The chemical structure of Palbociclib, the active ingredient in Palbocent 125 mg capsules, can be described as follows:

Chemical Structure

• Chemical Formula: C24H29N7O2
• Molecular Weight: 447.54 g/mol

Structural Representation

Palbociclib’s chemical structure features a complex arrangement that includes:

• A pyrido[2,3-d]pyrimidin-7(8H)-one core.
• Multiple nitrogen atoms and a piperazine ring, which contribute to its mechanism of action as a CDK4/6 inhibitor.
  

  Key Precautions for Palbocent 125 mg Capsules

  1. Neutropenia Monitoring: Neutropenia is the most commonly reported side effect. Complete blood counts should be monitored before starting treatment, at the beginning of each cycle, and on day 15 of the first two cycles. If grade 3 or 4 neutropenia occurs, dose interruption or reduction may be necessary.
  2. Embryo-Fetal Toxicity: Palbocent can cause fetal harm if administered during pregnancy. Women of reproductive potential should use effective contraception during treatment and for at least three weeks after the last dose.
  3. Breastfeeding: It is advised that women do not breastfeed while taking Palbocent due to potential risks to the infant.
  4. Dizziness and Fatigue: Patients may experience dizziness and fatigue, making it advisable to avoid driving or operating heavy machinery until they know how the medication affects them.
  5. Drug Interactions: Palbocent may interact with other medications, particularly those metabolized by CYP3A. Patients should inform their healthcare provider about all medications they are taking.

  Dietary Restrictions

  1. Administration with Food: Palbocent should be taken with food to enhance absorption. It is recommended to take the medication at the same time each day.
  2. Alcohol Consumption: While no specific interactions between Palbocent and alcohol have been documented, it is advisable to avoid alcohol during treatment due to potential side effects and overall health considerations.
  3. Avoid Grapefruit: Grapefruit and grapefruit juice may increase the levels of palbociclib in the blood, leading to increased side effects. It is best to avoid these products while on treatment.

  Foods to Avoid

  1. Grapefruit and Grapefruit Juice: These should be completely avoided as they can increase the levels of palbociclib in the bloodstream, potentially leading to heightened side effects and toxicity.
  2. High-Fat Meals: While not explicitly stated in the search results, it is generally advisable to avoid excessively high-fat meals when taking medications that should be taken with food, as they can affect the absorption of the drug.

  General Dietary Advice

  • Take with Food: Palbocent should be taken with food to enhance its absorption. It’s recommended to take it at the same time each day for consistency.

  By adhering to these dietary restrictions, patients can help ensure that Palbocent works effectively while minimizing the risk of adverse effects. Always consult with a healthcare provider for personalized dietary recommendations while on this medication.

  Drug Interactions

  1. CYP3A Inhibitors: Palbocent is metabolized primarily by the CYP3A enzyme. Co-administration with strong CYP3A inhibitors (e.g., ketoconazole, itraconazole) can increase palbociclib exposure, potentially leading to increased side effects. If such combinations cannot be avoided, dose adjustments may be necessary.
  2. CYP3A Substrates: The dose of sensitive CYP3A substrates with a narrow therapeutic index (e.g., cyclosporine, sirolimus, tacrolimus) may need to be reduced, as palbociclib can increase their exposure.
  3. Hormonal Therapies: Palbocent is often used in combination with hormonal anticancer therapies, such as aromatase inhibitors (e.g., letrozole) or fulvestrant. These combinations are intended to enhance therapeutic effects in treating breast cancer.
  4. Other Medications: There are numerous other medications that may interact with palbociclib, including common drugs like aspirin, lorazepam, and metoprolol. It is important for patients to inform their healthcare provider about all medications they are taking to assess potential interactions.

  Food and Alcohol Interactions

  • Grapefruit and Grapefruit Juice: These should be avoided as they can significantly increase the blood levels of palbociclib, leading to a higher risk of side effects.
  • Alcohol: Although there are no documented interactions between palbociclib and alcohol, it is generally advisable to avoid alcohol consumption during treatment due to potential side effects like dizziness and fatigue.

  key medications that should be avoided or have their dosages adjusted when taking Palbocent 125 mg capsules:

  Strong CYP3A Inhibitors

  • Palbocent is primarily metabolized by the CYP3A enzyme.
  • Avoid concomitant use of strong CYP3A inhibitors like clarithromycin, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, and voriconazole.
  • If coadministration with a strong CYP3A inhibitor cannot be avoided, reduce the dose of Palbocent.

