Difference between revisions of "Venetoclax (Venclexta)"

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==General information==
 
==General information==
−
Class/mechanism: From the [http://www.cancer.gov/publications/dictionaries/cancer-drug?CdrID=698675 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.<ref name="insert">[http://www.rxabbvie.com/pdf/venclexta.pdf Venetoclax (Venclexta) package insert]</ref><ref>[[Media:Venetoclax.pdf| Venetoclax (Venclexta) package insert (locally hosted backup)]]</ref><ref>[https://www.venclexta.com/ Venclexta manufacturer's website]</ref>
+
Class/mechanism: From the [http://www.cancer.gov/publications/dictionaries/cancer-drug?CdrID=698675 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.<ref name="insert">[http://www.rxabbvie.com/pdf/venclexta.pdf Venetoclax (Venclexta) package insert]</ref><ref>[[:File:Venetoclax.pdf| Venetoclax (Venclexta) package insert (locally hosted backup)]]</ref><ref>[https://www.venclexta.com/ Venclexta manufacturer's website]</ref>
 
<br>Route: PO
 
<br>Route: PO
 
<br>Extravasation: n/a
 
<br>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 [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://reference.medscape.com/drug/zytiga-abiraterone-999651 Medscape], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the prescribing information.<ref name="insert"></ref>
+
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 [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://reference.medscape.com/drug/zytiga-abiraterone-999651 Medscape], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the prescribing information.<ref name="insert"></ref>
  
 
==Diseases for which it is used==
 
==Diseases for which it is used==
−
*[[Chronic lymphocytic leukemia (CLL) and Small lymphocytic lymphoma (SLL)|Chronic lymphocytic leukemia]]
+
*[[Acute myeloid leukemia]]
−
 
+
*[[Chronic lymphocytic leukemia]]
−
==Preliminary results==
+
*[[Mantle cell lymphoma]]
 +
*[[Multiple myeloma]]
 +
*[[T-cell prolymphocytic leukemia]]
 +
*[[Waldenström macroglobulinemia]]
  
 +
==History of changes in FDA indication==
 
===[[Acute myeloid leukemia]]===
 
===[[Acute myeloid leukemia]]===
−
# '''Abstract:''' Marina Konopleva, MD, PhD, Daniel A. Pollyea, MD, MS, Jalaja Potluri, MD, Brenda J. Chyla, PhD, Todd Busman, MS, Evelyn McKeegan, PhD, Ahmed Salem, PhD, Ming Zhu, PhD, Justin L. Ricker, MD, PhD, William Blum, MD, Courtney D. DiNardo, MD, Martin Dunbar, DRPH, Rachel Kirby, Nancy Falotico, Joel D. Leverson, PhD, Rod A. Humerickhouse, MD, PhD, Mack Mabry, MD, Richard M. Stone, MD, Hagop M. Kantarjian, MD and Anthony G. Letai, MD, PhD. A Phase 2 Study of ABT-199 (GDC-0199) in Patients with Acute Myelogenous Leukemia (AML). ASH 2014 abstract 118 [https://ash.confex.com/ash/2014/webprogram/Paper72531.html link to abstract]
+
*2018-11-21: Accelerated approval for use in combination with [[Azacitidine (Vidaza)|azacitidine]] or [[Decitabine (Dacogen)|decitabine]] or low-dose [[Cytarabine (Ara-C)|cytarabine]] for the treatment of newly-diagnosed [[Acute_myeloid_leukemia|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; based on M14-358 and M14-387)''
−
 
+
**2020-10-16: Regular approval in combination with azacitidine, decitabine, or low-dose cytarabine (LDAC) for newly-diagnosed [[Acute_myeloid_leukemia|acute myeloid leukemia (AML)]] in adults 75 years or older, or who have comorbidities precluding intensive induction chemotherapy. ''(Converted to regular approval; based on VIALE-A and VIALE-C)''
−
===[[Mantle cell lymphoma]]===
 
−
# '''Abstract:''' Matthew Steven Davids, John Francis Seymour, John F. Gerecitano, Brad S. Kahl, John M. Pagel, William G. Wierda, Mary Ann Anderson, Nikita Rudersdorf, Lori A. Gressick, Nicholas P. Montalvo, Jianning Yang, Ming Zhu, Martin Dunbar, Elisa Cerri, Sari H. Enschede, Rod Humerickhouse, Andrew Warwick Roberts. Phase I study of ABT-199 (GDC-0199) in patients with relapsed/refractory (R/R) non-Hodgkin lymphoma (NHL): Responses observed in diffuse large B-cell (DLBCL) and follicular lymphoma (FL) at higher cohort doses. J Clin Oncol 32:5s, 2014 (suppl; abstr 8522) [http://meetinglibrary.asco.org/content/133739-144 link to abstract]
 
