Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 30mg/mL (420mg/14 mL)
Early Breast Cancer
Neoadjuvant treatment
- Indicated in combination with trastuzumab (or trastuzumab hyaluronidase-oysk) and docetaxel for the neoadjuvant treatment of patients with HER2-positive, locally advanced, inflammatory, or early stage breast cancer (either greater than 2 cm in diameter or node positive) as part of a complete treatment regimen for early breast cancer
- Initial dose: Pertuzumab 840 mg IV infusion, THEN 420 mg IV infusion q3Weeks AND
- Trastuzumab: 8 mg/kg IV infusion initially, then 6 mg/kg IV infusion q3Weeks OR
- Trastuzumab hyaluronidase-oysk: 600 mg/10,000 units (600 mg trastuzumab and 10,000 units hyaluronidase) SC q3Weeks irrespective of body weight
- Docetaxel: 75 mg/m² IV infusion initially; may increase to 100 mg/m² IV infusion q3Weeks if initial dose is well tolerated
- Administer sequentially; pertuzumab and trastuzumab or trastuzumab hyaluronidase-oysk can be given in any order; taxane should be administered after pertuzumab and trastuzumab or trastuzumab hyaluronidase-oysk
-
Neoadjuvant dosage regimens
- Administered q3Weeks for 3-6 cycles as part of 1 of the following treatment regimens for early breast cancer
- 4 preoperative cycles of pertuzumab in combination with trastuzumab and docetaxel followed by 3 postoperative cycles of fluorouracil, epirubicin, and cyclophosphamide (FEC) as given in the NeoSphere trial
- 3 or 4 preoperative cycles of FEC alone followed by 3 or 4 preoperative cycles of pertuzumab in combination with docetaxel and trastuzumab as given in TRYPHAENA and BERENICE trials 6 preoperative cycles of pertuzumab in combination with docetaxel, carboplatin, and trastuzumab (TCH) (escalation of docetaxel above 75 mg/m² is not recommended) as given in TRYPHAENA trial
- 4 preoperative cycles of dose-dense doxorubicin and cyclophosphamide (ddAC) alone followed by 4 preoperative cycles of pertuzumab in combination with paclitaxel and trastuzumab as given in BERENICE trial
- Following surgery, patients should continue to receive trastuzumab or trastuzumab hyaluronidase-oysk to complete 1 year of treatment (up to 18 cycles)
Adjuvant treatment
- Indicated in combination with trastuzumab or trastuzumab hyaluronidase-oysk and chemotherapy for adjuvant treatment of patients with HER2-positive early breast cancer at high risk of recurrence
- Initial dose: Pertuzumab 840 mg IV infusion, THEN 420 mg IV infusion q3Weeks AND
- Trastuzumab: 8 mg/kg IV initially, then 6 mg/kg IV q3Weeks OR
- Trastuzumab hyaluronidase-oysk: 600 mg/10,000 units (600 mg trastuzumab and 10,000 units hyaluronidase) SC q3Weeks irrespective of body weight
- For a total of 1 year (up to 18 cycles) or until disease recurrence or unmanageable toxicity, whichever occurs first, as part of a complete regimen for early breast cancer, including standard anthracycline and/or taxane-based chemotherapy as given in APHINITY trial
- Pertuzumab and trastuzumab or trastuzumab hyaluronidase-oysk should start on Day 1 of the first taxane-containing cycle
Metastatic Breast Cancer
Indicated in combination with trastuzumab and docetaxel for HER2-positive metastatic breast cancer in patients who have not received prior anti-HER2 therapy or chemotherapy for metastatic disease
Initial dose: 840 mg IV infusion over 60 min, THEN 420 mg IV infusion over 30-60 min q3Weeks thereafter
Trastuzumab: 8 mg/kg IV infusion over 90 min initially, THEN 6 mg/kg IV infusion over 30-90 min q3Weeks thereafter
Docetaxel: 75 mg/m² IV infusion initially; may increase to 100 mg/m² IV infusion q3Weeks if initial dose is well tolerated
Dosage Modifications
Withhold or discontinue pertuzumab if trastuzumab is withheld or discontinued; may continue therapy with trastuzumab if docetaxel has been discontinued
Pertuzumab dose reductions are not recommended
Hepatic impairment: Safety and efficacy not established
Renal impairment
- Mild-to-moderate (CrCl 30-90 mL/min): No dosage adjustment necessary
- Severe (CrCl <30 mL/min): Safety and efficacy not established
Hypersensitivity
- Discontinue immediately if severe hypersensitivity reaction occurs
Infusion-related reactions
- Slow or interrupt infusion rate of if the patient develops an infusion-related reaction
Left ventricular ejection fraction (LVEF)
- Monitor LVEF ~q12Weeks
- For patients receiving anthracycline-based chemotherapy, a LVEF of ≥50% is required after completion of anthracyclines, before starting pertuzumab and trastuzumab
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Metastatic breast cancer
- Monitor LVEF ~q12Weeks
- Pretreatment LVEF is ≥55%
- Monitor LVEF ~q12Weeks (once during neoadjuvant therapy)
