Palbociclib

Palbociclib
Clinical data
Trade names	Ibrance, others
Other names	PD-0332991
AHFS/Drugs.com	Monograph
MedlinePlus	a615013
License data	US DailyMed: Palbociclib;
Pregnancy; category	AU: D;
Routes of; administration	By mouth
ATC code	L01EF01 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Bioavailability	46%
Protein binding	85%
Metabolism	Liver (CYP3A, SULT2A1, glucuronidation)
Elimination half-life	29 (±5) hours
Excretion	74% feces, 18% urine
Identifiers
	IUPAC name 6-Acetyl-8-cyclopentyl-5-methyl-2-{[5-(1-piperazinyl)-2-pyridinyl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one;
CAS Number	571190-30-2;
PubChem CID	5330286;
DrugBank	DB09073;
ChemSpider	4487437;
UNII	G9ZF61LE7G;
KEGG	D10372 ;
ChEBI	CHEBI:85993 ;
ChEMBL	ChEMBL189963;
PDB ligand	LQQ (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID40972590 ;
ECHA InfoCard	100.238.221
Chemical and physical data
Formula	C24H29N7O2
Molar mass	447.543 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C2N(c1nc(ncc1/C(=C2/C(=O)C)C)Nc3ncc(cc3)N4CCNCC4)C5CCCC5;
	InChI InChI=1S/C24H29N7O2/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29); Key:AHJRHEGDXFFMBM-UHFFFAOYSA-N;

Palbociclib, sold under the brand name Ibrance among others, is a medication developed by Pfizer for the treatment of HR-positive and HER2-negative breast cancer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.^[5]^[6] Palbociclib was the first CDK4/6 inhibitor to be approved as a cancer therapy.^[7]

^ "Prescription medicines: registration of new chemical entities in Australia, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Archived from the original on 10 April 2023. 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.
^ "Ibrance EPAR". European Medicines Agency. 9 November 2016. Retrieved 16 May 2024.
^ Cite error: The named reference Finn2009 was invoked but never defined (see the help page).
^ Cite error: The named reference pmid24369047 was invoked but never defined (see the help page).
^ "Updated Data from Phase 3 Trial of Ibrance (palbociclib) Plus Letrozole in HR+, HER2- Metastatic Breast Cancer Confirm Improvement in Progression-Free Survival" (Press release). Pfizer. Archived from the original on 22 June 2021. Retrieved 16 December 2017.

[1] "Prescription medicines: registration of new chemical entities in Australia, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Archived from the original on 10 April 2023. Retrieved 9 April 2023.

[2] "Prescription medicines and biologicals: TGA annual summary 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 31 March 2024.

[3] "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.

[4] "Ibrance EPAR". European Medicines Agency. 9 November 2016. Retrieved 16 May 2024.

[Finn2009-5] Cite error: The named reference Finn2009 was invoked but never defined (see the help page).

[pmid24369047-6] Cite error: The named reference pmid24369047 was invoked but never defined (see the help page).

[pfizer.com-7] "Updated Data from Phase 3 Trial of Ibrance (palbociclib) Plus Letrozole in HR+, HER2- Metastatic Breast Cancer Confirm Improvement in Progression-Free Survival" (Press release). Pfizer. Archived from the original on 22 June 2021. Retrieved 16 December 2017.

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