Skip to Content


Class: Antineoplastic Agents
VA Class: AN900
Chemical Name: 2-Chloro-N-[4-chloro-3-(2-pyridinyl)phenyl]-4-(methylsulfonyl)-benzamide
Molecular Formula: C19H14Cl2N2O3S
CAS Number: 879085-55-9
Brands: Erivedge


  • May cause embryofetal death or severe birth defects.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

  • Embryotoxic and teratogenic in animals; teratogenic effects include severe midline defects, missing digits, and other irreversible malformations.1

  • Verify pregnancy status prior to initiating vismodegib.1 Advise male and female patients of risks to the fetus, including need for contraception and potential for drug exposure through semen.1


Antineoplastic agent; hedgehog signaling pathway inhibitor.1 3

Uses for Vismodegib

Basal Cell Carcinoma

Treatment of metastatic basal cell carcinoma.1 3 7 9

Treatment of locally advanced basal cell carcinoma that has recurred following surgery or in those who are not candidates for surgery or radiation.1 3 7 9

Vismodegib Dosage and Administration


Restricted Distribution Program

  • Distribution of vismodegib is restricted; drug is available only through designated specialty pharmacies.10 Specific information available from the manufacturer at or at 888-249-4918.10


Oral Administration

Administer orally once daily without regard to meals.1

Swallow capsules whole; do not open or crush capsules.1

Do not replace missed doses; resume therapy with next scheduled dose.1



Basal Cell Carcinoma
Metastatic or Locally Advanced Disease

150 mg once daily until disease progression or unacceptable toxicity occurs.1

Special Populations

No special population dosage recommendations at this time.1

Cautions for Vismodegib


  • Manufacturer states none known.1



Fetal/Neonatal Morbidity and Mortality

May cause fetal harm, including death or severe birth defects.1 Teratogenicity, embryotoxicity, and fetotoxicity demonstrated in animals.1

Advise male and female patients of risk of embryofetal death and severe birth defects.1 Counsel all patients regarding pregnancy prevention and planning, including need for effective contraception during and after therapy.1

In females with reproductive potential, exclude pregnancy within 7 days before initiating vismodegib.1 Initiate highly effective contraception (i.e., failure rate <1%) prior to first dose; continue during therapy and for 7 months following last dose of drug.1

Advise males of potential to expose females to drug through semen.1 Use of effective barrier methods of contraception (e.g., condoms with spermicide) is recommended for male patients, including those with history of vasectomy, during sexual intercourse with female partners during therapy and for 2 months following last dose of drug.1

If pregnancy occurs or is suspected in female patients during therapy or within 7 months following completion of therapy, or female sexual partners of male patients are exposed to the drug during pregnancy, apprise of potential fetal hazard.1

Report exposure during pregnancy to manufacturer and encourage pregnant women to participate in manufacturer's pregnancy pharmacovigilance program at 888-835-2555.1

Other Warnings/Precautions

Blood Donation

Patients should not donate blood or blood components while receiving vismodegib and for at least 7 months following last dose of drug.1

Specific Populations


Category D.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)


Not known whether vismodegib is distributed into milk.1 Discontinue nursing or the drug.1

Pediatric Use

Safety and efficacy not established.1

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.1

Hepatic Impairment

Safety and efficacy not established.1

Renal Impairment

Safety and efficacy not established.1

Common Adverse Effects

Muscle spasms, alopecia, dysgeusia, weight loss, fatigue, nausea, diarrhea, decreased appetite, constipation, arthralgia, vomiting, ageusia.1 7

Amenorrhea of unknown reversibility also reported.1

Interactions for Vismodegib

Minimally metabolized by CYP2C9 and 3A4/5.1

Inhibitor of CYP2C8, 2C9, and 2C19; does not induce CYP1A2, 2B6, or 3A4/5.1

Substrate of P-glycoprotein (P-gp).1

Inhibitor of breast cancer resistance protein (BCRP).1

Drugs Affecting Hepatic Microsomal Enzymes

Pharmacokinetic interactions unlikely when used concomitantly with drugs that induce or inhibit CYP isoenzymes.1

Inhibitors of P-glycoprotein Transport

Potential increased vismodegib exposure and toxicity.1

Drugs Transported by Breast Cancer Resistance Protein

Potential for increased plasma concentration of drugs transported by BCRP.1 11

Drugs Affecting Gastric Acidity

Potential for decreased vismodegib exposure.1 Clinical data are lacking, but increased dosages of vismodegib unlikely to overcome interaction.1 Effect of concomitant use on efficacy of vismodegib unknown.1

Specific Drugs





Possible reduced bioavailability of vismodegib1

Unknown effect on efficacy of vismodegib1

Increased vismodegib dosages unlikely to overcome interaction1


Pharmacokinetic interaction unlikely1


Pharmacokinetic interaction unlikely1

Histamine H2-receptor antagonists

Possible reduced bioavailability of vismodegib1

Unknown effect on efficacy of vismodegib1

Increased vismodegib dosages unlikely to overcome interaction1

Hormonal contraceptives

Ethinyl estradiol and norethindrone: Pharmacokinetic interaction not observed1

Macrolides (azithromycin, clarithromycin, erythromycin)