- LVEF drops to <40% OR LVEF 40-45% with ≥10% decrease below baseline: Withhold pertuzumab and trastuzumab or trastuzumab hyaluronidase-oysk for at least 3 weeks
- LVEF >45% or 40-45% with a decrease of <10% points below baseline: Resume pertuzumab and trastuzumab or trastuzumab hyaluronidase-oysk after 3 weeks if LVEF recovered
-
Early breast cancer
- Monitor LVEF ~q12Weeks
- Pretreatment LVEF is ≥50%
- For patients receiving anthracycline-based chemotherapy, a LVEF of ≥50% is required after completion of anthracyclines, before starting pertuzumab and trastuzumab or trastuzumab hyaluronidase-oysk
- LVEF <50% with ≥10% decrease below baseline: Withhold pertuzumab and trastuzumab or trastuzumab hyaluronidase-oysk for at least 3 weeks
- LVEF ≥50% or <10% points below baseline: Resume pertuzumab and trastuzumab or or trastuzumab hyaluronidase-oysk
Dosing Considerations
Patient selection
- Patient selection should be based on HER2 protein overexpression or HER2 gene amplification in tumor specimen
- Assessment of HER2 protein overexpression and HER2 gene amplification should be performed using FDA-approved tests specific for breast cancer by laboratories with demonstrated proficiency
- Information on FDA-approved tests for the detection of HER2 protein overexpression and HER2 gene amplification is available at: http://www.fda.gov/CompanionDiagnostics
Gastric Cancer (Orphan)
Orphan designation for treatment of gastric cancer
Orphan sponsor
- Genentech, Inc.; 1 DNA Way; South San Francisco, CA 94080-4990
Safety and efficacy not established
Based on a population pharmacokinetic analysis, no significant difference was observed in the pharmacokinetics of pertuzumab between patients <65 years and patients ≥65 years
Adverse Effects
>10% (all grades,pertuzumab in combination with trastuzumab and docetaxel)
Alopecia (61%)
Diarrhea (67%)
Nausea (42%)
Neutropenia (53%)
Fatigue (37%)
Rash (34%)
Peripheral neuropathy (32%)
Decreased appetite (29%)
Mucosal inflammation (28%)
Asthenia (26%) Vomiting (24%)
Peripheral edema (23%)
Nail disorder (23%)
Myalgia (23%)
Anemia (23%)
Headache (21%)
Stomatitis (19%)
Pyrexia (19%)
Dysgeusia (18%)
Leukopenia (18%)
Upper respiratory tract infection (17%)
Constipation (15%) Arthralgia (15%)
Dyspnea (14%)
Febrile neutropenia (14%)
Increased lacrimation (14%)
Pruritus (14%)
Insomnia (13%)
Dizziness (13%)
Nasopharyngitis (12%)
Dry skin (11%)
>10% (Grade 3/4, pertuzumab in combination with trastuzumab and docetaxel)
Febrile neutropenia (13%)
Leukopenia (12%)
1-10% (Grade 3/4, pertuzumab in combination with trastuzumab and docetaxel)
Fatigue (2%)
Asthenia (2%)
Anemia (2%)
Mucosal inflammation (1%)
Pyrexia (1%)
Nail disorder (1%)
Nausea (1%)
Vomiting (1%)
Headache (1%)
<1% (Grade 3/4, pertuzumab in combination with trastuzumab and docetaxel)
Peripheral edema (0.5%)
Stomatitis (0.5%)
Postmarketing Reports
Thrombocytopenia
Infusion reactions
Tumor lysis syndrome (TLS)
Warnings
Black Box Warnings
Left ventricular dysfunction (LVEF)
- Subclinical and clinical cardiac failure manifesting as decreased LVEF and CHF may occur with pertuzumab therapy
- Evaluate cardiac function prior to and during treatment
- Discontinue treatment for a confirmed clinically significant decrease in left ventricular function
Embryo-fetal toxicity
- Exposure to pertuzumab can result in embryo-fetal death and birth defects
- Advise patients of these risks and the need for effective contraception
- Also see Pregnancy
Contraindications
Hypersensitivity
Cautions
Decreases in LVEF have been reported with drugs that block HER2 activity; assess LVEF prior to initiation of pertuzumab and monitor regularly during treatment (see Dosage Modifications and Black Box Warnings)
Fetal harm may occur when pertuzumab is administered to a pregnant woman (see Pregnancy)
Infusion reactions has been associated with pertuzumab administration; observe patients closely for 60 minutes after the first infusion and for 30 minutes after subsequent pertuzumab infusions (see Dosing Modifications)
Severe hypersensitivity, including anaphylaxis, has been observed in clinical trials; monitor and treat appropriately if such reactions occur (see Contraindications and Dosage Modifications)
Cases of possible tumor lysis syndrome reported; patients with significant tumor burden (e.g., bulky metastases) may be at higher risk; patients could present with hyperuricemia, hyperphosphatemia, and acute renal failure which may represent possible TLS; providers should consider additional monitoring and/or treatment as clinically indicated
Pregnancy & Lactation
Pregnancy
There is a pregnancy pharmacovigilance program for therapy administered during pregnancy, or if patient becomes pregnant while receiving therapy or within 7 months following last dose in combination with trastuzumab, health care providers and patients should immediately report exposure to Genentech at 1-888-835-2555
