AI Search

Home News & Opinion Reference

Journals

Education

Services

Drugs Conditions Procedures Pathogens Laboratory Calculators Antibiotic Resistance

venetoclax

Brand Name : Venclexta

Synonyms : venetoclax

Class : B-Cell Lymphoma Inhibitors, Miscellaneous antineoplastics

Dosage Forms & Strengths

Tablet

10mg

50mg

100mg

lymphoma

Follow a weekly progress schedule over a period of 5 weeks to gradually enhance the dose to the recommended daily dose intake of 400 mg. progress dosing schedule is generally designed to gradually decrease tumor burden and diminish risk of tumor lysis syndrome. Week 1-20 mg orally one time a day. Week 2-50 mg orally one time a day. Week 3-100 mg orally one time a day. Week 4-200 mg orally one time a day. Week 5 and after-400 mg orally one time a day. Monotherapy 400 mg orally every day after completing the 5-week dosage schedule. Continue treatment until there is evidence of disease progression or the occurrence of unacceptable toxicity. Combination with Obinutuzumab 1-cycle Day 1- Obinutuzumab 100 mg intravenously Day 2- Obinutuzumab 900 mg intravenously Days 8 & 15- Obinutuzumab 1000 mg intravenously Day 22- Start venetoclax dosing according to the 5-week ramp-up schedule. 2-cycle Day 1- Obinutuzumab 100 mg intravenously. Day 28-After completion of the ramp-up schedule on 2-cycle day 28, continue the venetoclax dosing 400 mg every day from 3-cycle day-1 to 12-cycle day-28. 3-6 cycle Day 1- Obinutuzumab 100 mg intravenously. Day 1 to 28-Continue venetoclax 400 mg orally every day. 7-12 cycle Day 1 to 28-Continue venetoclax 400 mg orally every day. Combination with rituximab Venetoclax Complete the 5-week ramp-up dosing schedule to reach 400 mg orally every day. Continue the venetoclax dosing 400 mg orally every day for 24 months from the 1-cycle day-1 of rituximab. Rituximab Initiate 375 mg/m² Intravenously after the patient has received venetoclax 400 mg every day for 7 days. 500 mg/m² Intravenously on day-1 for 2-6 cycles. Acute Myeloid Leukemia venetoclax dosing generally depends on a combination agent. Day 1-100 mg orally every day. Day 2-200 mg orally every day. Day 3-400 mg orally every day. Day 4 and after (combination with azacitidine /decitabine): 400 mg orally every day. Day 4 and after (combination with low dosage cytarabine): 600 mg orally every day. combination with azacitidine, decitabine or low-dose cytarabine- Continue treatment until there is evidence of disease progression or the occurrence of unacceptable toxicity.

Dosage Forms & Strengths

Tablet

10mg

50mg

100mg

lymphoma

DRUG INTERACTION

venetoclax

Known drug interactions

No interactions found.

Frequency defined

>10%

Pyrexia (18%)

Thrombocytopenia (29%)

Abdominal pain (18%)

Edema (22%)

Fatigue (32%)

URT infection (36%)

Neutropenia (50%)

Anemia (33%)

Nausea (42%)

Constipation (16%)

Thrombocytopenia, Grade 3 or 4 (20%)

Neutropenia, Grade 3 or 4 (45%)

Mucositis (13%)

Vomiting (16%)

Lymphopenia (11%)

Anemia, Grade 3 or 4 (18%)

1-10%

Febrile neutropenia (6%)

Abdominal pain, Grade 3 or 4 (3%)

Fatigue, Grade 3 or 4 (4%)

Nausea, Grade 3 or 4 (1%)

Vomiting, Grade 3 or 4 (1%)

URT infection, Grade 3 or 4 (1%)

Edema, Grade 3 or 4 (2%)

Diarrhea, Grade 3 or 4 (3%)

