Zefinib

Gefitinib is a kinase inhibitor.

The chemical name of gefitinib is

4-Quinazolinamine N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl) propoxy]

Gefitinib has the molecular formula

C22H24ClFN4O3

a relative molecular mass of 446.9 daltons and is a white-colored powder.

Gefitinib is a free base.

The molecule has pKas of

• 5.4

• 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

• Slightly soluble in methanol, ethanol (99.5%), ethyl acetate, propan-2-ol and acetonitrile

Gefitinib is indicated as monotherapy for the treatment of patients with locally advanced or metastatic non small cell lung cancer after failure of both platinum based and docetaxel chemotherapies.

The effectiveness of Gefitinib is based on objective response rates.

There are no controlled trials demonstrating a clinical benefit, such as improvement in disease-related symptoms or increased survival.

Results from two large, controlled, randomized trials in first-line treatment of non-small cell lung cancer showed no benefit from adding Gefitinib to doublet, platinum based chemotherapy.

Therefore, Gefitinib is not indicated for use in this setting.

Usage

Gefitinib is used to treat metastatic (cancer that has already spread) non-small cell lung cancer in patients who have certain types of abnormal epidermal growth factor (EGFR) genes, and did not receive cancer medicines in the past.

Your doctor will perform a test before you take this medicine.

In preclinical testing, oral gefitinib inhibited the growth of NSCLC tumors that express the epidermal growth factor receptor (EGFR), a mediator of cell signaling, and phase 1 trials have demonstrated that a fraction of patients with NSCLC progressing after chemotherapy experience both a decrease in lung cancer.

• Read the label carefully before use.

• Keep out of the reach of children.

• Protect from Light.

Patient Selection

Select patients for the first-line treatment of metastatic NSCLC with IRESSA based on the presence of EGFR exon 19 deletions or exon 21 L858R mutations in their tumor or plasma specimens.

If these mutations are not detected in a plasma specimen, test tumor tissue if feasible.

Recommended Dose

The recommended dose of IRESSA is 250 mg orally once daily with or without food until disease progression or unacceptable toxicity.

Do not take a missed dose within 12 hours of the next dose.

Administration To Patients Who Have Difficulty Swallowing Solids

Immerse Zefinib tablets in 4 to 8 ounces of water by dropping the tablet in water, and stir for approximately 15 minutes.

Immediately drink the liquid or administer through a naso-gastric tube.

Rinse the container with 4 to 8 ounces of water and immediately drink or administer through the naso-gastric tube.