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Author Details
Written By
Pallavi
Reviewed By
Shital Pawar

Last updated : 25 oct 2025 | 06:18 AM (IST)

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TRASTUZUMAB

History of Trastuzumab

Trastuzumab (Herceptin) was developed by Genentech scientists, including Axel Ullrich and H. Michael Shepard, with support from research by Robert Weinberg and Mark Greene on the HER2 receptor. Dr. Dennis Slamon led the clinical trials, which began in 1992, and the drug gained FDA approval in 1998 after showing strong results. Later, in 2014, Biocon and Mylan received approval to market a biosimilar version, leading to a legal dispute with Roche that was settled in 2016, allowing both companies to launch their biosimilars.


Approved Uses of Trastuzumab

    Trastuzumab is used to treat breast and stomach cancers that have high levels of the HER2 protein. It works by blocking this protein to stop cancer cells from growing and helps the body’s immune system fight them more effectively.


Mechanism of Action Trastuzumab

    The approved trastuzumab works by targeting the HER2 (human epidermal growth factor receptor 2) protein, which is overexpressed in certain types of cancer cells, particularly breast and gastric cancers. Trastuzumab is a monoclonal antibody that binds specifically to the extracellular domain of the HER2 receptor. This binding blocks the receptor’s activation and downstream signaling pathways that promote cell growth and survival. Additionally, trastuzumab mediates antibody-dependent cellular cytotoxicity (ADCC), a process where immune cells are recruited to destroy the cancer cells. Through these mechanisms, trastuzumab inhibits the proliferation of HER2-positive tumor cells and helps slow or stop cancer progression.


Administration of Trastuzumab

    Trastuzumab can be given either as an intravenous (IV) infusion or a subcutaneous (SC) injection. The IV form is usually infused slowly into a vein, with the first dose taking about 90 minutes and later doses around 30 minutes if well tolerated. The SC form is injected under the skin, typically in the thigh, over a few minutes. The dosing schedule depends on the treatment plan and is usually given weekly or every three weeks as prescribed by the doctor.


Side Effects of Trastuzumab

    Trastuzumab can cause a range of side effects, from mild to serious. Common side effects include fever, chills, fatigue, nausea, vomiting, diarrhea, headache, and reactions during infusion such as shortness of breath or flushing. Some people may also experience muscle or joint pain and skin rashes. More serious side effects, though less common, include heart-related issues like reduced heart function or heart failure, especially in patients who have received certain chemotherapy drugs. In rare cases, severe allergic reactions, lung problems, or liver abnormalities may occur. Regular medical checkups are important to monitor and manage these effects during treatment.


Contraindications and Precautions

    Trastuzumab is contraindicated in patients with a known hypersensitivity to trastuzumab or any of its components, especially if they have experienced severe allergic or infusion-related reactions in the past. It should be used with extreme caution in patients with pre-existing heart conditions, such as congestive heart failure or reduced left ventricular ejection fraction, as trastuzumab can worsen cardiac function.

    Before starting treatment, a baseline heart function test (e.g., echocardiogram or MUGA scan) is recommended, and regular monitoring should continue throughout therapy. Caution is also advised in patients with lung diseases, as trastuzumab can rarely cause interstitial lung disease or pneumonitis. During pregnancy, trastuzumab is generally avoided due to the risk of harm to the unborn baby, and effective contraception is advised during and for several months after treatment. Overall, close medical supervision is essential to minimize potential risks and manage any complications early.


Final word

    Trastuzumab is a targeted therapy that has significantly improved outcomes for patients with HER2-positive breast and gastric cancers. By specifically blocking the HER2 receptor, it helps slow cancer progression and enhances the effectiveness of other treatments. While generally well tolerated, it requires careful monitoring, especially for heart-related side effects. When used appropriately under medical supervision, trastuzumab offers a valuable and effective option in the treatment of HER2-positive cancers.


Frequently Asked Questions (FAQs) about Trastuzumab

Q1. How does trastuzumab specifically target cancer cells?

Trastuzumab binds to the extracellular domain of the HER2 receptor, which is over expressed in certain cancer cells. This blocks the receptor's signaling pathways involved in cell growth and survival, while also activating the immune system to destroy the cancer cells through antibody-dependent cellular cytotoxicity (ADCC).

Q2. Can trastuzumab be combined with other therapies?

Yes, trastuzumab is often used in combination with chemotherapy, hormone therapy, or other targeted agents (such as pertuzumab) to improve treatment outcomes, particularly in HER2-positive breast cancer. The combination depends on the stage and type of cancer.

Q3. What cardiac monitoring is required during trastuzumab therapy?

Patients receiving trastuzumab must undergo regular assessment of left ventricular ejection fraction (LVEF) before starting treatment and every 3 months during therapy. Monitoring helps detect early signs of cardio-toxicity, allowing timely intervention.

Q4. Is trastuzumab effective in HER2-low breast cancer?

Traditional trastuzumab therapy is not approved for HER2-low breast cancer. However, new antibody-drug conjugates (ADCs) like trastuzumab deruxtecan have shown promise in HER2-low expressing tumors and are being explored in clinical settings.

Q5. What is the difference between intravenous (IV) and subcutaneous (SC) trastuzumab?

IV trastuzumab requires infusion in a clinical setting and takes longer, especially the first dose. The SC formulation, which includes a fixed dose and recombinant human hyaluronidase, is injected under the skin in a few minutes and may be more convenient for eligible patients.

Q6. How long is trastuzumab treatment continued in early-stage breast cancer?

In early-stage HER2-positive breast cancer, trastuzumab is typically given for one year. However, the exact duration may vary depending on individual response, treatment goals, and tolerance.

Q7. Can trastuzumab be used during pregnancy or breastfeeding?

Trastuzumab is not recommended during pregnancy due to the risk of fetal harm, including oligohydramnios and potential kidney issues in the fetus. Breastfeeding should also be avoided during and for several months after treatment.

8. What are the signs of trastuzumab-induced cardiotoxicity?

Symptoms may include shortness of breath, fatigue, swelling in the legs or feet, and reduced exercise tolerance. Any of these signs should be reported to a doctor immediately for evaluation.

Q9. Are biosimilars of trastuzumab available?

Yes, several trastuzumab biosimilars have been approved globally. These biosimilars have shown similar efficacy, safety, and quality to the reference product and may provide cost-effective treatment options.

Q10. What should be done if a dose of trastuzumab is missed?

If a scheduled dose is missed, the healthcare provider will determine when to resume treatment and may adjust the dosing schedule based on the time since the last dose and the patient’s overall condition.


Medical Advisory

    Information provided is for educational purposes only and should not replace professional medical advice. Always consult your doctor before use.

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