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

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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

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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

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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

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each 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.