Pertuzumab (Perjeta) - Uses, Dose, Side effects

Pertuzumab (Perjeta) is a humanized monoclonal antibody that is used in the treatment of metastatic breast cancer.

Indications of Pertuzumab (Perjeta):

  • Metastatic breast cancer:

    • It is used for the treatment of human epidermal growth factor receptor 2 (HER2) positive metastatic breast cancer concurrently with trastuzumab and docetaxel in patients who have not received prior anti-HER2 therapy or chemotherapy to treat metastatic disease.
  • Early breast cancer:

    • It is used for adjuvant treatment of HER2-positive early breast cancer at high risk of recurrence concurrently with trastuzumab and chemotherapy.
  • Early breast cancer:

    • It is indicated for neoadjuvant treatment of locally advanced, inflammatory, or an early stage HER2-positive, breast cancer (>2 cm in diameter or node-positive) in combination with trastuzumab and chemotherapy as part of a complete treatment regimen for early breast cancer.

Pertuzumab (Perjeta) dose in adults:

Pertuzumab (Perjeta) dose in the treatment of metastatic HER2+ breast cancer:

  • 840 mg intravenous over 1 hour followed by a maintenance dose of 420 mg over 30 to 60 minutes every 3 weeks until disease progression or unacceptable toxicity in combination with trastuzumab and docetaxel.

Pertuzumab (Perjeta) dose in the adjuvant treatment of early HER2+ breast cancer:

  • 840 mg intravenous over 1 hour followed by a maintenance dose of 420 mg over 30 to 60 minutes every 3 weeks for a total of 1 year (up to 18 cycles) or until disease progression or unacceptable toxicity, as part of a combination regimen containing trastuzumab and including standard anthracycline- and/or taxane-based therapy, pertuzumab and trastuzumab should begin on day 1 of the first taxane containing cycle.

Pertuzumab (Perjeta) dose in the neoadjuvant treatment of early HER2+ breast cancer:

  • 840 mg intravenous over 1 hour followed by a maintenance dose of 420 mg over 30 to 60 minutes every 3 weeks for 3 to 6 cycles; may be administered as one of the regimens below.
  • Trastuzumab should be continued until 1 year after surgery.
  • Four preoperative cycles of pertuzumab, trastuzumab, and docetaxel, followed by 3 postoperative cycles of fluorouracil, epirubicin, and cyclophosphamide (FEC)


  • Three or four preoperative cycles of FEC (alone) followed by 3 or 4 preoperative cycles of pertuzumab, trastuzumab, and docetaxel


  • Six preoperative cycles of pertuzumab, trastuzumab, docetaxel, and carboplatin


  •  Four preoperative cycles of dose-dense doxorubicin and cyclophosphamide alone, followed by 4 preoperative cycles of pertuzumab, trastuzumab, and paclitaxel
  • Missed doses or delays:

    • If <6 weeks has elapsed, administer the 420 mg maintenance dose. Do not wait until the next planned dose.
    • If ≥6 weeks has elapsed, readminister the 840 mg initial dose over 1 hour followed by the maintenance dose of 420 mg (over 30 to 60 minutes) every 3 weeks.

Use in Children:

The safety and efficacy of the drug in children is not established.

Pregnancy Risk Category: D

[US Boxed Warning]

  • Pertuzumab crosses the placenta.
  • It can lead to oligohydramnios and pulmonary hypoplasia as well as skeletal anomalies and neonatal deaths.
  • If exposure is during pregnancy, or seven months prior to conception, monitoring for oligohydramnios may be necessary.
  • The European Society for Medical Oncology's guidelines for cancer in pregnancy are:
    • If pregnancy is suspected, it is important to wait until after the delivery of HER2 positive patients.
    • Before starting treatment, it is important to get rid of any pregnancy. Effective contraception should also be used during treatment and for the first seven months.

Use of Pertuzumab while breastfeeding

  • It is not known if pertuzumab is excreted in breast milk.
  • Breast milk contains immunoglobulin.
  • According to the manufacturer breastfeeding during therapy is a decision that should be made after considering the risks and benefits to the infant as well as the benefits to the mother.
  • Consider the extended half-life of trastuzumab as well as the 7-month washout period for pertuzumab when considering breastfeeding after treatment has been completed.

Pertuzumab (Perjeta) Dose adjustment in renal disease:

  • Creatinine clearance ≥30 mL/minute:

    • No dosage adjustment necessary.
  • Creatinine clearance <30 mL/minute:

    • There are no dosage adjustments provided in the manufacturer's labeling.

Pertuzumab (Perjeta) Dose adjustment in liver disease:

There are no dosage adjustments provided in the manufacturer's labeling.

