Palbociclib

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Structural formula
Structure of palbociclib
General
Non-proprietary name Palbociclib
other names

6-Acetyl-8-cyclopentyl-5-methyl-2 - {[5- (piperazin-1-yl) pyridin-2-yl] amino} pyrido [2,3- d ] pyrimidin-7 (8 H ) -one

Molecular formula C 24 H 29 N 7 O 2
External identifiers / databases
CAS number
EC number 810-186-2
ECHA InfoCard 100.238.221
PubChem 5330286
ChemSpider 4487437
DrugBank DB09073
Wikidata Q15269707
Drug information
ATC code

L01 XE33

Drug class

Antineoplastic

properties
Molar mass 447.53 g · mol -1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances
06 - Toxic or very toxic

danger

H and P phrases H: 301
P: 301 + 310
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Palbociclib is a medicine used to treat certain types of breast cancer . He is the first representative of the new class of cyclin-dependent kinase inhibitors and at peroral effective administration.

Mechanism of action

By inhibiting the cyclin-dependent kinases CDK4 and CDK6, palbociclib causes decreased cell proliferation during the transition from phase G1 to S of the cell cycle .

Pharmacokinetics

After oral administration, maximum plasma concentrations occur after 6 to 12 hours. The absolute bioavailability after oral administration averages 46%. The majority of palbociclib (approximately 85% in vitro ) is bound to plasma proteins. It is excreted in the faeces (on average 74%) and in the urine (on average 17%).

The mean elimination half-life is approximately 28.8 hours.

application areas

Palbociclib is approved in the USA (accelerated break through therapy procedure ) and the EU as Ibrance for the treatment of HR- positive, HER2 -negative, locally advanced or metastatic breast cancer . It must be combined with aromatase inhibitors or fulvestrant , which are used as hormone therapy for cancer treatment.

Side effects

The most common side effects observed were infections, reductions in white and red blood cells and platelets , tiredness, loss of appetite, inflammation of the mouth and lips, nausea, vomiting, diarrhea, rash and hair loss.

Preparation names

Pfizer : Ibrance (EU, USA, CA )

Web links

Individual evidence

  1. ↑ a b Data sheet PD 0332991 isethionate ≥98% (HPLC) from Sigma-Aldrich , accessed on November 26, 2016 ( PDF ).
  2. ↑ a b c Ibrance: Summary of Product Characteristics .
  3. ↑ Drugs @ FDA: FDA Approved Drug Products - Ibrance (Palbociclib)
  4. ^ Community register of medicinal products for human use