−
 
 
−
===[[Waldenström macroglobulinemia]]===
 
−
# '''Abstract:''' Matthew Steven Davids, John Francis Seymour, John F. Gerecitano, Brad S. Kahl, John M. Pagel, William G. Wierda, Mary Ann Anderson, Nikita Rudersdorf, Lori A. Gressick, Nicholas P. Montalvo, Jianning Yang, Ming Zhu, Martin Dunbar, Elisa Cerri, Sari H. Enschede, Rod Humerickhouse, Andrew Warwick Roberts. Phase I study of ABT-199 (GDC-0199) in patients with relapsed/refractory (R/R) non-Hodgkin lymphoma (NHL): Responses observed in diffuse large B-cell (DLBCL) and follicular lymphoma (FL) at higher cohort doses. J Clin Oncol 32:5s, 2014 (suppl; abstr 8522) [http://meetinglibrary.asco.org/content/133739-144 link to abstract]
 
  
−
==History of changes in FDA indication==
+
===[[Chronic lymphocytic leukemia|Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)]]===
−
*4/11/16: FDA approved "for the treatment of patients with [[Chronic lymphocytic leukemia (CLL) and Small lymphocytic lymphoma (SLL)|chronic lymphocytic leukemia (CLL) with 17p deletion]], as detected by an FDA-approved test, who have received at least one prior therapy.''
+
*'''2016-04-11: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm495351.htm Initial accelerated approval]''' for the treatment of patients with [[Chronic lymphocytic leukemia|chronic lymphocytic leukemia (CLL)]] with [[Biomarkers#17p|17p]] [[Biomarkers#Deletion|deletion]], as detected by an FDA-approved test, who have received at least one prior therapy. ''(Based on M12-175, M13-982, M14-032 ibrutinib cohort, and M14-032 idelalisib cohort)''
 +
**2018-06-08: Granted regular approval for patients with [[Chronic lymphocytic leukemia|chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)]], with or without [[Biomarkers#17p|17p]]  [[Biomarkers#Deletion|deletion]], who have received at least one prior therapy. ''(Regular approval; Biomarker-specific indication relaxed; based on MURANO)''
 +
*2019-05-15: Approved for adult patients with [[Chronic lymphocytic leukemia|chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)]]. ''(Prior treatment exposure requirement removed; based on GCLLSG CLL14)''
  
 +
==History of changes in EMA indication==
 +
*2016-12-04: Initial authorization as Venclyxto
 +
==History of changes in Health Canada indication==
 +
*2016-09-30: Initial notice of compliance with conditions
 +
*2020-01-13: Conditions were met
 +
==History of changes in PMDA indication==
 +
*2019-09-20: Newly indicated for the treatment of relapsed or refractory [[Chronic lymphocytic leukemia|chronic lymphocytic leukemia/small lymphocytic lymphoma]].
 +
*2021-03-23: New indication and a new dosage for the treatment of [[acute myeloid leukemia]].
 
==Also known as==
 
==Also known as==
−
ABT-199, GDC-0199
+
*'''Code names:''' ABT-199, GDC-0199
 +
*'''Brand name:''' Venclexta, Venclyxto
  
 
==References==
 
==References==
 
<references/>
 
<references/>
  
−
[[Category:Drug index]]
+
[[Category:Drugs]]
−
[[Category:Chemotherapy]]
+
[[Category:Oral medications]]
 +
[[Category:Mutation-specific medications]]
  
 
[[Category:Bcl-2 inhibitors]]
 
[[Category:Bcl-2 inhibitors]]
  
−
[[Category:Chronic lymphocytic leukemia (CLL) and Small lymphocytic lymphoma (SLL) medications]]
+
[[Category:Acute myeloid leukemia medications]]
 +
[[Category:Chronic lymphocytic leukemia medications]]
 +
[[Category:Mantle cell lymphoma medications]]
 +
[[Category:Multiple myeloma medications]]
 +
[[Category:T-cell prolymphocytic leukemia medications]]
 +
[[Category:Waldenström macroglobulinemia medications]]
 +
 
 +
[[Category:FDA approved in 2016]]
 +
[[Category:EMA approved in 2016]]
 +
[[Category:Health Canada approved in 2016]]
 +
[[Category:PMDA approved in 2019]]
  
−
[[Category:Drugs FDA approved in 2016]]
+
[[Category:AbbVie product]]

Latest revision as of 14:57, 17 November 2023

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

  • 2018-11-21: Accelerated approval 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; based on M14-358 and M14-387)
    • 2020-10-16: Regular approval in combination with azacitidine, decitabine, or low-dose cytarabine (LDAC) for newly-diagnosed acute myeloid leukemia (AML) in adults 75 years or older, or who have comorbidities precluding intensive induction chemotherapy. (Converted to regular approval; based on VIALE-A and VIALE-C)

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

History of changes in EMA indication

  • 2016-12-04: Initial authorization as Venclyxto

History of changes in Health Canada indication

  • 2016-09-30: Initial notice of compliance with conditions
  • 2020-01-13: Conditions were met

History of changes in PMDA indication

Also known as

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

References

  1. ↑ 1.0 1.1 Venetoclax (Venclexta) package insert
  2. ↑ Venetoclax (Venclexta) package insert (locally hosted backup)
  3. ↑ Venclexta manufacturer's website
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