Tyrosine Kinase Inhibitors

Kinase Inhibitor

Cytochrome P450 3A Inducers

Carcinoma, Non-Small-Cell Lung

<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">Brigatinib is a kinase inhibitor. The chemical name for brigatinib is 5-chloro-N<span class="Sup">4</span>-[2-(dimethylphosphoryl)phenyl]-N<span class="Sup">2</span>-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidine-2,4-diamine. The molecular formula is C<span class="Sub">29</span>H<span class="Sub">39</span>ClN<span class="Sub">7</span>O<span class="Sub">2</span>P which corresponds to a formula weight of 584.10 g/mol. Brigatinib has no chiral centers. The chemical structure is shown below:</p><div class="Figure"><img alt="Chemical Structure" src="alunbrig-01.jpg"/></div><p>Brigatinib is an off-white to beige/tan solid. The pK<span class="Sub">a</span>s were determined to be: 1.73 ± 0.02 (base), 3.65 ± 0.01 (base), 4.72 ± 0.01 (base), and 8.04 ± 0.01 (base).</p><p>ALUNBRIG is supplied for oral use as film-coated tablets containing 180 mg, 90 mg or 30 mg of brigatinib and the following inactive ingredients: lactose monohydrate, microcrystalline cellulose, sodium starch glycolate (Type A), magnesium stearate, and hydrophobic colloidal silica. The tablet coating consists of talc, polyethylene glycol, polyvinyl alcohol, and titanium dioxide.</p></section>

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