Possible increased exposure (via P-gp inhibition by macrolides) to vismodegib and increased risk for toxicity1


Pharmacokinetic interaction unlikely1


Pharmacokinetic interaction unlikely1

Proton-pump inhibitors

Possible reduced bioavailability of vismodegib1

Unknown effect on efficacy of vismodegib1

Increased vismodegib dosages unlikely to overcome interaction1


Pharmacokinetic interaction not observed1

Vismodegib Pharmacokinetics



Absolute bioavailability: 31.8%.1

Saturable absorption; increase in exposure not observed with doses >150 mg.1 3 5


Steady-state exposure not affected by food.1

Special Populations

Pharmacokinetics not studied in renal or hepatic impairment.1

Population pharmacokinetic analyses indicate that weight (41–140 kg), age (26–89 years), Clcr (30–80 mL/min), and gender do not have clinically meaningful effects on systemic exposure.1



Not known if distributed into milk.1

Plasma Protein Binding

>99%; binds albumin and α1-acid glycoprotein (saturable).1 4



Undergoes oxidation, glucuronidation, and pyridine ring cleavage; oxidative metabolites produced by CYP2C9 and 3A4/5.1

Elimination Route

Excreted unchanged and as metabolites primarily in feces (82%) and to a lesser extent in urine (4.4%).1


4 days following continuous once-daily dosing.1

12 days following a single dose.1





20–25°C (may be exposed to 15–30°C).1


  • Inhibits the hedgehog pathway by binding to and inhibiting smoothened, a transmembrane protein involved in hedgehog signal transduction.1

  • In patients with metastatic or locally advanced basal cell carcinoma, therapy associated with tumor regression, stable disease, and down-regulation of glioma-associated protein 1 (GLI1) in normal skin and hair follicles. 1 3 5 6

Advice to Patients

  • Importance of patients reading medication guide before initiation of therapy and each time prescription is refilled.2

  • Importance of women informing their clinician if they are or plan to become pregnant.1 2 Advise patients to contact their clinician immediately if pregnancy is confirmed or suspected; advise pregnant women of risk to the fetus.1 2

  • Importance of both women and men using effective contraception during therapy. 1 2 Advise women to avoid pregnancy during and for at least 7 months after therapy with the drug.1 2 Advise men to use condoms with spermicide during and for at least 2 months after therapy with the drug.1 2

  • Importance of women informing clinicians immediately if they are breast-feeding or plan to breast-feed.1 2 Advise women of the potential for serious adverse reactions from the drug in nursing infants.1

  • Importance of patients not donating blood or blood components while receiving vismodegib and for at least 7 months after discontinuance.1 2

  • Advise patients to swallow capsules whole and not to crush or open capsules.1 2

  • Advise patients not to replace any missed doses and to resume regular dosing schedule after a missed dose.1 2

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.1 2

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Distribution is restricted.10 (See Restricted Distribution Program under Dosage and Administration.)



Dosage Forms


Brand Names




150 mg



AHFS DI Essentials. © Copyright, 2016, American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

Date published: October 31, 2012
Last reviewed: October 31, 2012
Date modified: February 08, 2016


1. Genentech USA, Inc. Erivedge (vismodegib) capsules prescribing information. South San Francisco, CA. 2012 Jan.

2. Genentech USA, Inc. Erivedge (vismodegib) capsules medication guide. South San Francisco, CA. 2012 Jan.

3. Von Hoff DD, LoRusso PM, Rudin CM et al. Inhibition of the hedgehog pathway in advanced basal-cell carcinoma. N Engl J Med. 2009; 361:1164-72. [PubMed 19726763]

4. Graham RA, Lum BL, Cheeti S et al. Pharmacokinetics of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with locally advanced or metastatic solid tumors: the role of alpha-1-acid glycoprotein binding. Clin Cancer Res. 2011; 17:2512-20. [PubMed 21300760]

5. LoRusso PM, Rudin CM, Reddy JC et al. Phase I trial of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with refractory, locally advanced or metastatic solid tumors. Clin Cancer Res. 2011; 17:2502-11. [PubMed 21300762]

6. Dierks C. GDC-0449--targeting the hedgehog signaling pathway. Recent Results Cancer Res. 2010; 184:235-8. [PubMed 20072843]

7. Sekulic A, Migden MR, Oro AE et al. Efficacy and safety of vismodegib in advanced basal-cell carcinoma. N Engl J Med. 2012; 366:2171-9. [PubMed 22670903]

8. Therasse P, Arbuck SG, Eisenhauer EA et al. New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada. J Natl Cancer Inst. 2000; 92:205-16. [PubMed 10655437]

9. Genentech, Inc., South San Francisco, CA. Personal Communications.

10. Genentech USA, Inc. Get started: For healthcare professionals. South San Francisco, CA. Accessed 2012 May 7.

11. Huang SM, Strong JM, Zhang L et al. New era in drug interaction evaluation: US Food and Drug Administration update on CYP enzymes, transporters, and the guidance process. J Clin Pharmacol. 2008; 48:662-70. [PubMed 18378963]