Detailed introduction to the drug properties of Gosatuzumab/Todavir

Gosatuzumab/Trodelvy (Trodelvy) is a new type of targeted drug that represents an important breakthrough in antibody-drug conjugate technology (ADC) in tumor treatment. Its structure connects a humanized antibody targeting the Trop-2 receptor to the potent cytotoxic drug SN-38. It combines the dual mechanism of target accuracy and chemotherapy efficacy, and has unique therapeutic advantages.

The Trop-2 protein targeted by Trodelvy is a transmembrane glycoprotein that is highly expressed in malignant tumors of various epithelial origins, while its expression is lower in normal tissues, so it has good targeting properties. The antibody part of the drug can accurately recognize Trop-2 on the surface of tumor cells, and then release the coupled SN-38 into the tumor cells through endocytosis, blocking the function of DNA topoisomerase I, thereby inhibiting tumor cell replication and inducing apoptosis.

In addition,The linker used by Trodelvy is pH-sensitive and can be broken in the acidic environment within tumor cells to accurately release cytotoxic drugs and reduce toxic damage to normal tissues. Its "bystander effect" also causes neighboring tumor cells that do not express Trop-2 to be killed within a certain range, improving treatment coverage.

The drug has been approved by the FDA for the treatment of triple-negative breast cancer (mTNBC), HR+/HER2- breast cancer and urothelial cancer, especially for patients who have failed multiple lines of treatment. Its clinical efficacy is superior to traditional chemotherapy drugs in some refractory tumors.

From a pharmacokinetic perspective,Trodelvy has a moderate half-life, which can not only maintain a stable blood concentration, but also help reduce accumulation toxicity; it is mainly metabolized by the liver, so attention should be paid to the drug or genetic differences in the UGT1A1 metabolism pathway. Common adverse reactions include leukopenia, nausea, hair loss, and diarrhea, which can all be managed through supportive care.

Reference materials:https://www.trodelvy.com/