Abemaciclib

VERZENIO

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Pronunciation: a-bem-a-SYE-klib (ver-ZEN-ee-oe)

Abemaciclib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Abemaciclib ballicule

Abemaciclib VERZENIO mascot mnemonic cartoon — Visual mnemonic: Abemaciclib mascot
**“Abe clips Verizon, yo”**

What it isCDK4/6 inhibitor; hormone receptor-positive HER2-negative breast cancer.

Why this oneIt is the only CDK4/6 inhibitor with a monotherapy indication and is given continuously rather than cyclically.

What limits itDiarrhea is its dose-limiting signature; treat at the first loose stool. Venous thromboembolism and CYP3A4 interactions also matter.

Abemaciclib molecular structure (skeletal formula) — Molecular structure: Abemaciclib

FDA-approved for

HR-positive HER2-negative breast cancer (2017)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
HR+/HER2− breast cancer — with endocrine therapy (fulvestrant, tamoxifen, or an aromatase inhibitor)	adult	150 mg BID	150 mg BID	150 mg BID
HR+/HER2− breast cancer — monotherapy	adult	200 mg BID	200 mg BID	200 mg BID

Renal No adjustment for mild–moderate impairment (CLcr ≥30 mL/min); severe/ESRD/dialysis not studied.

Hepatic No adjustment for mild–moderate (Child-Pugh A/B); severe (Child-Pugh C): reduce dosing frequency to once daily.

Instructions

Take at about the same times every day, with or without food.
Swallow tablets whole; do not chew, crush, or split; do not ingest broken or cracked tablets.
If a dose is missed or vomited, take the next dose at its scheduled time.
At the first sign of loose stools, start an antidiarrheal (e.g., loperamide) and increase oral fluids.
Discontinue in patients unable to tolerate 50 mg BID.

Available strengths

tab 50, 100, 150, 200 mg

Cautions

Diarrhea (can be severe with dehydration and infection)
Neutropenia (including febrile and fatal neutropenic sepsis)
Interstitial lung disease/pneumonitis (severe, life-threatening, or fatal)
Hepatotoxicity (transaminase elevations)
Venous thromboembolism
Embryo-fetal toxicity

Adverse reactions

diarrhea, neutropenia, nausea, abdominal pain, infections, fatigue, anemia, leukopenia, decreased appetite, vomiting, headache, alopecia, thrombocytopenia

Pregnancy Can cause fetal harm (teratogenic in animals); advise effective contraception during treatment and for 3 weeks after the last dose.

Lactation Advise not to breastfeed during treatment and for 3 weeks after the last dose.

Cost

Abemaciclib (VERZENIO)

Strength		#/mo	CostPlus
50 mg	tab	60 BID	not offered
100 mg	tab	60 BID	not offered
150 mg	tab	60 BID	not offered
200 mg	tab	60 BID	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Abemaciclib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2029 est.

NO BOXED WARNINGS

Principal riskDiarrhea, near-universal and dose-limiting

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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Memory aids: interaction avatars

CYP3A4 substrate

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