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Abemaciclib

Selective CDK4/6 inhibitor (antineoplastic) · Antineoplastic

START
150 mg PO twice daily (with endocrine therapy)
TYPICAL MAX
300 mg/day (150 mg once daily in severe hepatic)
STOP IF
Severe diarrhoea unresponsive, ILD/pneumonitis, or grade 3 hepatotoxicity
WATCH
CBC at baseline/q2w ×2 cycles then monthly, LFTs, diarrhoea management, VTE
CDSCO approvedSchedule HATC L01EF03
Dose laddermg/d
100reduced200intermediate300standard/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo adjustment30CAUTIONNot studied — caution90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
2hONSET8hPEAK1d12hDURATION
ONSET
2h · absorption
PEAK
8h · Tmax
1d ·
DURATION
12h · twice-daily
EXCRETION
~81% faecal; ~3% renal
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Can cause fetal harm — avoid; effective contraception during and 3 weeks after.
FDA category + note
Top interactionssee all 12
  • AdalimumabSevereDatabaseDDInter
  • ApalutamideSevereDatabaseDDInter
  • AtazanavirSevereDatabaseDDInter
  • BaricitinibSevereDatabaseDDInter

Mechanism

Selective ATP-competitive inhibitor of cyclin-dependent kinases 4 and 6, blocking Rb phosphorylation and arresting hormone-receptor-positive breast cancer cells in G1; continuous dosing distinguishes it from palbociclib/ribociclib.

Indications

HR-positive HER2-negative advanced breast cancer (with endocrine therapy)Adjuvant therapy of node-positive HR-positive HER2-negative early breast cancer (with endocrine therapy)

Dosing

Adult
Advanced: 150 mg PO twice daily with endocrine therapy. Early-disease adjuvant: 150 mg PO twice daily for 2 years.
Pediatric
Not established.
Renal adjustment
No adjustment for CrCl ≥30; severe (CrCl <30) not studied.
Hepatic adjustment
Severe (Child-Pugh C): reduce to 150 mg once daily.
Geriatric
No specific adjustment.
Max dose
300 mg/day (150 mg twice daily)

Pharmacokinetics

Onset
Tumour effect over weeks
Peak effect
~8 h (Tmax)
Duration
~12 h (twice-daily)
Half-life
~18–38 h (active metabolites)
Bioavailability
~45%; food does not significantly affect
Protein binding
~95%
Metabolism
Hepatic CYP3A4 (active M2/M20 metabolites)
Excretion
~81% faecal; ~3% renal

Contraindications

  • Severe hypersensitivity
  • Caution: pregnancy, significant hepatic impairment, active infection

Side effects

Common
DiarrhoeaFatigueNeutropeniaNauseaAbdominal painAnaemia
Serious
  • Severe diarrhoea / dehydration
  • Severe neutropenia
  • Interstitial lung disease / pneumonitis
  • Hepatotoxicity
  • Venous thromboembolism

Pregnancy & lactation

Pregnancy

Can cause fetal harm — avoid; effective contraception during and 3 weeks after.

Lactation

Avoid breastfeeding during and 3 weeks after therapy.

Drug interactions

Adalimumab
Severe
Database

Drug interaction classified as: synergy

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

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

Clarithromycin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Clozapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cobicistat
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

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Sources: Goodman & Gilman 14e, Harrison 22e, Katzung, BNF·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20