Common Side Effects of Pertuzumab (Perjeta):

  • Central Nervous System:

    • Fatigue
    • Headache
    • Decreased Left Ventricular Ejection Fraction
    • Insomnia
    • Dizziness
  • Dermatologic:

    • Alopecia
    • Skin Rash
    • Pruritus
    • Palmar-Plantar Erythrodysesthesia
    • Xeroderma
  • Gastrointestinal:

    • Diarrhea
    • Nausea
    • Vomiting
    • Decreased Appetite
    • Mucositis
    • Constipation
    • Stomatitis
    • Dysgeusia
  • Hematologic & Oncologic:

    • Neutropenia
    • Anemia
    • Leukopenia
    • Febrile Neutropenia
  • Hypersensitivity:

    • Hypersensitivity
  • Neuromuscular & Skeletal:

    • Asthenia
    • Myalgia
    • Arthralgia
  • Respiratory:

    • Upper Respiratory Tract Infection
    • Epistaxis
  • Miscellaneous:

    • Fever
    • Infusion Reactions

Rare Side Effects Of Pertuzumab:

  • Cardiovascular:

    • Left Ventricular Dysfunction
    • Peripheral Edema
  • Central Nervous System:

    • Peripheral Sensory Neuropathy
    • Peripheral Neuropathy
  • Dermatologic:

    • Nail Disease
    • Paronychia
  • Gastrointestinal:

    • Dyspepsia
  • Hematologic & Oncologic:

    • Thrombocytopenia
  • Hepatic:

    • Increased Serum Alanine Aminotransferase
  • Ophthalmic:

    • Increased Lacrimation
  • Respiratory:

    • Dyspnea
    • Nasopharyngitis
    • Oropharyngeal Pain
    • Cough

Contraindications to Pertuzumab:

Hypersensitivity to pertuzumab and any component of the formulation

Warnings and precautions

  • Cardiotoxicity: [US Boxed Warning]

    • Pertuzumab has been shown to cause heart failure and decreased left ventricular ejection fraction. Therefore, it is important to monitor your cardiac health.
    • In the event of severe left-ventricular dysfunction, it is important to immediately stop therapy.
    • Cardiotoxicity can be caused by previous anthracycline treatment or chest radiation.
    • The rate of cardiotoxicity is dependent on whether pertuzumab has been given as a combination or placebo.
    • Patients with breast cancer were more likely to have LV dysfunction in the early stages of neoadjuvant treatment. However, patients who received adjuvant treatment with pertuzumab had a slightly higher incidence of symptomatic cardiac failure.
    • Pertuzumab therapy resulted in a decrease of left ventricular function in patients with borderline LV function.
    • Therapy should include a check of left ventricular ejection fraction every three months.
    • Therapy should be stopped if the LVEF drops below the threshold for early breast cancer/metastatic/early metastatic.
    • If there is no improvement, or any further reduction in symptoms, the therapy should be discontinued.
  • Adverse events in the GI:

    • Pertuzumab, trastuzumab, and docetaxel may cause diarrhea. This is often treated with loperamide and seldom requires treatment delay.
  • Hypersensitivity

    • Severe hypersensitivity including anaphylaxis or angioedema can be seen
    • Pertuzumab recipients have a higher incidence of hypersensitivity than those who received placebo.
    • Hypersensitivity requires immediate treatment and close monitoring.
  • Infusion reaction

    • Infusion reaction is defined as hypersensitivity, anaphylactic response, acute infusion reaction or cytokine production during or on the same infusion day; other common reactions include fever, fatigue, weakness, headache, myalgia and/or vomiting.
    • Monitor for at least 60 minutes following the first dose, and for at least 30 minutes during subsequent cycles.
    • With the right management, interruptions or slowing down of infusions in infusion reactions are possible
    • In the event of severe reactions to infusions, it is best not to resume therapy.

Monitoring parameters:

  • Pregnancy status
  • HER2 expression
  • Echo for LVEF at baseline and every 3 monthly
  • Monitor for hypersensitivity/infusion reactions

How to administer Pertuzumab (Perjeta)?

Initial dose:

  • You should administer it intravenously (840 mg) for at least 1 hour.

Maintenance dose

  • Infusion intravenous of (420 mg) slowly over half an hour to one hour.

Pertuzumab or trastuzumab can be administered together in combination therapy. However, taxane should always be administered after trastuzumab. Patients receiving anthracycline-based treatment should instill trastuzumab or pertuzumab after they have completed their anthracycline therapy. Infusion reactions should be monitored for between 30-60 minutes following each combination drug. After the infusion of pertuzumab, one hour monitoring is recommended. Half an hour observation is needed for subsequent cycles.

Mechanism of action of Pertuzumab (Perjeta):

  • Pertuzumab, a recombinant monoclonal humanized antibody, targets the extracellular human epidermal Growth Factor 2 (HER2) dimerization domain.
  • It stops cell growth and causes apoptosis. Pertuzumab binds differently to HER2 than trastuzumab.
  • Therefore, a combination of these drugs can cause more effective inhibition of HER2 signaling.

Half-life elimination:

  • Terminal: 18 days

International Brands of Pertuzumab:

  • Perjeta

Pertuzumab Brands in Pakistan:

No Brands Available in Pakistan.


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