ADC Drugs For Breast Cancer Treatment

WATERTOWN, Mass. - March 21, 2023 - PRLog -- Dertrastuzumab is an antibody-drug conjugate (ADC) drug consisting of a humanized monoclonal antibody targeting HER2 attached to a topoisomerase 1 inhibitor payload via a tetrapeptide cleavable linker. The antibody can be released to partially target and attach to HER2 on cancer cells, and upon entering the cancer cells, release chemotherapeutic drugs to kill the cancer cells as well as nearby cells.

ADC drugs combine the high specificity of monoclonal antibody drugs with the high activity of small molecule cytotoxic drugs to improve the targeting of tumor drugs and reduce toxic side effects. Currently, 15 ADC drugs have been approved worldwide, including three for breast cancer: T-DM1 and T-DXd, which target HER2, and sacituzumab govitecan, which targets Trop2.

Trastuzumab Emtansine (T-DM1)

Trastuzumab Emtansine (T-DM1) is the first ADC drug approved for breast cancer. As early as 2013 and 2019, it has been approved by FDA for the adjuvant therapy of HER2-positive advanced breast cancer patients who have received trastuzumab and paclitaxel chemotherapy and HER2-positive early breast cancer patients who have residual HER2-positive early breast cancer patients after receiving taxa and trastuzumab neoadjuvant therapy, respectively.

Trastuzumab Deruxtecan (T-Dxd, DS-8201)

The new generation of T-DXd greatly expands the adaptable population. T-DXd is also an ADC drug targeting HER2, jointly developed by AstraZeneca in the UK and Daiichi Sankyo in Japan. It is trastuzumab (Herceptin, Trastuzumab) and exatecan, through the peptide chain composed of compound drugs. T-DXd has a "bystander effect". While killing HER2-positive cells, it is also killing tumor cells with low HER2 expression.

The results of phase 3 clinical research on breast cancer with "low expression of HER2" show that the treatment effect of T-Dxd is significantly better than that of chemotherapy for breast cancer patients with low expression of HER2! The overall median progression-free survival increased from 5.1 months to 9.9 months, and the median overall survival increased from 16.8 months to 23.4 months! Based on this, T-DXd was approved by the US FDA for marketing.

Sacituzumab Govitecan

Sacituzumab govitecan is composed of an antibody targeting Trop-2 linked to SN-38, the active metabolite of the chemotherapy drug Irinotecan. The full name of TROP2 (https://www.biochempeg.com/article/323.html) protein is trophoblast cell surface antigen 2, which is highly expressed in a variety of tumors, such as pancreatic cancer, breast cancer, colon cancer, bladder cancer, oral squamous cell carcinoma and ovarian cancer.

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