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A - Regimen Name

GEFI Regimen
Gefitinib


Disease Site
Head and Neck

Intent
Palliative

Regimen Category
Evidence-Informed :

Regimen is considered appropriate as part of the standard care of patients; meaningfully improves outcomes (survival, quality of life), tolerability or costs compared to alternatives (recommended by the Disease Site Team and national consensus body e.g. pan-Canadian Oncology Drug Review, pCODR).  Recommendation is based on an appropriately conducted phase III clinical trial relevant to the Canadian context OR (where phase III trials are not feasible) an appropriately sized phase II trial. Regimens where one or more drugs are not approved by Health Canada for any indication will be identified under Rationale and Use.


Rationale and Uses

For the treatment of recurrent or metastatic squamous cell carcinoma of the head and neck in patients with progressive disease who are unsuitable for platinum-based chemotherapy (not Health Canada approved indication). Note that gefitinib did not improve overall survival compared to methotrexate (Stewart 2009).

 
B - Drug Regimen

gefitinib
250 mg PO Daily
(This drug is not currently publicly funded for this regimen and intent)

(Outpatient prescription available in 250mg tablets)

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C - Cycle Frequency

CONTINUOUS TREATMENT

Until disease progression or unacceptable toxicity.

 
D - Premedication and Supportive Measures

Antiemetic Regimen:

Minimal – No routine prophylaxis; PRN recommended

Other Supportive Care:

Provide patient with loperamide (including instructions) for diarrhea management.

Also refer to CCO Antiemetic Recommendations.

 
E - Dose Modifications

Doses should be modified according to the protocol by which the patient is being treated. The following recommendations have been adapted from clinical trials or product monographs and could be considered.

 

Dosage with toxicity

In a phase III clinical study, doses were held up to 2 weeks in the case of acute toxicities.

Toxicity

Action

Grade 2 skin, eye toxicity, intolerable diarrhea

Hold*, restart at 250mg daily when recovered

Grade 3 skin, eye toxicity, diarrhea, LFTs, dehydration

Hold*, may restart at 250mg daily when recovered

Grade 4 toxicity OR GI perforation OR treatment intolerance despite dose interruption

Discontinue

Keratitis

Hold and investigate. Consider discontinuing if ulcerative.

 

Acute/new or worsening pulmonary symptoms (e.g. dyspnea, cough, fever)

Hold and investigate.  Discontinue if interstitial lung disease confirmed.

*Hold up to 14 days for diarrhea and skin toxicity; if further hold required, discontinue



Hepatic Impairment

Increased gefitinib exposure has been reported in patients with moderate and severe hepatic impairment due to cirrhosis. Dose adjustment is not required, but use with caution and monitor closely. See table above for hepatic toxicity during treatment.

Renal Impairment

No adjustment required in mild or moderate renal impairment; no recommendations found for severe renal impairment.


Dosage in the Elderly

No adjustment required.

Dosage in other populations:

No dose adjustment required based on gender, body weight, or ethnicity.

 
F - Adverse Effects

Refer to gefitinib drug monograph(s) for additional details of adverse effects


Most Common Side Effects 

Less Common Side Effects, but may be
Severe or Life-Threatening

  • Rash (may be severe)
  • Diarrhea (may be severe)
  • Anorexia
  • Nausea, vomiting
  • Insomnia, fatigue
  • Paronychia
  • Mucositis
  • ↑ LFTs (may be severe)
  • Cough, dyspnea (may be severe)
  • Alopecia
  • Constipation
  • Arterial thromboembolism
  • GI perforation
  • Hypersensitivity
  • Pancreatitis
  • Keratitis
  • Nephrotoxicity
  • Bleeding
 
G - Interactions

Refer to gefitinib drug monograph(s) for additional details


  • Avoid use with potent CYP3A4 inducers (e.g. rifampin, phenytoin, St. John's wort) and inhibitors (e.g. diltiazem, erythromycin, Grapefruit juice)
  • Caution and monitor with drugs that increase gastric pH (e.g. proton pump inhibitors, H2-antagonists) as they may reduce gefitinib exposure
  • Caution and monitor for increased risk of bleeding when combined with anticoagulants and/or antiplatelets.
  • Caution and monitor with drugs that are CYP2D6 substrates (e.g. beta-blockers, serotonin H3-antagonists) as they be inhibited by gefitinib
  • Avoid use with vinorelbine given an increased risk of severe neutropenia
 
H - Drug Administration and Special Precautions

Refer to gefitinib drug monograph(s) for additional details


Administration:

  • May be administered with or without food
  • Avoid grapefruit, pomegranate, starfruit, Seville oranges, their juices or products during gefitinib treatment
  • Missed dose should be taken as soon as possible, but only if there are at least 12 hours before the next dose is due. Otherwise, skip and take the next dose as scheduled.

