for intolerable adverse reactions until improvement or resolution
- Treatment durations <8 weeks prior to interruptions have not been studied
Safety and efficacy not established
Clinical trials did not include sufficient numbers of patient 65 years or older to evaluate if a different dose is required
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Muscle spasms (71.7%)
Alopecia (63.8%)
Dysgeusia (55.1%)
Weight loss (44.9%)
Fatigue (39.9%)
Nausea (30.4%)
Diarrhea (29%)
Decreased appetite (25.4%)
Constipation (21%)
Arthralgias (15.9%)
Vomiting (13.8%)
Ageusia (10.9%)
1-10%
Hyponatremia (4%)
Azotemia (2%)
Hypokalemia (1%)
Frequency Not Defined
Amenorrhea
Premature fusion of epiphyses
Increased blood creatinine phosphokinase
Postmarketing Reports
Drug-induced liver injury
Skin and subcutaneous tissue disorders: Stevens-Johnson syndrome/toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms
Warnings
Black Box Warnings
Embryo-fetal toxicity
- Can cause fetal harm when administered to a pregnant woman based on its mechanism of action
- Shown to be embryotoxic, fetotoxic, and teratogenic in animals
- Teratogenic effects included severe midline defects, missing digits, and other irreversible malformations
- Verify pregnancy status of females of reproductive potential ≤7 days before initiating therapy
- Advise male and female patients of the risks of embryo-fetal death and severe birth defects and the need for contraception during and after treatment
- Advise males of the potential risk of drug exposure through semen and to use condoms with a pregnant partner or a female partner of reproductive potential
- Advise patients to contact their healthcare provider immediately if they suspect they (or, for males, their female partner) may be pregnant
- Report exposure during pregnancy to the Genentech Adverse Event Line at 1-888-835-2555
Contraindications
None
Cautions
Can cause fetal harm when administered to pregnant women, or if pregnant women are exposed to vismodegib via seminal fluid
Patient should not donate blood while taking vismodegib or for at least 24 months after last dose
Premature fusion of epiphyses reported in pediatric patients exposed to drug; In some cases, fusion progressed after drug discontinuation
Advise males not to donate semen during and for 3 months after therapy
Severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN) and drug reaction with eosinophilia and systemic symptoms (DRESS), which can be life-threatening or fatal, reported during treatment; permanently discontinue in patients with these reactions
Pregnancy & Lactation
Pregnancy
There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ERIVEDGE during pregnancy. Report pregnancies to Genentech at 1-888-835-2555
Can cause fetal harm when administered to a pregnant woman based on its mechanism of action (by either direct exposure or exposure from seminal fluid); see Black Box Warnings
Shown to be teratogenic, embryotoxic, and fetotoxic in rats at maternal exposures lower than the human exposures at the recommended dose of 150 mg/day; embryolethal in rats at exposures within the range achieved at the recommended human dose
Advise females of reproductive potential to use effective contraception during therapy and for 24 months after final dose; advise male patients to use condoms, even after a vasectomy, to avoid potential drug exposure in pregnant partners and female partners of reproductive potential during therapy and for 3 months after the final dose
Amenorrhea can occur in females of reproductive potential; reversibility of amenorrhea is unknown
Advise males to use condoms, even after a vasectomy, to avoid potential drug exposure in pregnant partners and female partners of reproductive potential during therapy and for 3 months after final dose; advise male patients not to donate semen during and for 3 months after the final dose
Lactation
Unknown whether distributed in breast milk; because of potential for serious adverse reactions in breastfed infants from therapy, advise a nursing woman that breastfeeding is not recommended during therapy and for 24 months after the final dose
A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Hedgehog (Hh) pathway inhibitor; the Hedgehog signaling pathway is important in embryogenesis, but in adults, it is mostly inactive; signaling is relayed by key proteins including Smoothened (SMO)
Hh ligand-expressing cancerous epithelial cells that are activated by the Hh signaling pathway may cause growth-promotion; vismodegib binds to and inhibits SMO, a transmembrane protein involved in Hedgehog signal transduction
Absorption
Bioavailability: 31.8%
Steady-state achieved within 7 days
Distribution
Protein Bound: >99%, binds to both albumin and alpha-1-acid glycoprotein
Vd: 16.4-26.6 L
Metabolism
>98% of total circulating drug components are the parent drug
Minimally metabolized by oxidation, glucuronidation, and pyridine ring cleavage
Minor substrate of CYP2C9 and CYP3A4
Minor inhibitor of CYP2C8, CYP2C9, and CYP2C19
An inhibitor of BCRP transporter
Elimination
Half-life: 4 days (at steady-state); 12 days (single-dose)
Excretion: Feces 82%, urine 4.4%
Administration
Oral Administration
May take with or without food
Swallow capsules whole; do not open or crush capsules
If a dose missed, resume with the next scheduled dose
Storage
Capsules: Store at room temperature 20-25°C (68-77°F); excursions permitted between 15-30°C (59-86°F)
Images
Patient Handout
Formulary
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