Welcome to “A to Z: Drugs in Highlight”
This series is designed to delve into the intricate realm of pharmaceutical drugs. As the world of pharmaceuticals continues to evolve with new discoveries and emerging challenges, we aim to shed light on the diverse array of medications available today, ranging from blockbuster medications to those that may not be as familiar. Whether you’re a healthcare professional, a student, or simply someone with a curious mind, “A to Z: Drugs in Highlight” promises to be an enlightening and engaging series.
H is for HERCEPTIN®
HERCEPTIN® (from Genentech, a subsidiary of the Roche Group) uses trastuzumab for treatment of breast cancer and stomach cancer. It is available as a powder to be made up in a solution for infusion into a vein or as ready-to-use solution for subcutaneous injection.
How it works:
HERCEPTIN® is used in cancers that overexpress human epidermal growth factor receptor 2 (HER2), meaning the cancer cells produce large quantities of the HER2 protein, which promotes faster tumour growth. HER2 overexpression occurs in about a quarter of breast cancers and a fifth of gastric cancers.
The active ingredient in Herceptin, trastuzumab, is a monoclonal antibody designed to attach to HER2. This attachment activates cells of the immune system, which then kill the tumour cells. Trastuzumab also stops HER2 signals that cause the tumour cells to grow.
By infusion into a vein, HERCEPTIN® is given over 90 minutes every week or every three weeks for breast cancer, and every three weeks for gastric cancer. The dose administered depends on several factors including the patient’s body weight, condition to be treated, and timing. By subcutaneous injection, the dose of HERCEPTIN® is 600 mg given over 2 to 5 minutes every three weeks.
Market impact:
HERCEPTIN® is approved for marketing in many countries across the world including in the United States (approved by the FDA in September 1998 (intravenous) and February 2019 (subcutaneous)) and Europe (approved by the EMA in August 2000). It has been used to treat more than 2.3 million patients worldwide.
HERCEPTIN® has been a major revenue generator for the Roche Group, with annual sales peaking around USD 7 billion. However, sales have seen a decline in recent years due to the introduction of biosimilars. In 2023, HERCEPTIN® generated approximately USD 1.83 billion for the Roche Group.
Patent protection:
Many of the patents protecting HERCEPTIN® have now expired, although there are some patent rights still in force protecting various aspects of the HERCEPTIN® technology.
For example, US patent no. 10808037 relates to a method for producing an antibody, comprising expressing the antibody in a Chinese Hamster Ovary (CHO) recombinant host cell culture, and following a production phase of the cell culture, sparging the pre-harvest cell culture fluid of the recombinant host cell with air to inhibit reduction of a disulfide bond in the antibody during processing, wherein the antibody is a therapeutic monoclonal antibody that binds to human epidermal growth factor receptor 2 (HER2), and wherein the air sparging is continued until the amount of dissolved oxygen (dO2) in the pre-harvest cell culture fluid is at least 10%.
European patent no. 2459167 relates to a liquid, highly concentrated, stable pharmaceutical atni-HER2 antibody formulation for subcutaneous injection comprising 120 mg/ml Trastuzumab, 20 mM L-histidine/HCl pH 5.5, 210 mM α, α-trehalose dihydrate, 10 mM methionine, 0.04% polysorbate 20 and 2'000 U/ml rHuPH20. The grant of European patent no. 2459167 was opposed. However, the patent was finally maintained in its current amended form by the European Patent Office’s Opposition Division in 2022.
