Palbocent 125

 

Indications 

Palbociclib is primarily used to treat hormone receptor-positive (HR+), HER2-negative advanced or metastatic breast cancer.

🔹 Common treatment combinations:

  1. With letrozole (an aromatase inhibitor) – for postmenopausal women as initial endocrine-based therapy.
  2. With fulvestrant – for women whose disease has progressed after prior hormone therapy.

Mechanism of Action

Palbociclib selectively inhibits CDK4 and CDK6, which are proteins involved in regulating cell division.

  • In HR+ breast cancer, these kinases are overactive, pushing cancer cells to divide uncontrollably.
  • By blocking CDK4/6, palbociclib slows down or stops cancer cell growth, particularly in cells that are hormone-receptor positive.

Dosage & Administration

  • Standard Dose: 125 mg once daily for 21 days, followed by 7 days off (a 28-day cycle).
  • Take with food, at the same time each day.
  • Can be used in capsule or tablet form.

Dose Adjustments:

May be required in cases of:

  • Low white blood cell counts (neutropenia)
  • Liver or kidney impairment
  • Drug interactions (e.g., with CYP3A inhibitors)

Efficacy / Effects

Clinical trials (e.g., PALOMA-2 and PALOMA-3) have shown that palbociclib:

  • Doubles progression-free survival in combination therapy vs hormone therapy alone.
  • Helps delay the need for chemotherapy.
  • Maintains quality of life with manageable side effects.

Common Side Effects

Very Common Explanation
Neutropenia Low white blood cells → risk of infection
Fatigue Tiredness, weakness
Nausea Often mild to moderate
Alopecia Hair thinning or loss
Diarrhea / Constipation GI disturbances
Stomatitis Mouth sores
 
Serious Side Effects (Rare but Important)
  • Febrile neutropenia (infection with low WBC)
  • Pulmonary embolism (blood clot in the lung)
  • Liver function abnormalities
  • QT prolongation (heart rhythm changes – rare)

Monitoring During Treatment

  • Complete blood counts (CBC): before starting and every 2 weeks for the first 2 months, then monthly.
  • Liver function tests
  • Signs of infection or unusual bleeding
  • Drug interaction check (CYP3A interactions)