Palbociclib

Cytostatic · Protein kinase inhibitor

Indications

Hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer. In combination with letrozole for the treatment of postmenopausal women with oestrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer as initial endocrine-based therapy for metastatic disease.

Dosage

Cap/Tab: Adults: Starting dose: 125 mg once daily taken with food for 21 days followed by 7 days off treatment. Dose may be adjusted as required. Children: Not recommended. In combination with a strong CYP3A inhibitor: Reduce the Palbociclib dose to 75 mg once daily. If the strong inhibitor is discontinued, increase the Palbociclib dose (after 3 to 5 half-lives of the inhibitor) to the dose used prior to the initiation of the strong CYP3A inhibitor. As initial endocrine-based therapy in combination with letrozole in postmenopausal women: Starting dose: 125 mg daily with food for 21 days followed by 7 days off therapy to comprise a complete cycle of 28 days. With letrozole 2.5 mg daily continuously throughout the 28-day cycle. Disease progression following endocrine therapy in combination with fulvestrant: Starting dose: 125 mg daily with food for 21 days followed by 7 days off therapy…

Adverse Effects

Neutropenia, leukopenia, infections, fatigue, nausea, anaemia, stomatitis, headache, diarrhoea, thrombocytopenia, constipation, alopecia, vomiting, rash, decreased appetite.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Precautions: Renal or hepatic disease, neutropenia. Monitor complete blood count prior to start of therapy and at the beginning of each cycle, as well as on Day 14 of the first two cycles and as clinically indicated. Infections: Monitor for signs and symptoms and withhold dosing as appropriate. Monitor patients for signs and symptoms of pulmonary embolism. Risk of fetal harm. Advise patients of potential risk to a fetus and to use effective contraception.

Interactions

Strong and moderate CYP3A inducers, strong CYP3A inhibitors. Grapefruit or grapefruit juice.

Pharmacokinetics

Bioavailability: 46%. Metabolism: Extensively hepatic. Half-life elimination: 29 hrs (patients with advanced breast cancer) Time to peak, plasma: 6-12 hrs Excretion: Faeces (74.1%). Urine (17.5%).

Brands with this active ingredient

• Ibrance
• Palbonix

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.