Venetoclax

Venetoclax
Clinical data
Pronunciation	/vɛˈnɛtəklæks/; ve-NE-tə-klaks
Trade names	Venclexta, Venclyxto
Other names	GDC-0199, ABT-199, RG-7601
AHFS/Drugs.com	Monograph
MedlinePlus	a616028
License data	US DailyMed: Venetoclax;
Pregnancy; category	AU: C;
Routes of; administration	By mouth
ATC code	L01XX52 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only; EU: Rx-only; In general: ℞ (Prescription only);
Pharmacokinetic data
Protein binding	>99.9%
Metabolism	Liver (CYP3A4, CYP3A5)
Elimination half-life	~26 hours
Excretion	Feces (>99.9%; 20.8% as unchanged venetoclax)
Identifiers
	IUPAC name 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	1257044-40-8;
PubChem CID	49846579;
DrugBank	DB11581;
ChemSpider	29315017;
UNII	N54AIC43PW;
KEGG	D10679;
ChEBI	CHEBI:133021;
ChEMBL	ChEMBL3137309;
PDB ligand	LBM (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID30154863 ;
ECHA InfoCard	100.254.611
Chemical and physical data
Formula	C45H50ClN7O7S
Molar mass	868.45 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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]

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

[Drugs.com_pregnancy-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.

[Venclexta_FDA_label-7] Cite error: The named reference Venclexta FDA label was invoked but never defined (see the help page).

[Venclyxto_EPAR-8] ^ ^a ^b ^c ^d ^e ^f Cite error: The named reference Venclyxto EPAR was invoked but never defined (see the help page).

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