  Grapefruit and Grapefruit Juice

  • Avoid grapefruit or grapefruit juice during Palbocent treatment as they can increase palbociclib exposure and side effects.

  Strong CYP3A Inducers

  • Avoid concomitant use of strong CYP3A inducers like phenytoin, rifampin, carbamazepine, enzalutamide, and St John’s Wort, as they can decrease palbociclib levels.

  Sensitive CYP3A Substrates

  • The dose of sensitive CYP3A substrates with a narrow therapeutic index like alfentanil, cyclosporine, dihydroergotamine, ergotamine, everolimus, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus may need to be reduced, as palbociclib can increase their exposure.

  Risks During Pregnancy

  1. Fetal Harm: Palbocent can cause significant fetal harm when administered to a pregnant woman. It has been associated with risks of major birth defects and miscarriage.
  2. Animal Studies: Animal reproduction studies have shown that administration of palbociclib during organogenesis resulted in embryo-fetal toxicity at maternal exposures that were significantly higher than those expected in humans.
  3. Advisory for Women of Reproductive Potential: Women who are pregnant or may become pregnant should be advised of the potential risks to the fetus. Effective contraception is recommended during treatment and for at least three weeks after the last dose of Palbocent.
  4. Background Risk: The estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies in the general population is approximately 2%-4% and 15%-20%, respectively.

  Dosage of Palbocent 125 mg

  The recommended dosage of Palbocent 125 mg is:

  • One 125 mg capsule taken orally once daily for 21 consecutive days
  • Followed by 7 days off treatment to comprise a complete cycle of 28 days
  • Palbocent should be taken with food at approximately the same time each day

  Storage

  Palbocent 125 mg capsules should be stored:

  • Below 30°C (86°F)
  • In a dry and clean place
  • Away from sunlight
  • Out of reach of children

  Reviews

  There are no specific reviews for Palbocent 125 mg capsules mentioned in the provided search results. However, the results indicate that Palbocent is a targeted therapy medication used to treat certain types of breast cancer, particularly hormone receptor-positive, HER2-negative advanced or metastatic breast cancer, when used in combination with hormonal therapies like aromatase inhibitors or fulvestrant.                                                                                                                                    Palbocent (palbociclib) is a targeted therapy used for treating hormone receptor-positive, HER2-negative advanced or metastatic breast cancer. Here’s how it compares to other breast cancer treatments:

  Mechanism of Action

  • Palbocent: As a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), Palbocent blocks the cell cycle progression from the G1 phase to the S phase by preventing the phosphorylation of the retinoblastoma (Rb) protein. This leads to reduced tumor cell proliferation and increased cell senescence, particularly when used in combination with antiestrogens or aromatase inhibitors.
  • Other Treatments:
    • Aromatase Inhibitors (e.g., Letrozole, Anastrozole): These medications lower estrogen levels in the body, which can slow the growth of hormone-sensitive tumors. They work by inhibiting the aromatase enzyme responsible for converting androgens to estrogens.
    • Fulvestrant: This is an estrogen receptor antagonist that degrades the estrogen receptor and inhibits estrogen signaling, used especially in cases of disease progression after initial hormonal therapy.
    • Chemotherapy: Traditional chemotherapy agents target rapidly dividing cells, including cancer cells, but often come with a broader range of side effects due to their impact on normal cells as well.

  Indications

  • Palbocent: Specifically indicated for HR-positive, HER2-negative advanced or metastatic breast cancer, often in combination with an aromatase inhibitor or fulvestrant.
  • Other Treatments: Hormonal therapies like aromatase inhibitors and fulvestrant are also used for HR-positive breast cancer, while chemotherapy may be indicated for HER2-positive or triple-negative breast cancers.

  Efficacy

  • Palbocent: Clinical studies demonstrate that palbociclib, when combined with aromatase inhibitors, significantly improves progression-free survival compared to hormonal therapy alone. It has shown enhanced efficacy in reducing tumor growth and prolonging patient survival.
  • Other Treatments: Aromatase inhibitors and fulvestrant are effective in managing HR-positive breast cancer, but their efficacy may be limited in cases of resistance or disease progression. Chemotherapy can be effective in aggressive cancers but is associated with more severe side effects.

  Side Effects

  • Palbocent: Common side effects include neutropenia, infections, fatigue, nausea, and diarrhea. Regular monitoring of blood counts is required due to the risk of neutropenia.
  • Other Treatments: Side effects vary; aromatase inhibitors may cause joint pain and hot flashes, while chemotherapy can lead to nausea, hair loss, and increased risk of infections due to bone marrow suppression.