Difference between revisions of "Venetoclax (Venclexta)"
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− | == | + | ==General information== |
− | 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. | + | 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> |
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+ | Route: PO | ||
+ | <br>Extravasation: n/a | ||
==Diseases for which it is used== | ==Diseases for which it is used== | ||
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==Also known as== | ==Also known as== | ||
ABT-199, GDC-0199 | ABT-199, GDC-0199 | ||
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+ | ==References== | ||
+ | <references/> | ||
[[Category:Drug index]] | [[Category:Drug index]] |
Revision as of 09:08, 14 April 2016
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
Diseases for which it is used
Preliminary results
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 link to abstract
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) 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) link to abstract
History of changes in FDA indication
- 4/11/16: FDA 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.
Also known as
ABT-199, GDC-0199