Palbociclib interactions

Food & lifestyle

• grapefruit juice

  Moderate

  Metabolism

  Administration with food may enhance the oral bioavailability of palbociclib in some patients and reduce the intersubject variability of palbociclib exposure. According to the product labeling, palbociclib absorption and exposure were very low in approximately 13% of the population when taken in the fasted state. Food intake increased the palbociclib exposure in this small subset of the population, but did not alter palbociclib exposure in the rest of the population to a clinically relevant extent. Compared to palbociclib given under overnight fasted conditions, the population average palbociclib peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 38% and 21%, respectively, when given with high-fat, high-calorie food (approximately 800 to 1000 calories; 150, 250, and 500 to 600 calories from protein, carbohydrate and fat, respectively).

  What to do: Patients should take palbociclib with food and avoid consumption of grapefruit or grapefruit juice during treatment.

  1 source

  1. "Product Information. Ibrance (palbociclib)." Pfizer U.S. Pharmaceuticals Group (2015):

• high-fat foods

  Moderate

  Absorption

  Administration with food may enhance the oral bioavailability of palbociclib in some patients and reduce the intersubject variability of palbociclib exposure. According to the product labeling, palbociclib absorption and exposure were very low in approximately 13% of the population when taken in the fasted state. Food intake increased the palbociclib exposure in this small subset of the population, but did not alter palbociclib exposure in the rest of the population to a clinically relevant extent. Compared to palbociclib given under overnight fasted conditions, the population average palbociclib peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 38% and 21%, respectively, when given with high-fat, high-calorie food (approximately 800 to 1000 calories; 150, 250, and 500 to 600 calories from protein, carbohydrate and fat, respectively).

  What to do: Patients should take palbociclib with food and avoid consumption of grapefruit or grapefruit juice during treatment.

  1 source

  1. "Product Information. Ibrance (palbociclib)." Pfizer U.S. Pharmaceuticals Group (2015):

Conditions

Conditions in which Palbociclib needs care, as documented in this source.

• Hepatic Insufficiency

  Moderate

  Based on a population pharmacokinetic analysis with palbociclib mild hepatic impairment had no effect on the exposure of palbociclib. Close monitoring is recommended when using this agent in patients with moderate or severe hepatic impairment as the pharmacokinetics of palbociclib have not been studied in these patients. Dose modification of concomitant medications may be needed based of hepatic impairment.

  1 source

  1. "Product Information. Ibrance (palbociclib)." Pfizer U.S. Pharmaceuticals Group (2015):

• Kidney Diseases

  Moderate

  Based on a population pharmacokinetic analysis with palbociclib mild and moderate renal impairment had no effect on the exposure of palbociclib. Close monitoring is recommended when using this agent in patients with severe renal impairment as the pharmacokinetics of palbociclib in these patients have not been studied.

  1 source

  1. "Product Information. Ibrance (palbociclib)." Pfizer U.S. Pharmaceuticals Group (2015):

• Lung Diseases

  Moderate

  The use of certain multikinase inhibitors has been associated with pulmonary toxicity. Serious cases of interstitial lung disease (ILD), including fatal cases and interstitial pneumonitis or pulmonary fibrosis have been reported. Caution is recommended when using these agents in patients with a history of interstitial pneumonitis or pulmonary fibrosis or those patients presenting with acute onset of new or progressive unexplained pulmonary symptoms such as dyspnea, cough, and fever pending diagnostic evaluation. If ILD is confirmed, permanently discontinue these agents and institute appropriate measures. Immediately withhold treatment in patients diagnosed with ILD/pneumonitis and permanently discontinue therapy if no other potential causes of ILD/pneumonitis have been identified.

  7 sources

  1. "Product Information. Vandetanib (vandetanib)." Astra-Zeneca Pharmaceuticals (2011):
  2. "Product Information. Zelboraf (vemurafenib)." Genentech (2011):
  3. "Product Information. Xalkori (crizotinib)." Pfizer U.S. Pharmaceuticals Group (2011):
  4. "Product Information. Mekinist (trametinib)." GlaxoSmithKline (2013):
  5. "Product Information. Zykadia (ceritinib)." Novartis Pharmaceuticals (2014):
  6. "Product Information. Zydelig (idelalisib)." Gilead Sciences (2014):
  7. "Product Information. Alecensa (alectinib)." Genentech (2015):

• Neutropenia

  Moderate

  The use of palbociclib may cause neutropenia, including febrile neutropenia and neutropenic sepsis. It is recommended to monitor complete blood counts prior to starting treatment and at the beginning of each therapy cycle with palbociclib, as well as on Day 15 of the first 2 cycles, and as clinically indicated thereafter. Dose interruption, dose reduction, or delay in starting treatment cycles is recommended for patients who develop Grade 3 or 4 neutropenia. Care and close monitoring is recommended, in particular for any episodes of fever.

  1 source

  1. "Product Information. Ibrance (palbociclib)." Pfizer U.S. Pharmaceuticals Group (2015):

• Premenopausal

  Moderate

  Pre/perimenopausal women treated with the combination palbociclib plus fulvestrant therapy should be treated with luteinizing hormone-releasing hormone (LHRH) agonists according to current clinical practice standards. Care and close monitoring is recommended.

  1 source

  1. "Product Information. Ibrance (palbociclib)." Pfizer U.S. Pharmaceuticals Group (2015):

Therapeutic duplication

Drug classes that overlap with Palbociclib, so taking both doubles up the same effect. This source publishes no per-row citations for duplication.

• cdk 4/6 inhibitors

  The recommended maximum number of medicines in the 'CDK 4/6 inhibitors' category to be taken concurrently is usually one.Your list includes two medicines belonging to the 'CDK 4/6 inhibitors' category.

  Example product in the source data (US market): Letrozole/ribociclib