VENCLEXTA™ (venetoclax) Tablets Prescribing Information

Clinical pharmacology

Mechanism of Action:
Venetoclax is a selective and orally bioavailable small-molecule inhibitor of BCL-2, an anti-apoptotic protein. Overexpression of BCL-2 has been demonstrated in CLL cells where it mediates tumor cell survival and has been associated with resistance to chemotherapeutics. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins like BIM, triggering mitochondrial outer membrane permeabilization and the activation of caspases. In nonclinical studies, venetoclax has demonstrated cytotoxic activity in tumor cells that overexpress BCL-2.

Indications and usage

INDICATIONS AND USAGE:
VENCLEXTA is a BCL-2 inhibitor indicated for the treatment of patients with chronic lymphocytic leukemia (CLL) with 17p deletion, as detected by an FDA approved test, who have received at least one prior therapy.

This indication is approved under accelerated approval based on overall response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.

Dosage and administration

Drug UPDATES: VENCLEXTA™ (venetoclax) tablets
[Drug information / PDF]
Package insert - Dosing: Click (+) next to Dosage and Administration section (drug info link)

Initial U.S. Approval: 2016

DOSAGE AND ADMINISTRATION
Initiate therapy with VENCLEXTA at 20 mg once daily for 7 days, followed by a weekly ramp-up dosing schedule to the recommended daily dose of 400 mg. (2.2)
VENCLEXTA tablets should be taken orally once daily with a meal and water. Do not chew, crush, or break tablets. (2.2)
Perform prophylaxis for tumor lysis syndrome. (2.3)

How supplied

HOW SUPPLIED:
DOSAGE FORMS AND STRENGTHS
Tablets: 10 mg, 50 mg, 100 mg

Reference

[Drug information / PDF]

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates. A local search option of this data can be found here.