<1%

Mucositis, Grade 3 or 4

Pyrexia, Grade 3 or 4

Constipation, Grade 3 or 4

Combination with rituximab

>10%

Lymphopenia (87%)

Hypophosphatemia (57%)

Hyperkalemia (24%)

Leukopenia, Grade 3 or 4 (46%)

Diarrhea (40%)

Increased AST/SGOT (46%)

Neutropenia, Grade 3 or 4 (62-64%)

Constipation (14%)

Anemia (16%)

Hypophosphatemia, Grade 3 or 4 (14%)

Hypokalemia (29%)

Hypernatremia (24%)

Increased alkaline phosphatase (35%)

Nausea (21%)

Hyperbilirubinemia (33%)

Rash (13%)

Neutropenia (65-86%)

Musculoskeletal pain (19%)

Thrombocytopenia (15%)

Hyponatremia (30%)

LRT infection (18%)

URT infection (39%)

Headache (11%)

Insomnia (11%)

Hypocalcemia (62%)

Lymphopenia, Grade 3 or 4 (56%)

Abdominal pain (13%)

1-10%

Febrile neutropenia (4%)

Mucositis (10%)

Hyperkalemia, Grade 3 or 4 (3%)

Hyponatremia, Grade 3 or 4 (6%)

Hypernatremia, Grade 3 or 4 (1%)

Hypokalemia, Grade 3 or 4 (6%)

LRT infection, Grade 3 or 4 (2%)

TLS, Grade 3 or 4 (3%)

Lymphopenia, Grade 3/4 (7%)

Increased AST/SGOT (2%)

Pneumonia (10%)

Hyperbilirubinemia, Grade 3 or 4 (4%)

URT infection, Grade 3/4 (2%)

Diarrhea, Grade 3 or 4 (3%)

Vomiting (8%)

Hypocalcemia, Grade 3 or 4 (5%)

Increased alkaline phosphatase, Grade 3/4 (1%)

Musculoskeletal pain, Grade 3/4 (1%)

Actions and Spectrum:

Venetoclax is a BCL-2 inhibitor used to treat certain blood cancers like CLL, SLL, and AML. It works by binding to BCL-2 and blocks its function and cause cancer cell death. It has shown promise in treating non-Hodgkin lymphoma, multiple myeloma, and certain solid tumors.

Black Box Warning:

Tumor lysis syndrome (TLS)

Contraindication/Caution:

Venetoclax cause hypersensitivity, pregnancy and breastfeeding risks, and potent CYP3A inhibitors.

Pregnancy consideration:

AU TGA pregnancy category: C
US FDA pregnancy category: Not assigned.

Lactation:  

Excreted into human milk is Not known.

Pregnancy category:

Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology:

Venetoclax is a small molecule inhibitor that selectively inhibits the B-cell lymphoma 2 (BCL-2) protein an anti-apoptotic protein that regulates programmed cell death.

Pharmacodynamics:

Venetoclax inhibits B-cell lymphoma 2 (Bcl-2) preventing apoptosis by binding to it displacing proapoptotic proteins and activating caspases thus restoring apoptosis in CLL cells preventing tumor cell survival and chemotherapy resistance.

Pharmacokinetics:

Absorption

AUC is 32.8 mcg·hr/mL.

Distribution

It is highly protein bound with a binding rate of > 99.9%.

Metabolism

CYP3A4/5 enzyme metabolizes venetoclax.

Elimination and Excretion

Half-life of 26 hours and eliminated from the body by feces.

Administration:

It is taken orally once daily and dose depends on the patientweight and other factors.

Patient information leaflet

Generic Name: venetoclax

Pronounced: [ ven-ET-oh-klax ]

Why do we use venetoclax?

Venetoclax treats blood cancers like CLL, SLL, and AML. It targets B-cell lymphoma 2 (BCL-2) by inhibiting apoptosis and slowing cancer growth. It can be used alone or with other medications depending on the cancer type and stage.