Venetoclax
VENCLEXTA
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.
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
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
NO BOXED WARNINGS
Principal riskTumor lysis syndrome; the ramp-up is mandatory
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2033 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Venetoclax ballicule
