vismodegib (Rx)

Brand and Other Names:Erivedge
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Dosing & Uses

AdultPediatricGeriatric

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

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Interactions

Interaction Checker

and vismodegib

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            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.

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              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

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              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

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              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.

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              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%

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              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)

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              Erivedge oral
              -
              150 mg capsule

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              A Patient Handout is not currently available for this monograph.
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              Formulary

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              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
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              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.