Pipeline of TROP-2-Targeted Immunotherapies

This competitive intelligence report about TROP-2-Targeted Immunotherapies provides a competitor evaluation in the field of product candidates in research and development targeting TROP-2. This report will be prepared on demand within one working day upon order placement. The report lists TROP-2-targeted R&D programs by R&D phase in a tabular format and describes in brief the profile of TROP-2-targeted immunotherapies by drug modality. The report will be provided in pdf format and sent by e-mail to the customer.

As an example of this category of on demand reports, please see our free sample report of “Pipeline of 5T4-Targeted Immunotherapies”.

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.

Two Trop-2 directed antibody-drug conjugates are currently approved and commerciliazed: Trodelvy and Datroway. 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. DATROWAY is comprised of a humanized anti-TROP2 IgG1 monoclonal antibody, attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers.

Trodelvy is currently approved in more than 50 countries for second-line or later metastatic triple-negative breast cancer (TNBC) patients and in more than 40 countries for certain patients with pre-treated HR+/HER2- metastatic breast cancer. Trodelvy is currently being evaluated in multiple ongoing Phase 3 trials across a range of tumor types with high Trop-2 expression. These studies with Trodelvy, both in monotherapy and in combination with pembrolizumab, involve earlier lines of treatment for TNBC and HR+/HER2- breast cancer—including in curative settings—as well as in lung and gynecologic cancers, where previous proof-of-concept studies have demonstrated clinical activity.

DATROWAY (6 mg/kg) is approved in more than 30 countries worldwide for the treatment of adult patients with unresectable or metastatic HR positive, HER2 negative (IHC 0, IHC 1+ or IHC 2+/ISH-) breast cancer who have received prior endocrine-based therapy and chemotherapy for unresectable or metastatic disease. DATROWAY (6 mg/kg) is approved in Russia and the U.S. for the treatment of adult patients with locally advanced or metastatic EGFR-mutated NSCLC who have received prior EGFR-directed therapy and platinum-based chemotherapy. Continued approval for this indication in the U.S. may be contingent upon verification and description of clinical benefit in the confirmatory trial.

Trodelvy already became a blockbuster biologic with 2024 sales of US$ 1,315 mln.

The commercial success of Trodelvy and the clinical validation of TROP-2 by Trodelvy and Datroway has attracted many followers applying their proprietary drug modality technologies to generate next generation TROP2-targeted immunotherapy candidates.