Generic
Palbociclib
Indications
Palbociclib is a kinase inhibitor indicated for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer in combination with: An aromatase inhibitor as initial endocrine-based therapy in postmenopausal women; or Fulvestrant in women with disease progression following endocrine therapy.
Dosage Administration
The recommended dose of Palbociclib is a 125 mg capsule taken orally once daily for 21 consecutive days followed by 7 days off treatment to comprise a complete cycle of 28 days. Palbociclib should be taken with food. Patients should be encouraged to take their dose of Palbociclib at approximately the same time each day. For men treated with combination Palbociclib plus aromatase inhibitor therapy, consider treatment with an LHRH agonist according to current clinical practice standards. Recommended Dose Modification for Adverse Reactions: Recommended Starting Dose: 125 mg/day First Dose Reduction: 100 mg/day Second Dose Reduction: 75 mg/day If further dose reduction below 75 mg/day is required, discontinue. Or, as directed by the registered physician. Use in Children: Palbociclib is not indicated for use in children.
Contraindications
There is no known antidote for Palbociclib. The treatment of overdose of Palbociclib should consist of general supportive measures.
Side Effects
Palbociclib is primarily metabolized by CYP3A and Sulfotransferase (SULT) enzyme SULT2A1. Palbociclib is a time-dependent inhibitor of CYP3A. Agents That May Increase Palbociclib Plasma Concentrations: Effect of CYP3A-Inhibitors: Coadministration of a strong CYP3A inhibitor (Itraconazole) increased the plasma exposure of Palbociclib in patients by 87%. Avoid concomitant use of strong CYP3A inhibitors (e.g., Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Lopinavir/Ritonavir, Nefazodone, Nelfinavir, Posaconazole, Ritonavir, Saquinavir, Telaprevir, Telithromycin, And Voriconazole). Avoid grapefruit or grapefruit juice during Palbociclib treatment. If coadministration of Palbociclib with a strong CYP3A inhibitor cannot be avoided, reduce the dose of Palbociclib. Agents That May Decrease Palbociclib Plasma Concentrations: Effect of CYP3A Inducers: Coadministration of a strong CYP3A Inducer (Rifampin) decreased the plasma exposure of Palbociclib in healthy subjects by 85%. Avoid concomitant use of strong CYP3A inducers (E.G., Phenytoin, Rifampin, Carbamazepine, Enzalutamide, and St John�s Wort). Drugs That May Have Their Plasma Concentrations Altered By Palbociclib: Coadministration of Midazolam with multiple doses of Palbociclib increased the Midazolam plasma exposure by 61%, in patients, compared to administration of Midazolam alone. The dose of the sensitive CYP3A substrate with a narrow therapeutic index (e.g., Alfentanil, Cyclosporine, Dihydroergotamine, Ergotamine, Everolimus, Fentanyl, Pimozide, Quinidine, Sirolimus, And Tacrolimus) may need to be reduced, as Palbociclib may increase its exposure.
Pregnancy And Lactation
Common side effects of Palbociclib include: WBC decreased, Neutrophils decreased, Neutropenia, Platelets decreased, infections, AST increased, ALT increased, Leukopenia, Fatigue, Nausea, Hair loss, Inflammation of the mouth and lips, Diarrhea, Anemia, Rash, Weakness/lethargy, Vomiting, Thrombocytopenia, Dry skin, Fever.
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