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Synonyms: ABT-199 | GDC-0199 | Venclexta® | Venclyxto®
venetoclax is an approved drug (FDA and EMA (2016))
Compound class: Synthetic organic
Comment: Venetoclax is a BH3 mimetic that selectively targets Bcl-2 , utilised for its pro-apoptotic activity. It is noteworthy that venetoclax is the first approved medicine designed to induce a natural process that helps cells self-destruct.
The IUPAC name provided by PubChem matches 'Example 5' claimed in patent US8580794 .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Doherty GA, Elmore SW, Hasvold LA, Souers AJ, Tao Z-F, Wang GT, Wang L, Mantei R, Hansen TM. (2013)
Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases.
Patent number: US8580794. Assignee: Abbvie Inc.. Priority date: 26/05/2009. Publication date: 12/11/2013.
FDA approves venetoclax for CLL or SLL, with or without 17 p deletion, after one prior therapy.
Accessed on 18/06/2018. Modified on 18/06/2018. FDA.gov, https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm610308.htm?utm_campaign=Oncology%206%2F8%2F18%20&utm_medium=email&utm_source=Eloqua&elqTrackId=3413c3557cf04e12aaa41ce1a31ef707&elq=4d3e9515bb1e4f708c454b998d0707f7&elqaid=3844&elqat=1&elqCampaignId=2978
3. Seymour JF, Kipps TJ, Eichhorst B, Hillmen P, D'Rozario J, Assouline S, Owen C, Gerecitano J, Robak T, De la Serna J et al.. (2018)
Venetoclax-Rituximab in Relapsed or Refractory Chronic Lymphocytic Leukemia.
N Engl J Med, 378 (12): 1107-1120. [PMID:29562156]
4. Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ et al.. (2013)
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.
Nat Med, 19 (2): 202-8. [PMID:23291630]
5. Tian BP, Xia LX, Bao ZQ, Zhang H, Xu ZW, Mao YY, Cao C, Che LQ, Liu JK, Li W et al.. (2017)
Bcl-2 inhibitors reduce steroid-insensitive airway inflammation.
J Allergy Clin Immunol, 140 (2): 418-430. [PMID:28043871]