Palbokin 125 mg (Capsule)

Indications

• Indicated for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer
• Used in combination with an aromatase inhibitor as initial endocrine-based therapy in postmenopausal women or with fulvestrant in women with disease progression following endocrine therapy
• Specifically targets ER-positive breast cancer cell lines

Pharmacology

• Inhibitor of Cyclin-dependent kinases (CDK) 4 and 6
• Reduces cellular proliferation of Estrogen receptor (ER)-positive breast cancer cell lines
• Leads to decreased retinoblastoma (RB) protein phosphorylation and increased cell senescence
• Effective in patient-derived ER-positive breast cancer xenograft model

Dosage & Administration

• Recommended dose: 125 mg capsule taken orally once daily for 21 consecutive days followed by 7 days off treatment
• Should be taken with food
• Recommended dose modification for adverse reactions
• Not indicated for use in children

Interaction

• Primarily metabolized by CYP3A and Sulfotransferase (SULT) enzyme SULT2A1
• Avoid concomitant use of strong CYP3A inhibitors and inducers
• May alter plasma concentrations of sensitive CYP3A substrates with narrow therapeutic index

Side Effects

• Common side effects include decreased WBC, neutrophils, and platelets, infections, increased AST and ALT, leukopenia, fatigue, nausea, hair loss, and more

Pregnancy & Lactation

• Can cause fetal harm and risk of major birth defects and miscarriage in pregnant women

Precautions & Warnings

• Neutropenia is the most frequently reported adverse reaction with an incidence of 80%-83%
• Grade 3 neutrophil counts reported in 66% of patients
• Risk of severe, life-threatening ILD/pneumonitis, embryo-fetal toxicity, and febrile neutropenia
• Require monitoring of complete blood counts and pulmonary symptoms

Overdose Effects

• No known antidote. Treatment should consist of general supportive measures

Therapeutic Class

• Protein kinase inhibitor

Storage Conditions

• Keep below 30°C temperature, away from light & moisture
• Keep out of the reach of children

Related Brands

• Palbolib 125 mg (Capsule) - aristopharma-ltd