Cytochrome P450 2B6 Inhibitors

Cytochrome P450 3A Inhibitors

Kinase Inhibitor

Organic Cation Transporter 1 Inhibitors

Organic Cation Transporter 2 Inhibitors

P-Glycoprotein Inhibitors

Receptor Tyrosine Kinase Inhibitors

Non-Small-Cell Lung Carcinoma

<section class="Section" data-sectioncode="34089-3"><a name="S11"></a><a name="section-9"></a><p></p><h1>11 DESCRIPTION</h1><p class="First">Crizotinib is a kinase inhibitor. The molecular formula for crizotinib is C<span class="Sub">21</span>H<span class="Sub">22</span>Cl<span class="Sub">2</span>FN<span class="Sub">5</span>O and the molecular weight is 450.34 daltons. Crizotinib is described chemically as (<span class="Italics">R</span>)-3-[1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)-1<span class="Italics">H</span>-pyrazol-4-yl]pyridin-2-amine.</p><p>The chemical structure of crizotinib is shown below:</p><div class="Figure"><a name="id3040"></a><img alt="Chemical Structure" src="xalkori-01.jpg"/></div><p>Crizotinib is a white to pale-yellow powder with a pKa of 9.4 (piperidinium cation) and 5.6 (pyridinium cation). The solubility of crizotinib in aqueous media decreases over the range pH 1.6 to pH 8.2 from greater than 10 mg/mL to less than 0.1 mg/mL. The log of the distribution coefficient (octanol/water) at pH 7.4 is 1.65.</p><p>XALKORI (crizotinib) for oral administration is supplied as printed hard-shell capsules containing 250 mg or 200 mg of crizotinib together with colloidal silicon dioxide, microcrystalline cellulose, anhydrous dibasic calcium phosphate, sodium starch glycolate, magnesium stearate, and hard gelatin capsule shells as inactive ingredients.</p><p>The pink opaque capsule shell components contain gelatin, titanium dioxide, and red iron oxide. The white opaque capsule shell components contain gelatin and titanium dioxide. The printing ink contains shellac, propylene glycol, strong ammonia solution, potassium hydroxide, and black iron oxide.</p></section>

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