Venetoclax

Venetoclax
Clinical data
Pronunciation/vɛˈnɛtəklæks/
ve-NE-tə-klaks
Trade namesVenclexta, Venclyxto
Other namesGDC-0199, ABT-199, RG-7601
AHFS/Drugs.comMonograph
MedlinePlusa616028
License data
Pregnancy
category
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding>99.9%[7]
MetabolismLiver (CYP3A4, CYP3A5)
Elimination half-life~26 hours
ExcretionFeces (>99.9%; 20.8% as unchanged venetoclax)
Identifiers
  • 4-(4-{[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl}-1-piperazinyl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.254.611 Edit this at Wikidata
Chemical and physical data
FormulaC45H50ClN7O7S
Molar mass868.45 g·mol−1
3D model (JSmol)
  • CC1(CCC(=C(C1)c2ccc(cc2)Cl)CN3CCN(CC3)c4ccc(c(c4)Oc5cc6cc[nH]c6nc5)C(=O)NS(=O)(=O)c7ccc(c(c7)[N+](=O)[O-])NCC8CCOCC8)C
  • InChI=1S/C45H50ClN7O7S/c1-45(2)15-11-33(39(26-45)31-3-5-34(46)6-4-31)29-51-17-19-52(20-18-51)35-7-9-38(42(24-35)60-36-23-32-12-16-47-43(32)49-28-36)44(54)50-61(57,58)37-8-10-40(41(25-37)53(55)56)48-27-30-13-21-59-22-14-30/h3-10,12,16,23-25,28,30,48H,11,13-15,17-22,26-27,29H2,1-2H3,(H,47,49)(H,50,54) COPY
  • Key:LQBVNQSMGBZMKD-UHFFFAOYSA-N

Venetoclax, sold under the brand names Venclexta and Venclyxto, is a medication used to treat adults with chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), or acute myeloid leukemia (AML).[7][8]

The most common side effects are low levels of neutrophils (a type of white blood cell), diarrhea, nausea, anemia (low red blood cell counts), nose and throat infection and tiredness.[8]

Venetoclax attaches to a protein called Bcl-2.[8] This protein is present in high amounts in CLL cancer cells, where it helps the cells survive for longer in the body and makes them resistant to cancer medicines.[8] By attaching to Bcl-2 and blocking its actions, venetoclax causes the death of cancer cells and thereby slows down progression of the disease.[8]

  1. ^ "Venetoclax (Venclexta) Use During Pregnancy". Drugs.com. 29 May 2019. Retrieved 25 April 2020.
  2. ^ "AusPAR: Venetoclax". Therapeutic Goods Administration (TGA). 26 April 2022. Retrieved 27 April 2022.
  3. ^ "Prescription medicines: registration of new chemical entities in Australia, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 9 April 2023.
  4. ^ "Prescription medicines and biologicals: TGA annual summary 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 31 March 2024.
  5. ^ "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.
  6. ^ "Venclyxto 10 mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 21 April 2020. Retrieved 25 April 2020.
  7. ^ a b c Cite error: The named reference Venclexta FDA label was invoked but never defined (see the help page).
  8. ^ a b c d e f Cite error: The named reference Venclyxto EPAR was invoked but never defined (see the help page).