Cyp3a Inhibitors
Severe
Textbook
Markedly increased exposure to palbociclib (by 87% with itraconazole).
Avoid concomitant use. If coadministration cannot be avoided, the dose of palbociclib should be reduced.
Source: G&G 14e · p1394
Drug reference
Palbociclib
Tyrosine Kinase Inhibitor · Antineoplastic
Tyrosine Kinase InhibitorAntineoplasticATC null
CDSCO approvedSchedule H
EXCRETION
—
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
X
FDA category + note
Top interactionssee all 12 →
- Cyp3a InhibitorsSevereTextbookG&G 14e · p1394
- AdalimumabSevereDatabaseDDInter
- AmprenavirSevereDatabaseDDInter
- ApalutamideSevereDatabaseDDInter
Mechanism
Palbociclib is a cyclin-dependent kinase (CDK) 4/6 inhibitor. By selectively inhibiting CDK4 and CDK6, it blocks cell cycle progression from G1 phase to S phase, thereby impeding the proliferation of cancer cells.
Indications
Treating hormone receptor-positive, HER2-negative, advanced breast cancer (when combined with fulvestrant)As first-line or subsequent therapy when combined with fulvestrant (for hormone receptor-positive, HER2-negative advanced breast cancer)breast canceradvanced or metastatic breast cancer that is estrogen receptor (ER) positive and HER2 negative (in combination with letrozole as initial endocrine-based therapy or with fulvestrant in women with disease progression after endocrine-based therapy)Used for 2 years (did not improve outcomes in adjuvant setting compared to other CDK4/6 inhibitors)For ER-positive metastatic breast cancer in combination with endocrine therapy
Dosing
- Adult
- HR+/HER2- breast cancer: 125 mg OD for 21 consecutive days of repeated 28-day cycles, with letrozole or fulvestrant.
Pharmacokinetics
Half-life
29 h (mean plasma elimination)
Metabolism
CYP3A (substrate and inhibitor); SULT2A1 (participates)
Side effects
Common
neutropenialeukopeniainfectionsstomatitisfatiguenauseaanemiaheadachediarrheathrombocytopenia
Pregnancy & lactation
Pregnancy
X
Drug interactions
Adalimumab
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Amprenavir
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Apalutamide
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Atazanavir
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Baricitinib
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Berotralstat
Severe
Database
Drug interaction classified as: absorption
Source: DDInter
Boceprevir
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Carbamazepine
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Ceritinib
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Certolizumab
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Cladribine
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Related guidelines
Other Tyrosine Kinase Inhibitor drugs
Ask House about Palbociclib
Continue into a citation-backed clinical answer with the drug context already attached.
Sources: Goodman & Gilman 14e, Harrison 22e, BNF·Verified: 2026-05-10 · House clinical team