Based on its mechanism of action and findings in animal studies, therapy can cause fetal harm when administered to a pregnant woman; there are no available data on use of drug in pregnant women; however, in post-marketing reports, use of another HER2/neu receptor antagonist (trastuzumab) during pregnancy resulted in cases of oligohydramnios and oligohydramnios sequence manifesting as pulmonary hypoplasia, skeletal abnormalities, and neonatal death
Monitor women who received drug in combination with trastuzumab during pregnancy or within 7 months prior to conception for oligohydramnios; if oligohydramnios occurs, perform fetal testing that is appropriate for gestational age and consistent with community standards of care
Verify pregnancy status of females of reproductive potential prior to initiation of therapy
Based on mechanism of action and animal data, drug can cause embryo-fetal harm when administered during pregnancy; advise females of reproductive potential to use effective contraception during treatment and for 7 months following last dose in combination with trastuzumab
Animal data
- In an animal reproduction study, administration to pregnant cynomolgus monkeys during period of organogenesis resulted in oligohydramnios, delayed fetal kidney development, and embryo-fetal deaths at clinically relevant exposures that were 2.5 to 20-fold greater than exposures in humans receiving the recommended dose, based on Cmax; apprise patient of potential risks to a fetus; there are clinical considerations if drug in combination with trastuzumab is used during pregnancy or within 7 months prior to conception
Lactation
There is no information regarding presence of drug in human milk, effects on breastfed infant or on milk production; published data suggest that human IgG is present in human milk but does not enter neonatal and infant circulation in substantial amounts; consider developmental and health benefits of breast feeding along with mother’s clinical need for treatment and any potential adverse effects on breastfed child or from underlying maternal condition; consideration should also take into account elimination half-life of pertuzumab and trastuzumab wash out period of 7 months
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Monoclonal antibody that binds to the extracellular dimerization domain of the human epidermal growth factor receptor 2 protein (HER2); mediates antibody-dependent cellular cytotoxicity by inhibiting proliferation of cells that overexpress HER2
Absorption
With an initial dose of 840 mg followed by a maintenance dose of 420 mg q3Weeks thereafter, steady-state concentration of pertuzumab was reached after first maintenance dose
Elimination
Half-life: 18 days
Total body clearance: 0.24 L/day
Administration
IV Incompatibilities
Do not mix with other drugs
D5W
IV Compatibilities
0.9% NaCl
IV Preparation
Withdraw appropriate volume of pertuzumab from the vials
Dilute into a 250 mL of 0.9% NaCl PVC or non-PVC polyolefin infusion bag
Mix diluted solution by gentle inversion; do not shake
Administer immediately once prepared
If diluted infusion solution is not used immediately, it can be stored at 2-8°C for up to 24 hr
IV Administration
IV infusion only
Do not administer as an IV push or bolus
Loading dose: Infuse over 60 minutes Subsequent doses: Infuse over 30-60 minutes
Monitor for infusion related adverse effects (eg, hypersensitivity, pyrexia, chills, headache, fatigue, asthenia, vomiting) for 60 minutes following first infusion, and for 30 minutes following subsequent infusions
Delayed or missed dose
-
Time between 2 sequential doses <6 weeks
- Administer as soon as possible
- Pertuzumab 420 mg IV AND
- Trastuzumab 6 mg/kg or trastuzumab hyaluronidase-oysk 600 mg/10,000 units SC
- Do not wait until the next planned dose
-
Time between 2 doses >6 weeks
- Readminister loading dose
- Pertuzumab loading dose 840 mg IV, then subsequent doses of 420 IV q3Week thereafter AND
- Trastuzumab loading 8 mg/kg IV, followed 6 mg/kg q3Weeks thereafter OR
- Administer trastuzumab hyaluronidase-oysk 600 mg/10,000 units SC as soon as possible; do not wait until the next planned dose
Storage
Unopened vials
- Refrigerate at 2-8°C (36-46°F) until time of use
- Do not freeze; do not shake
- Keep vial in the outer carton in order to protect from light
Diluted solutions
- Refrigerate at 2-8°C for up to 24 hr
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Perjeta intravenous - | 420 mg/14 mL (30 mg/mL) vial |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
pertuzumab intravenous
