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venetoclax

BCL2 inhibitor (BH3 mimetic) · Antineoplastic agent

BCL2 inhibitor (BH3 mimetic)Antineoplastic agent
CDSCO approved
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
D
FDA category + note
Top interactionssee all 12
  • AbirateroneSevereDatabaseDDInter
  • AdalimumabSevereDatabaseDDInter
  • AmiodaroneSevereDatabaseDDInter
  • AmprenavirSevereDatabaseDDInter

Mechanism

Venetoclax is a first-in-class, orally bioavailable, small-molecule inhibitor of BCL2. It was designed as a BH3 mimetic that inhibits BCL2 interaction with the proapoptotic BH3-only family members, such as BIM, BID, and BAD. In the presence of venetoclax, BH3-only proteins can translocate to mitochondria and initiate BAX/BAK-dependent apoptosis. It helps restore apoptosis in CLL cells.

Indications

CLLSLLnewly diagnosed AML (in combination with azacitidine, decitabine, or low-dose cytarabine) in patients 75 years or older or with comorbidities that preclude the use of chemotherapy

Pharmacokinetics

Half-life
18 to 26 h (elimination)
Bioavailability
oral absorption significantly improved 3- to 5-fold by administration with a meal
Protein binding
>99.9%
Metabolism
CYP3A4/5
Excretion
<0.1%

Side effects

Common
neutropeniadiarrheanauseaanemiaupper respiratory tract infectionthrombocytopeniafatiguetumor lysis syndromenausea/vomiting/diarrhea

Pregnancy & lactation

Pregnancy

D

Drug interactions

Abiraterone
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amiodarone
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Aprepitant
Severe
Database

Increased venetoclax exposure.

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Baricitinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Bepridil
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Berotralstat
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Boceprevir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Bosentan
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

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Sources: Goodman & Gilman 14e, Harrison 22e·Verified: 2026-05-10 · House clinical team