Difference between revisions of "Venetoclax (Venclexta)"

Revision as of 22:40, 8 January 2020

General information

Class/mechanism: From the NCI Drug Dictionary: An orally bioavailable, selective small molecule inhibitor of the anti-apoptotic protein Bcl-2, with potential antineoplastic activity. GDC-0199 mimics BH3-only proteins, the native ligands of Bcl-2 and apoptosis activators, by binding to the hydrophobic groove of Bcl-2 proteins thereby repressing Bcl-2 activity and restoring apoptotic processes in tumor cells. Bcl-2 protein is overexpressed in some cancers and plays an important role in the regulation of apoptosis; its expression is associated with increased drug resistance and tumor cell survival. Compared to the Bcl-2 inhibitor navitoclax, this agent does not inhibit bcl-XL and does not cause bcl-XL-mediated thrombocytopenia.^[1]^[2]^[3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, Medscape, UpToDate (courtesy of Lexicomp), or the prescribing information.^[1]

Diseases for which it is used

History of changes in FDA indication

Acute myeloid leukemia

11/21/2018: Approval expanded for use in combination with azacitidine or decitabine or low-dose cytarabine for the treatment of newly-diagnosed acute myeloid leukemia (AML) in adults who are age 75 years or older, or who have comorbidities that preclude use of intensive induction chemotherapy. (New disease entity)

Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)

4/11/2016: Approved 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. (Initial approval)
6/8/2018: Granted regular approval for patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL), with or without 17p deletion, who have received at least one prior therapy. (Regular approval; Biomarker-specific indication relaxed)
5/15/2019: Approved for adult patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL). (Prior treatment exposure requirement removed)

Also known as

Code names: ABT-199, GDC-0199
Brand name: Venclexta

References

[insert-1] 1.0 ^1.1 Venetoclax (Venclexta) package insert

[2] Venetoclax (Venclexta) package insert (locally hosted backup)

[3] Venclexta manufacturer's website

[1]

[2]

[3]

@@ Line 17: / Line 17: @@
 ===[[Chronic lymphocytic leukemia|Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)]]===
-*4/11/2016: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm495351.htm Approved] for the treatment of patients with [[Chronic lymphocytic leukemia|chronic lymphocytic leukemia (CLL) with 17p deletion]], as detected by an FDA-approved test, who have received at least one prior therapy. ''(Initial approval)''
+*4/11/2016: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm495351.htm Approved] for the treatment of patients with [[Chronic lymphocytic leukemia|chronic lymphocytic leukemia (CLL)]] with 17p [[Biomarkers#deletion|deletion]], as detected by an FDA-approved test, who have received at least one prior therapy. ''(Initial approval)''
 *6/8/2018: Granted regular approval for patients with [[Chronic lymphocytic leukemia|chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)]], with or without 17p deletion, who have received at least one prior therapy. ''(Regular approval; Biomarker-specific indication relaxed)''
 *5/15/2019: Approved for adult patients with [[Chronic lymphocytic leukemia|chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)]]. ''(Prior treatment exposure requirement removed)''