Your Health, We Care
Release date: 2026-05-12 15:34:30 Recommended: 5
Palbociclib is primarily metabolized by CYP3A enzymes. Coadministration with strong CYP3A inhibitors should be avoided; if unavoidable, reduce the palbociclib dose to 75 mg, and resume the original dose after discontinuation of the inhibitor (after 3-5 half-lives). Patients should also avoid consuming grapefruit or grapefruit juice. Concurrent use with strong CYP3A inducers should be avoided. For sensitive CYP3A substrates with a narrow therapeutic index, dose reduction may be necessary. For patients with severe hepatic impairment (Child-Pugh Class C), the recommended dose is 75 mg. The pharmacokinetics in patients requiring hemodialysis have not been studied.
Based on its mechanism of action, palbociclib can cause fetal harm. Therefore, females of reproductive potential must use effective contraception during treatment and for at least 3 weeks after the last dose. This drug may also impair male fertility and has genotoxic potential; male patients are advised to consider sperm preservation before treatment. Male patients with female partners of reproductive potential should use effective contraception during treatment and for 3 months after the last dose. Female patients should immediately inform their healthcare provider if they are known or suspected to be pregnant. Additionally, due to the potential for serious adverse reactions in breastfed infants, females should not breastfeed during treatment and for 3 weeks after the last dose.
In the PALOMA-2 study, adverse reactions of any grade occurring at an incidence of ≥10% in the palbociclib plus letrozole arm (compared to placebo plus letrozole) included: neutropenia (80% vs 6%), infections (60% vs 42%), leukopenia (39% vs 2%), fatigue (37% vs 28%), nausea (35% vs 26%), alopecia (33% vs 16%), stomatitis (30% vs 14%), diarrhea (26% vs 19%), anemia (24% vs 9%), rash (18% vs 12%). The most common grade 3 or higher adverse reactions (≥5%) were neutropenia (66% vs 2%), leukopenia (25% vs 0%), infections (7% vs 3%), and anemia (5% vs 2%). In the PALOMA-3 study, the adverse reaction profile was similar, with neutropenia (83% vs 4%) and leukopenia (53% vs 5%) being particularly prominent.
