Palbociclib


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Hormone receptor positive, HER2-negative locally advanced carcinoma of breast; Hormone receptor positive, HER2 negative metastatic carcinoma of breast In combination with aromatase inhibitor, or in combination with fulvestrant in women who have received prior endocrine therapy: 125 mg once daily for 21 days, followed by 7 days off, repeat every 28 days until disease progression or unacceptable toxicity.
Dosage Details
Oral
Hormone receptor positive, HER2-negative locally advanced carcinoma of breast, Hormone receptor positive, HER2-negative metastatic carcinoma of breast
Adult: In combination with aromatase inhibitor, or in combination with fulvestrant in women who have received prior endocrine therapy: 125 mg once daily for 21 days, followed by 7 days off, repeat every 28 days until disease progression or unacceptable toxicity. Pre/perimenopausal women should be treated with luteinising hormone-releasing hormone (LHRH) agonists prior to initiation of treatment and continued throughout the duration of treatment. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guideline). Recommended dose reduction: 1st reduction: 100 mg once daily; 2nd reduction: 75 mg once daily; discontinue if dose reduction below 75 mg once daily is required.
Special Patient Group
Patient taking potent CYP3A inhibitors: Reduce dose to 75 mg once daily for 21 days, followed by 7 days off, repeat every 28 days.
Hepatic Impairment
Severe: Reduce dose to 75 mg once daily for 21 days, followed by 7 days off, repeat every 28 days.
Administration
Hard Capsule: Should be taken with food. Take at the same time each day. Swallow whole, do not chew/crush/open. Avoid grapefruit products.
Contraindications
Pregnancy and lactation.
Special Precautions
Hepatic impairment.
Adverse Reactions
Significant: Bone marrow suppression (e.g. neutropenia, leucopenia, anaemia, thrombocytopenia), infection, diarrhoea, nausea, stomatitis, vomiting.
Eye disorders: Blurred vision, increased lacrimation, dry eye.
Gastrointestinal disorders: Dysgeusia.
General disorders and administration site conditions: Fatigue, asthenia, pyrexia.
Investigations: Increased ALT/AST.
Metabolism and nutrition disorders: Decreased appetite.
Respiratory, thoracic and mediastinal disorders: Epistaxis.
Skin and subcutaneous tissue disorders: Alopecia, rash, dry skin.
Patient Counseling Information
This drug may cause fatigue, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor CBC with differential prior to treatment initiation, every 2 weeks for the 1st 2 cycles, then prior to each cycle, and as clinically indicated. Perform pregnancy test prior to initiation of therapy. Monitor signs and symptoms of infection and pulmonary embolism.
Overdosage
Symptoms: Nausea, vomiting, neutropenia. Management: Supportive treatment.
Drug Interactions
Increased plasma concentration and systemic exposure with strong CYP3A inhibitors (e.g. clarithromycin, telithromycin, itraconazole, ketoconazole, posaconazole, voriconazole, indinavir, ritonavir, ritonavir-boosted lopinavir, nelfinavir, saquinavir, telaprevir, nefazodone, verapamil). Decreased plasma concentration with moderate CYP3A inducers (e.g. bosentan, efavirenz, etravirine, modafinil, nafcillin) or strong CYP3A inducers (e.g. carbamazepine, phenytoin, enzalutamide, rifampicin). May increase the plasma concentration of CYP3A substrates (e.g. ciclosporin, everolimus, sirolimus, tacrolimus, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine).
Food Interaction
Increased exposure with grapefruit or grapefruit juice. Decreased exposure with St John’s wort.
Action
Description: Palbociclib is a reversible, selective inhibitor of cyclin-dependent kinase (CDK) 4 and 6. Cyclin D1, CDK 4 and 6 are downstream of multiple signalling pathways which lead to cellular proliferation. Inhibition of CDK4/6 reduces proliferation of breast cancer cell lines by blocking progression from G1 into S phase of the cell cycle.
Pharmacokinetics:
Absorption: Increased with high fat and high calorie food. Time to peak plasma concentration: Approx 6-12 hours.
Distribution: Volume of distribution: Approx 2,583 L. Plasma protein binding: Approx 85%.
Metabolism: Metabolised in the liver by CYP3A and sulfotransferase (SULT) enzyme 2A1, primarily via oxidation and sulfonation, with acylation and glucuronidation contributing as minor pathway.
Excretion: Mainly via faeces (approx 74%, mainly as metabolites); urine (approx 18%, mainly as metabolites). Elimination half-life: Approx 29 hours.
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store between 20-25°C.
This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
ATC Classification
L01XE33 - palbociclib ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
Disclaimer: This information is independently developed by MIMS based on Palbociclib from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in