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Gefitinib

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Overview

What is IRESSA?

Gefitinib is a kinase inhibitor.

The chemical name of gefitinib is 4-Quinazolinamine -(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl) propoxy] and the following structural formula:

Gefitinib has the molecular formula CHClFNO, a relative molecular mass of 446.9 daltons and is a white-colored powder. Gefitinib is a free base. The molecule has pKs of 5.4 and 7.2. Gefitinib can be defined as sparingly soluble at pH 1, but is practically insoluble above pH 7, with the solubility decreasing sharply between pH 4 and pH 6. In non-aqueous solvents, gefitinib is freely soluble in glacial acetic acid and dimethyl sulfoxide, soluble in pyridine, sparingly soluble in tetrahydrofuran, and slightly soluble in methanol, ethanol (99.5%), ethyl acetate, propan-2-ol and acetonitrile.

IRESSA (gefitinib) tablets are available as brown film-coated tablets, containing 250 mg of gefitinib, for oral administration. The inactive ingredients of the tablet core of IRESSA tablets are lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, povidone, sodium lauryl sulfate and magnesium stearate. The tablet coating is composed of hypromellose, polyethylene glycol 300, titanium dioxide, red ferric oxide and yellow ferric oxide.



What does IRESSA look like?



What are the available doses of IRESSA?

Tablets: 250 mg.

What should I talk to my health care provider before I take IRESSA?

How should I use IRESSA?

IRESSA is indicated for the first-line treatment of patients with or metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test [].

Limitation of Use: Safety and efficacy of IRESSA have not been established in patients with metastatic NSCLC whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution mutations [].

Select patients for the first-line treatment of metastatic NSCLC with IRESSA based on the presence of EGFR exon 19 deletion or exon 21 (L858R) substitution mutations in their tumor [, ]. Information on FDA-approved tests for the detection of EGFR mutations in NSCLC is available at: .


What interacts with IRESSA?

Sorry No Records found


What are the warnings of IRESSA?

Sorry No Records found


What are the precautions of IRESSA?

Sorry No Records found


What are the side effects of IRESSA?

Sorry No records found


What should I look out for while using IRESSA?

None.


What might happen if I take too much IRESSA?

Twenty three patients were treated weekly with doses from 1500 mgto3500 mg, and IRESSA exposure did not increase with increasing dose. Adverse events were mostly mild to moderate in severity, and were consistent with the known safety profile of IRESSA. In the event of suspected overdose, interrupt IRESSA, institute supportive care, and observe until clinical stabilization. There are no specific measures/treatments that should be taken following IRESSA overdosing.


How should I store and handle IRESSA?

Store at 20° to 25°C (68° to 77°F); excursions permitted from 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. IRESSA(gefitinib) is available as 250 mg tablets.IRESSA 250 mg tablets are round, biconvex, brown film-coated, debossed with "IRESSA 250" on one side and plain on the other side.IRESSA(gefitinib) tablets are supplied as:          Bottles of 30 Tablets (NDC 0310-0482-30) Store at controlled room temperature 20°C-25°C (68°F-77°F) [see]. IRESSA(gefitinib) is available as 250 mg tablets.IRESSA 250 mg tablets are round, biconvex, brown film-coated, debossed with "IRESSA 250" on one side and plain on the other side.IRESSA(gefitinib) tablets are supplied as:          Bottles of 30 Tablets (NDC 0310-0482-30) Store at controlled room temperature 20°C-25°C (68°F-77°F) [see]. IRESSA(gefitinib) is available as 250 mg tablets.IRESSA 250 mg tablets are round, biconvex, brown film-coated, debossed with "IRESSA 250" on one side and plain on the other side.IRESSA(gefitinib) tablets are supplied as:          Bottles of 30 Tablets (NDC 0310-0482-30) Store at controlled room temperature 20°C-25°C (68°F-77°F) [see]. IRESSA(gefitinib) is available as 250 mg tablets.IRESSA 250 mg tablets are round, biconvex, brown film-coated, debossed with "IRESSA 250" on one side and plain on the other side.IRESSA(gefitinib) tablets are supplied as:          Bottles of 30 Tablets (NDC 0310-0482-30) Store at controlled room temperature 20°C-25°C (68°F-77°F) [see]. IRESSA(gefitinib) is available as 250 mg tablets.IRESSA 250 mg tablets are round, biconvex, brown film-coated, debossed with "IRESSA 250" on one side and plain on the other side.IRESSA(gefitinib) tablets are supplied as:          Bottles of 30 Tablets (NDC 0310-0482-30) Store at controlled room temperature 20°C-25°C (68°F-77°F) [see].


