gefitinib

medtigo

gefitinib

Brand Name :

Iressa

Synonyms :

gefitinib

Class :

Antineoplastics and EGFR Inhibitors

Action and Spectrum

Actions:

Inhibition of EGFR signaling: gefitinib specifically binds to the ATP-binding site of the EGFR tyrosine kinase, blocking its activity and downstream signaling pathways that promote cell growth and survival.
Anti-tumor activity: By inhibiting EGFR signaling, gefitinib can reduce the proliferation and survival of cancer cells, resulting in anti-tumor activity.
Reversal of drug resistance: gefitinib has been shown to reverse resistance to other chemotherapy drugs in NSCLC cells that have acquired resistance to chemotherapy.

Spectrum:

The spectrum of gefitinib activity is primarily in treating advanced or metastatic NSCLC with specific EGFR mutations. gefitinib is indicated for the first-line treatment of NSCLC with exon 19 deletions or exon 21 (L858R) substitution mutations in the EGFR gene. It is also indicated for the treatment of NSCLC that has progressed after prior chemotherapy, regardless of EGFR mutation status.

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency defined:

>10%

Skin reactions

Diarrhea

Decreased appetite

Vomiting

Increased ALT

1-10%

Increased AST

Stomatitis

Conjunctivitis

Increased ALT

Nail disorders

Diarrhea

Increased AST

Increased bilirubin

Decreased appetite

Skin reactions

Interstitial lung disease

Vomiting

<1%

Interstitial lung disease

Increased bilirubin

Stomatitis

Corneal erosion and aberrant eyelash growth

Nail disorders

Gastrointestinal perforation

Ocular keratitis

Erythema multiforme and dermatitis bullous

Fatal hepatoxicity

Black Box Warning

Contraindication / Caution

Contraindication/Caution:

Contraindication:

The drug is contraindicated in patients who are hypersensitive to it

Caution:

Interstitial lung disease: gefitinib has been associated with interstitial lung disease, a severe and potentially fatal side effect. Patients should be monitored for cough, fever, and dyspnea symptoms and discontinue the treatment if interstitial lung disease is suspected.
Hepatic impairment: gefitinib is metabolized by the liver, so patients with severe hepatic impairment should be monitored closely for adverse effects.
Renal impairment: There is limited data on using gefitinib in patients with severe renal impairment, so caution should be exercised when using this medication in this population.

Pregnancy / Lactation

Pregnancy consideration: The drug is unsafe for pregnant women and the developing fetus.

Lactation: No data on the excretion of gefitinib in breast milk is available. Hence, potential adverse effects and potential benefits should be compared and considered.

Pregnancy category:

Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.
Category B: There is no affirmation of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women.
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a product in humans; Pregnant women must take care of the potential risks.
Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh risks over benefits. The drug is not for pregnant women.
Category N: No data is available for the drug under this category.

Pharmacology

Pharmacology:

gefitinib blocks the intracellular tyrosine kinase domain of EGFR, preventing the activation of downstream signaling pathways involved in tumor cell proliferation and survival. The drug binds reversibly to the ATP binding site of EGFR, inhibiting its autophosphorylation and downstream signaling.

Pharmacodynamics:

gefitinib has been shown to selectively inhibit mutant forms of EGFR found in some types of NSCLC, but it is less effective against wild-type EGFR.

Pharmacokinetics:

Absorption

Mean oral bioavailability is 60%

Peak plasma concentration is achieved in 3-7 hours

Steady state achieved in 10 days

Distribution

Protein-bound is 90%

The volume of distribution is 1400 L

Metabolism

The drug is extensively metabolized predominantly by CYP3A4

Elimination/Excretion

The half-life is 48 hours

The drug is excreted 86% in feces; and less than 4% urine

Adminstartion

Administration:

gefitinib is an oral medication usually administered once daily on an empty stomach. It should be taken at least 1 hour before or 2 hours after a meal. The recommended dose of gefitinib is 250 mg per day, although the HCP must adjust the dose based on individual patient factors such as age, body weight, and renal or hepatic function.

gefitinib tablets should be swallowed whole with water and not crushed or chewed. If a patient misses a dose, they should not take a double dose to make up for the missed one. Instead, they should take the next scheduled dose at the usual time.

Patient Information Leaflet

Patient information leaflet

Generic Name: gefitinib

Pronounced: ge-FI-ti-nib

Why do we use gefitinib?

gefitinib is a medication used in the treatment of certain types of cancer, specifically non-small cell lung cancer (NSCLC). It belongs to a class of drugs called tyrosine kinase inhibitors (TKIs) which work by blocking the action of the epidermal growth factor receptor (EGFR) protein.

It is important to note that gefitinib is not a cure for cancer and may not work for everyone. The healthcare professional should decide the usage of gefitinib or any other medication for cancer treatment.

gefitinib

No data available for drug.

DRUG INTERACTION

gefitinib

&

gefitinib +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

gefitinib

No data available for drug.

DRUG INTERACTION

gefitinib

&

gefitinib +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

gefitinib

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology

Adminstartion

Patient Information Leaflet

CONTACT INFORMATION

ADDRESS

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