Vismodegib


Concise Prescribing Info
Indications/Uses
Locally advanced or metastatic basal cell carcinoma.
Dosage/Direction for Use
Adult : PO 150 mg once daily until disease progression or unacceptable toxicity.
Dosage Details
Oral
Locally advanced basal cell carcinoma, Metastatic basal cell carcinoma
Adult: 150 mg once daily until disease progression or unacceptable toxicity. If a dose is missed, skip the missed dose and wait until the next scheduled dose.
Administration
May be taken with or without food.
Contraindications
Pregnancy and lactation.
Special Precautions
Severe renal impairment.
Adverse Reactions
Significant: Amenorrhea, nausea, vomiting, diarrhoea, constipation, abdominal pain, decreased appetite, premature fusion of epiphyses in paediatric patients.
Gastrointestinal disorders: Dysgeusia, ageusia, hypogeusia, dyspepsia.
General disorders and administration site conditions: Fatigue, pain asthenia.
Investigations: Weight loss, increased hepatic enzymes, increased blood creatinine phosphokinase.
Metabolism and nutrition disorders: Dehydration.
Musculoskeletal and connective tissue disorders: Muscle spasm, arthralgia, pain in extremity, back pain, chest pain, myalgia, flank pain.
Skin and subcutaneous tissue disorders: Alopecia, pruritus, rash, madarosis, abnormal hair growth.
Patient Counseling Information
Avoid blood or sperm donation during therapy and for at least 24 months or 3 months, respectively, following drug discontinuation.
MonitoringParameters
Perform pregnancy test within 1 week prior to initiation of therapy and monthly thereafter.
Drug Interactions
Decreased plasma concentration and decreased efficacy with CYP enzyme inducers (e.g. rifampicin, carbamazepine, phenytoin). May increase the exposure of BCRP substrates (e.g. sulfasalazine, rosuvastatin, topotecan) and OATP1B1 substrates (e.g. repaglinide, bosentan, valsartan, statins).
Food Interaction
Decreased plasma concentration with St John’s wort, avoid concomitant use.
Action
Description: Vismodegib inhibits hedgehog pathway signalling by binding to and inhibiting Smoothened homologue (SMO) transmembrane protein, thereby blocking the activation and nuclear localisation of Glioma-Associated Oncogene (GLI) transcription factors, and the induction of hedgehog target genes which are involved in the proliferation, survival and differentiation of basal cancer cells.
Pharmacokinetics:
Absorption: Absorbed from the gastrointestinal tract. Absolute bioavailability: Approx 32%. Time to peak plasma concentration: Approx 2-4 days.
Distribution: Volume of distribution: 16.4-26.6 L. Plasma protein binding: >99%, mainly to albumin and alpha1-acid glycoprotein.
Metabolism: Metabolised in the liver via oxidation, glucuronidation and pyridine ring cleavage.
Excretion: Mainly via faeces (approx 82%); urine (approx 4.4%). Elimination half-life: Approx 12 days (single dose); approx 4 days (continuous daily dosing).
Chemical Structure

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Storage
Store between 20-25°C. Protect from moisture.
This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
ATC Classification
L01XX43 - vismodegib ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
Disclaimer: This information is independently developed by MIMS based on Vismodegib from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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