Venetoclax

VENCLEXTA

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Pronunciation: ven-ET-oe-klax (ven-KLEX-ta)

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

What it isBCL-2 inhibitor restoring apoptosis; CLL and acute myeloid leukemia.

Why this oneIt enables deep, time-limited remissions in CLL rather than indefinite treatment.

What limits it⚑ Tumor lysis can be fatal, making the ramp-up and hydration mandatory. Strong CYP3A4 inhibitors can sharply raise exposure.

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

FDA-approved for

chronic lymphocytic leukemia (2016)
acute myeloid leukemia

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
CLL/SLL	adult	20 mg QD (wk 1 ramp-up)	400 mg QD	400 mg QD
AML (with azacitidine or decitabine)	adult	100 mg QD (day 1 ramp-up)	400 mg QD	400 mg QD
AML (with low-dose cytarabine)	adult	100 mg QD (day 1 ramp-up)	600 mg QD	600 mg QD

Titration CLL/SLL: escalate weekly per 5-week ramp-up; AML: escalate daily over 3-day ramp-up

Renal Undefined

Hepatic Reduce dose 50% in severe hepatic impairment

5-week ramp-up (CLL/SLL) or 3-day ramp-up (AML) required to reduce tumor lysis syndrome risk

Instructions

Take orally once daily with a meal and water
Swallow whole
Provide TLS prophylaxis (hydration, anti-hyperuricemics) before first dose
Do not give live attenuated vaccines until B-cell recovery

Available strengths

tab 10, 50, 100 mg

Contraindications

Concomitant strong CYP3A inhibitors at initiation and during ramp-up in CLL/SLL (tumor lysis syndrome risk)

Cautions

Tumor lysis syndrome — assess risk, premedicate, hydrate
Neutropenia — monitor blood counts
Serious infections
No live vaccines until B-cell recovery
Embryo-fetal toxicity

Adverse reactions

Neutropenia
Thrombocytopenia
Anemia
Diarrhea
Nausea
Fatigue
Upper respiratory tract infection
Edema

Pregnancy May cause embryo-fetal harm; advise effective contraception

Lactation Do not breastfeed during and for 1 week after treatment

Cost

Venetoclax (VENCLEXTA)

Strength		#/mo	CostPlus
10 mg	tab	30 qd	not offered
50 mg	tab	30 qd	not offered
100 mg	tab	30 qd	not offered

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

Generic entry2033 est.

NO BOXED WARNINGS

Principal riskTumor lysis syndrome; the ramp-up is mandatory

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger3 / 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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