Iressa

gefitinib

(je-fit-in-ib) ,

Iressa

(trade name)

Classification

Therapeutic: antineoplastics
Pharmacologic: enzyme inhibitors
Pregnancy Category: D

Indications

Patients who are currently benefiting from or have benefited from gefitinib in the past for treatment of non–small-cell lung cancer.

Action

genetic implication Inhibits activation of kinases found in transmembrane cell surface receptors, including epidermal growth factor receptor (EGFR-TK).

Therapeutic effects

Death of rapidly replicating cells, particularly malignant ones.

Pharmacokinetics

Absorption: 60% absorbed following oral administration.
Distribution: Extensively distributed.
Metabolism and Excretion: Mostly metabolized by the liver (CYP3A4 enzyme system); excreted in feces, <4% excreted in urine.
Half-life: 48 hr.

Time/action profile

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Contraindications/Precautions

Contraindicated in: Hypersensitivity; Obstetric / Lactation / Pediatric: Pregnancy, lactation, children.
Use Cautiously in: Idiopathic pulmonary fibrosis (↑ risk of pulmonary toxicity);Concurrent use of strong inhibitors of the CYP3A4 enzyme system (may ↑ risk of toxicity).

Adverse Reactions/Side Effects

Central nervous system

  • weakness

Ear, Eye, Nose, Throat

  • aberrant eyelash
  • conjunctivitis
  • corneal erosion/ulcer
  • eye pain
  • ↓ vision

Cardiovascular

  • peripheral edema

Respiratory

  • pulmonary toxicity (life-threatening)
  • dyspnea

Gastrointestinal

  • diarrhea (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)
  • anorexia
  • hepatotoxicity
  • mouth ulceration

Dermatologic

  • acne (most frequent)
  • dry skin (most frequent)
  • rash (most frequent)
  • pruritus

Metabolic

  • weight loss

Miscellaneous

  • allergic reactions including angioedema (life-threatening)

Interactions

Drug-Drug interaction

Strong inducers of the CYP3A4 enzyme system, including rifampin and phenytoin, ↓ blood levels and effects (consider ↑ dose of gefitinib to 500 mg/day).Strong inhibitors of the CYP3A4 enzyme system, including ketoconazole and itraconazole, ↑ blood levels and effects (use with caution).Absorption and efficacy may be ↓ by drugs that ↑ gastric pH including cimetidine and ranitidine.May ↑ the risk of bleeding with warfarin.Concurrent use with vinorelbine may ↑ risk/severity of neutropenia.

Route/Dosage

Oral (Adults) 250 mg once daily.

Availability

Tablets: 250 mg

Nursing implications

Nursing assessment

  • Assess for signs of pulmonary toxicity (dyspnea, cough, fever). If interstitial lung disease is confirmed, discontinue gefitinib and treat appropriately.
  • Assess patient for eye symptoms such as pain during therapy. May require interruption of therapy and removal of aberrant eyelash. After symptoms and eye changes have resolved, may reinstate therapy.
  • Lab Test Considerations: Monitor liver function tests periodically. May cause ↑ transaminases, bilirubin, and alkaline phosphatase. Discontinue gefitinib if elevations are severe.
    • Monitor for changes in prothrombin time and INR in patients taking warfarin. May cause ↑ levels.

Potential Nursing Diagnoses

Diarrhea (Adverse Reactions)
Impaired skin integrity (Side Effects)
Ineffective breathing pattern (Adverse Reactions)

Implementation

  • Available only through the Iressa Access Program. Patients must be currently on the medication or in an approved study and must sign the Patient Consent Form. Physicians and prescribers must enroll in program.
  • Oral: Administer one tablet daily without regard to food. Tablets can also be dispersed in half a glass of drinking water (noncarbonated). No other liquids should be used. Drop the tablet in the water, without crushing it, stir until the tablet is dispersed (approximately 10 min), and drink the liquid immediately. Rinse the glass with half a glass of water and drink. The liquid can also be administered through a nasogastric tube.
    • May interrupt therapy briefly (14 days) for patients with poorly tolerated diarrhea with dehydration or skin adverse reactions. Follow by restarting 250 mg dose.

Patient/Family Teaching

  • Instruct patient to take gefitinib as directed. Advise patient to read the Instruction Sheet with each Rx refill; new information may be available.
  • Advise patient to notify health care professional promptly if severe persistent diarrhea, nausea, vomiting, or anorexia occur; if shortness of breath or cough occur or worsen; or if eye irritation or other new symptoms develop.
  • Instruct patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Decrease in size and spread of tumors in non–small-cell lung cancer.
Drug Guide, © 2015 Farlex and Partners
References in periodicals archive ?
The TKIs for lung cancer include drugs such as afatinib (Gilotrif), crizotinib (Xalkori), erlotinib (Tarceva) and gefitinib (Iressa).
He spent over 12 years at AstraZeneca, where he was VP and head Oncology and Infection, during which time he was responsible for the development of Iressa (gefitinib) for non-small cell lung cancer (NSCLC) and the translational research that resulted in the successful personalised medicine strategy for AstraZeneca.
The global lung cancer therapeutics market can be segmented as follows: By Drugs Hycamtin Taxotere Gemzar Alimta Iressa Avastin Tarceva Pipeline Drugs Xalkori Afatinib Dacomitinib ARQ 197 Talactoferrin
While there, Morris also supported early clinical development activities for Iressa and held many leadership positions in the development of various novel targeted pipeline therapeutics for breast, colorectal, prostate and non-small cell lung cancers.
Global Banking News-August 24, 2018-Roche awarded US FDA's approval for cobas EGFR Mutation Test v2 with IRESSA for treating non-small cell lung cancer
Browse Non-Small Cell Lung Cancer (NSCLC) Therapeutics Market by Drug Classes (Angiogenesis Inhibitors - Avastin, Cyramza; Epidermal Growth Factor Receptor Blockers - Tarceva, Gilotrif, Iressa; Folate Antimetabolites - Alimta; Kinase Inhibitors - Xalkori, Zykadia; Microtubule Stabilizers - Abraxane, Docetaxel; and PD-1/ PD-L1 Inhibitors - Opdivo, Keytruda), and Clinical Pipeline Analysis of Phase 1, 2 and 3 Drugs (Avelumab, MPDL3280A, MEDI4736, Abemaciclib) and Forecast 2017-2021 at https://www.ihealthcareanalyst.com/report/non-small-cell-lung-cancer-therapeutics-market/
Lyn is currently undergoing a first line treatment called Iressa which improves quality of life, after being told she couldn't have radiotherapy.
Oncologists currently have at their disposal two EGFR inhibitors: gefitinib (trade name Iressa) and erlotinib (Tarceva).
There were a few bright spots in AZ's newer products: Symbicort sales were up 8% (CER) to $891 million in the quarter, Faslodex sales were up 20% to $175 million, Onglyza sales were up 24%, to $88 million, and Iressa sales were up 10% to $160 million.
An emerging class of drugs called tyrosine kinase inhibitors (TKI)-such as imitinib (Gleevec), gifitinib (Iressa) and sunitinib (Sutent)-has become a popular anticancer treatment.
Two targeted treatments, erlotinib (Tarceva) and gefitinib (Iressa), can dramatically, albeit transiently, reverse EGFR-positive cancers, by blocking the EGFR receptor and thus preventing its activation.