Special precautions:

  • Contains lactose; carefully consider use in patients with hereditary galactose intolerance, severe lactase deficiency or glucose-galactose malabsorption.
  • Risk of mortality among patients who develop interstitial lung disease (ILD) is higher in those who are smokers, have pre-existing ILD or are ≥ 65 years old.
 
I - Recommended Clinical Monitoring

Treating physicians may decide to monitor more or less frequently for individual patients but should always consider recommendations from the product monograph.

Recommended Clinical Monitoring

  • Liver function tests; baseline and at each visit
  • Renal function tests, including electrolytes, especially in patients at high risk of dehydration; baseline and at each visit
  • INR in patients on warfarin; baseline and when gefitinib is held or discontinued
  • Clinical toxicity assessment of GI, skin, eye and respiratory symptoms; at each visit
  • Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version


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J - Administrative Information

Outpatient prescription for home administration


 
K - References

Gefitinib drug monograph, Cancer Care Ontario.

Stewart JS, Cohen EE, Licitra L, et al. Phase III study of gefitinib compared with intravenous methotrexate for recurrent squamous cell carcinoma of the head and neck. J Clin Oncol. 2009 Apr 10;27(11):1864-71.

August 2019 removed archived PEBC guideline links


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M - Disclaimer

Regimen Abstracts
A Regimen Abstract is an abbreviated version of a Regimen Monograph and contains only top level information on usage, dosing, schedule, cycle length and special notes (if available). It is intended for healthcare providers and is to be used for informational purposes only. It is not intended to constitute or be a substitute for medical advice, and all uses of the Regimen Abstract are subject to clinical judgment. Such information is provided on an “as-is” basis, without any representation, warranty, or condition, whether express, or implied, statutory or otherwise, as to the information’s quality, accuracy, currency, completeness, or reliability, and Cancer Care Ontario disclaims all liability for the use of this information, and for any claims, actions, demands or suits that arise from such use.
Information in regimen abstracts is accurate to the extent of the ST-QBP regimen master listings, and has not undergone the full review process of a regimen monograph.  Full regimen monographs will be published for each ST-QBP regimen as they are developed.
Regimen Monographs
Refer to the New Drug Funding Program or Ontario Public Drug Programs websites for the most up-to-date public funding information.
The information set out in the drug monographs, regimen monographs, appendices and symptom management information (for health professionals) contained in the Drug Formulary (the "Formulary") is intended for healthcare providers and is to be used for informational purposes only. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects of a particular drug, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for a given condition. The information in the Formulary is not intended to constitute or be a substitute for medical advice and should not be relied upon in any such regard. All uses of the Formulary are subject to clinical judgment and actual prescribing patterns may not follow the information provided in the Formulary.
The format and content of the drug monographs, regimen monographs, appendices and symptom management information contained in the Formulary will change as they are reviewed and revised on a periodic basis. The date of last revision will be visible on each page of the monograph and regimen. Since standards of usage are constantly evolving, it is advised that the Formulary not be used as the sole source of information. It is strongly recommended that original references or product monograph be consulted prior to using a chemotherapy regimen for the first time.
Some Formulary documents, such as the medication information sheets, regimen information sheets and symptom management information (for patients), are intended for patients. Patients should always consult with their healthcare provider if they have questions regarding any information set out in the Formulary documents.
While care has been taken in the preparation of the information contained in the Formulary, such information is provided on an “as-is” basis, without any representation, warranty, or condition, whether express, or implied, statutory or otherwise, as to the information’s quality, accuracy, currency, completeness, or reliability.
CCO and the Formulary’s content providers shall have no liability, whether direct, indirect, consequential, contingent, special, or incidental, related to or arising from the information in the Formulary or its use thereof, whether based on breach of contract or tort (including negligence), and even if advised of the possibility thereof. Anyone using the information in the Formulary does so at his or her own risk, and by using such information, agrees to indemnify CCO and its content providers from any and all liability, loss, damages, costs and expenses (including legal fees and expenses) arising from such person’s use of the information in the Formulary.