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venetoclax (Venclexta)

Indications: - treatment of patients with chronic lymphocytic leukemia (CLL) with 17p deletion Dosage: - week 1: 20 mg PO QD - week 2: 50 mg PO QD - week 3: 100 mg PO QD - week 4: 200 mg PO QD - week 5: 400 mg PO QD (recommended daily dose of 400 mg) PO QD with food & water do not chew, crush, or break tablets [4] Tablets: 10 mg, 50 mg, 100 mg. [5] Adverse effects: - Serious adverse reactions were reported in 44% of patients - pneumonia - febrile neutropenia, pyrexia - autoimmune hemolytic anemia - tumor lysis syndrome - aggressive hydration plus allopurinol or rasburisase to to prevent tumor lysis syndrome [4] - diarrhea, nausea - upper respiratory tract infection - thrombocytopenia - fatigue - fetal injury in pregnant women Drug interactions: - CYP3A inhibitors - do not use during induction phase - for maintenance phase, reduce dose of venetoclax by at least 75% when used concomitantly with strong CYP3A inhibitors - avoid grapefruit - avoid coadministration with narrow therapeutic window P-glycoprotein substrates (digoxin, everolimus, sirolimus) - monitor INR closely in patients taking warfarin - live attenuated vaccine contraindicated Mechanism of action: - BCL-2 selective inhibitor

General

antineoplastic agent (chemotherapeutic agent)

Database Correlations

PUBCHEM correlations

References

  1. Venclexta https://www.venclexta.com/hcp.html
  2. FDA News Release. April 11, 2016 FDA approves new drug for chronic lymphocytic leukemia in patients with a specific chromosomal abnormality. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm495253.htm
  3. Windle ML FDA Drug Approvals and Changes: May edition. Medscape. May 20, 2016 http://reference.medscape.com/features/slideshow/drug-review/2016/may
  4. VENCLEXTA PRESCRIBING INFORMATION http://www.rxabbvie.com/pdf/venclexta.pdf
  5. Medscape: venetoclax (Rx) https://reference.medscape.com/drug/venclexta-venetoclax-1000078