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
Contraindicated (0)
Serious - Use Alternative (1)
- palifermin
palifermin increases toxicity of vismodegib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
Monitor Closely (21)
- aluminum hydroxide
aluminum hydroxide will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- aluminum hydroxide/magnesium carbonate
aluminum hydroxide/magnesium carbonate will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- aluminum hydroxide/magnesium trisilicate
aluminum hydroxide/magnesium trisilicate will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- aspirin/citric acid/sodium bicarbonate
aspirin/citric acid/sodium bicarbonate will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- calcium carbonate
calcium carbonate will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- cimetidine
cimetidine will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- dexlansoprazole
dexlansoprazole will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- dichlorphenamide
dichlorphenamide and vismodegib both decrease serum potassium. Use Caution/Monitor.
- esomeprazole
esomeprazole will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- famotidine
famotidine will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- ibuprofen/famotidine
ibuprofen/famotidine will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- lansoprazole
lansoprazole will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- levoketoconazole
levoketoconazole will increase the level or effect of vismodegib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Vismodegib is a substrate of efflux transporter P-glycoprotein (P-gp); coadministration with P-gp inhibitors increase vismodegib systemic exposure
- magnesium hydroxide
magnesium hydroxide will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- magnesium oxide
magnesium oxide will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- mavacamten
vismodegib will increase the level or effect of mavacamten by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Inititiation of weak CYP2C19 inhibitors may require decreased mavacamten dose.
- nizatidine
nizatidine will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- omeprazole
omeprazole will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- pantoprazole
pantoprazole will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- rabeprazole
rabeprazole will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown
- siponimod
siponimod and vismodegib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
Minor (1)
- levoketoconazole
levoketoconazole increases effects of vismodegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. Coadministration with CYP3A4 inhibitors in vitro does not appear to affect vismodegib plasma levels significantly.
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
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Erivedge oral - | 150 mg capsule |  |
Copyright © 2010 First DataBank, Inc.
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