PERTUZUMAB - INJECTION
(per-TOOZ-ue-mab)
COMMON BRAND NAME(S): Perjeta
WARNING: Pertuzumab can cause serious (possibly fatal) harm to an unborn baby if used during pregnancy. It should only be used during pregnancy if the benefits outweigh these risks. It is important that men and women using this medication use reliable forms of birth control (such as condoms, birth control pills) while using this medication and for 7 months after treatment stops. If you become pregnant, think you may be pregnant, or cause a pregnancy, tell your doctor right away.
USES: Pertuzumab is used to treat certain types of breast cancer. It is also used to treat early stage breast cancer in patients who will be having surgery to remove the cancer. The types of cancers pertuzumab is used to treat are tumors that produce more than the normal amount of a certain substance called HER2 protein.This medication is called a monoclonal antibody. It works by attaching to the HER2 cancer cells and blocking them from dividing and growing. It may also destroy the cancer cells or signal the body (immune system) to destroy the cancer cells.
HOW TO USE: This medication is given by a health care professional. It is injected slowly into a vein as directed by your doctor, usually once every 3 weeks. Your first infusion will be given over 60 minutes.The dosage, the speed of your injection, and the length of time you receive pertuzumab is based on your medical condition, other treatments you are taking, and your response to pertuzumab treatment.A health care professional should watch you for at least 60 minutes after your first infusion is finished and 30 minutes after the following infusions to make sure you do not have an infusion reaction (see also Side Effects section).Use this medication regularly to get the most benefit from it. To help you remember, mark the days on the calendar when you need to receive the medication.
SIDE EFFECTS: Diarrhea, nausea, vomiting, tiredness, and loss of appetite may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Temporary hair loss may occur. Normal hair growth should return after treatment has ended.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: trouble breathing, numbness/tingling of arms/legs, symptoms of heart failure (such as shortness of breath, swelling ankles/feet, unusual tiredness, unusual/sudden weight gain).Pertuzumab can commonly cause a rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe reaction. Tell your doctor right away if you develop any rash.This medication may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. Tell your doctor right away if you have any signs of infection (such as sore throat that doesn't go away, fever, chills, cough).This medication can sometimes cause a serious infusion (IV) reaction. Immediately tell your doctor if the following side effects occur while this drug is being given: chills, fever, headache, rash, vomiting, and weakness. Your doctor may decrease the speed of your injection.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before using pertuzumab, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: previous cancer treatments (including radiation therapy to the chest), heart disease, high blood pressure, previous severe reaction to monoclonal antibody treatment.Pertuzumab can make you more likely to get infections or may make current infections worse. Stay away from anyone who has an infection that may easily spread (such as chickenpox, COVID-19, measles, flu). Talk to your doctor if you have been exposed to an infection or for more details.Tell your health care professional that you are using pertuzumab before having any immunizations/vaccinations. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially tiredness, loss of appetite and numbness/tingling of arms/legs.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using pertuzumab. Pertuzumab may harm an unborn baby. See also Warning section.It is unknown if this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding is not recommended while using this drug or for 7 months after the last dose. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as heart exams, HER2 testing) should be done before you start using this medication and while you are using it. A pregnancy test should also be done before starting treatment. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: It is important to get each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule.
STORAGE: Not applicable. This medication is given in a hospital or clinic and will not be stored at home.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised March 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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