Pertuzumab

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Information about Pertuzumab

Pertuzumab is a humanized monoclonal antibody to the human epidermal growth factor receptor 2 (HER2) which is used in combination with other antineoplastic agents in the therapy of refractory, advanced breast cancer.

Liver safety of Pertuzumab

Pertuzumab has been implicated in rare instances of transient, occasionally marked serum enzyme elevations, but has not been linked to instances of clinically apparent liver injury with jaundice.

Mechanism of action of Pertuzumab

Pertuzumab (per tooz’ ue mab) is humanized monoclonal antibody to HER2 which is a growth factor receptor that is overexpressed in 20% to 25% of breast cancers. The interaction of epidermal growth factor (EGF) with HER2 results in rapid cell growth and proliferation via intracellular pathways that include MAP and PI3 kinase. Blockage of this pathway results in cell cycle arrest and cell death. Pertuzumab binds to the dimerization site on the HER2 receptor and prevents pairing of receptors and blocks their intracellular signaling. Because the binding site for pertuzumab is different from that of trastuzumab (another monoclonal antibody to HER2), they can be used together and are believed to have additive antitumor effects.

FDA approval information for Pertuzumab

Pertuzumab in combination with trastuzumab and docetaxel has been shown to increase the rate of pathological complete responses in women with advanced HER2 positive breast cancer and it was approved for this indication in 2012.

Dosage and administration for Pertuzumab

Pertuzumab is available in multiple use vials of 420 mg under the brand name Perjeta. The typical dose is 840 mg intravenously initially, followed by 420 mg every three weeks.

Side effects of Pertuzumab

Common side effects include diarrhea, nausea, fatigue, rash, abdominal pain and cardiac dysfunction. Rare, but serious side effects include infusion reactions (usually with the initial dose), cardiomyopathy (especially when combined with an anthracycline), pneumonitis and fetal toxicity.

 


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