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Clinical Information

Chemical Structure

No Image found
Clinical Pharmacology

The epidermal growth factor receptor (EGFR) is expressed on the cell surface of both normal and cancer cells and plays a role in the processes of cell growth and proliferation. Some EGFR activating mutations (exon 19 deletion or exon 21 point mutation L858R) within NSCLC cells have been identified as contributing to the promotion of tumor cell growth, blocking of apoptosis, increasing the production of angiogenic factors and facilitating the processes of metastasis.

Gefitinib reversibly inhibits the kinase activity of wild-type and certain activating mutations of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor, thereby inhibiting further downstream signalling and blocking EGFR-dependent proliferation.

Gefitinib binding affinity for EGFR exon 19 deletion or exon 21 point mutation L858R mutations is higher than its affinity for the wild-type EGFR. Gefitinib also inhibits IGF and PDGF-mediated signalling at clinically relevant concentrations; inhibition of other tyrosine kinase receptors has not been fully characterized. 

Non-Clinical Toxicology
None.

Disulfiram

Psychotic reactions have been reported in alcoholic patients who are using metronidazole and disulfiram concurrently. Metronidazole should not be given to patients who have taken disulfiram within the last two weeks (see ).

Alcoholic Beverages

Abdominal cramps, nausea, vomiting, headaches, and flushing may occur if alcoholic beverages or products containing propylene glycol are consumed during or following metronidazole therapy (see ).

Warfarin and other Oral Anticoagulants

Metronidazole has been reported to potentiate the anticoagulant effect of warfarin and other oral coumarin anticoagulants, resulting in a prolongation of prothrombin time. When metronidazole tablets are prescribed for patients on this type of anticoagulant therapy, prothrombin time and INR should be carefully monitored.

Lithium

In patients stabilized on relatively high doses of lithium, short-term metronidazole therapy has been associated with elevation of serum lithium and, in a few cases, signs of lithium toxicity. Serum lithium and serum creatinine levels should be obtained several days after beginning metronidazole to detect any increase that may precede clinical symptoms of lithium intoxication.

Busulfan

Metronidazole has been reported to increase plasma concentrations of busulfan, which can result in an increased risk for serious busulfan toxicity. Metronidazole should not be administered concomitantly with busulfan unless the benefit outweighs the risk. If no therapeutic alternatives to metronidazole are available, and concomitant administration with busulfan is medically needed, frequent monitoring of busulfan plasma concentration should be performed and the busulfan dose should be adjusted accordingly.

Drugs that Inhibit CYP450 Enzymes

The simultaneous administration of drugs that decrease microsomal liver enzyme activity, such as cimetidine, may prolong the half-life and decrease plasma clearance of metronidazole.

Drugs that Induce CYP450 Enzymes

The simultaneous administration of drugs that induce microsomal liver enzymes, such as phenytoin or phenobarbital, may accelerate the elimination of metronidazole, resulting in reduced plasma levels; impaired clearance of phenytoin has also been reported.

ILD or ILD-like adverse drug reactions (e.g., lung infiltration, pneumonitis, acute respiratory distress syndrome, or pulmonary fibrosis) occurred in 1.3% of the 2462 patients who received IRESSA across clinical trials; of these, 0.7% were Grade 3 or higher and 3 cases were fatal.

Withhold IRESSA and promptly investigate for ILD in any patient who presents with worsening of respiratory symptoms such as dyspnea, cough and fever. Permanently discontinue IRESSA if ILD is confirmed [].

The following adverse drug reactions are discussed in more detail in other sections of the labeling:

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72
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Tips

Tips

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Interactions

Interactions

A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).