TROP-2-Targeted Immunotherapy Pipeline Review

TROP-2-Targeted Immunotherapy Pipeline Review

Target: TROP-2; trophoblast antigen 2; epithelial glycoprotein-1 (EGP-1)

Product Category: Antibody; Cells; mRNA

This product provides basic information on immunotherapeutics on the market and in R&D targeting TROP-2.

This product consists of:

• Competitors described in a tabular format covering drug code/INN, target(s)/MoA, class of compound, product category, indication(s) & R&D stage.
• Project History with links to source of information (press release, homepage, abstracts, presentations, annual reports etc).
• One-month online access to La Merie Publishing’s database for immunotherapeutics targeting TROP-2 (prerequisite: access to internet).

This product is delivered on the very same day of purchase by e-mail containing competitor and project history reports in pdf format and database credentials. Reports are prepared on the same day.

The transmembrane glycoprotein Trop-2 is highly expressed in many cancers, but not all, and has differential expression in certain normal tissues. Trop-2 is also known as trophoblast antigen 2, cell surface glycoprotein Trop2, gastrointestinal tumor-associated antigen GA7331, pancreatic carcinoma marker protein GA733-1, membrane component chromosome 1 surface marker 1 M1S1, epithelial glycoprotein-1, EGP-1, CAA1, Gelatinous Drop-Like Corneal Dystrophy GDLD, and TTD2. It is coded by the gene Tacstd2. It is about 35 kDa. Trop2 spans the cellular membrane: it has an extracellular, a transmembrane, and an intracellular domain, along with a cytoplasmic tail essential for signaling.

Trop-2 is a cell surface antigen highly expressed in multiple tumor types, including in more than 90% of breast and bladder cancers. Trop-2 expression correlates with tumor aggressiveness. Trop-2 overexpression promotes the growth, proliferation, and metastasis of tumor cells.

Trodelvy^® (sacituzumab govitecan-hziy) is a first-in-class Trop-2 directed antibody-drug conjugate. Trodelvy is intentionally designed with a proprietary hydrolyzable linker attached to SN-38, a topoisomerase I inhibitor payload. This unique combination delivers potent activity to both Trop-2 expressing cells and the microenvironment.

Trodelvy is approved in almost 50 countries, with multiple additional regulatory reviews underway worldwide, for the treatment of adult patients with unresectable locally advanced or metastatic triple-negative breast cancer (TNBC) who have received two or more prior systemic therapies, at least one of them for metastatic disease. In the U.S., Trodelvy also has accelerated approval for treatment of certain patients with second-line metastatic urothelial cancer (UC); see below for the full U.S. indication for Trodelvy.

With 2022 sales of US$ 680 mln (+79% vs previous year), Trodelvy is on the way to become a blockbuster biologic.

This clinical and commercial success of Trodelvy has attracted many followers applying their proprietary drug modality technologies to generate next generation TROP2-targeted immunotherapy candidates.