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Palbociclib information


Palbociclib
Clinical data
Trade namesIbrance, others
Other namesPD-0332991
AHFS/Drugs.comMonograph
MedlinePlusa615013
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)[1][2]
  • CA: ℞-only[3]
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
Bioavailability46%
Protein binding85%
MetabolismLiver (CYP3A, SULT2A1, glucuronidation)
Elimination half-life29 (±5) hours
Excretion74% 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 checkY
ChEBI
  • CHEBI:85993 checkY
ChEMBL
  • ChEMBL189963
PDB ligand
  • LQQ (PDBe, RCSB PDB)
CompTox Dashboard (EPA)
  • DTXSID40972590 Edit this at Wikidata
ECHA InfoCard100.238.221 Edit this at Wikidata
Chemical and physical data
FormulaC24H29N7O2
Molar mass447.543 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.[4][5] Palbociclib was the first CDK4/6 inhibitor to be approved as a cancer therapy.[6]

  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. ^ Cite error: The named reference Finn2009 was invoked but never defined (see the help page).
  5. ^ Cite error: The named reference pmid24369047 was invoked but never defined (see the help page).
  6. ^ "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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