ReviewJournal of translational medicine2026
Unlocking the potential of EphA2 with precision-guided cancer therapy: bicycle drug conjugates.
Review in Journal of translational medicine, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
1 citing paper in PubMed.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundTherapeutic advances have improved cancer survival outcomes for an increasing number of patients, but novel approaches are still urgently needed for patients who cannot tolerate, or do not respond to current treatments. Erythropoietin-producing hepatocellular receptor A2 (EphA2) is highly expressed in a variety of solid tumors, which is associated with poor prognosis, especially in tumors considered difficult-to-treat, such as pancreatic and head and neck cancer. MAIN BODY: EphA2 has emerged as a promising therapeutic target for the treatment of solid tumors; however, efficacy and safety issues have halted clinical development of previous EphA2-targeting agents including MEDI-547, DS-8895a, MM-310, and dasatinib. Despite these setbacks, interest in targeting EphA2 in solid tumors remains, with ongoing development of investigational therapies such as antibodies, antibody drug conjugates, EphA2 antagonists, peptide drug conjugates, bicyclic peptide drug conjugates, and tyrosine kinase inhibitors. Among these, BT5528, a Bicycle® Drug Conjugate (BDC), has shown an emerging differentiated safety profile, in contrast to prior EphA2-targeting agents, and promising antitumor activity in patients with advanced solid tumors. BT5528 comprises an EphA2-targeting bicyclic (Bicycle) peptide, linked to the cytotoxin monomethyl auristatin E (MMAE) via a valine-citrulline cleavable linker. The high specificity of BT5528 to EphA2, combined with its high affinity, enables precision-guided delivery of MMAE, while its peptidic nature results in rapid distribution and retention of MMAE within the tumor, limited systemic exposure, and liver-sparing renal elimination.
conclusionThe preclinical and emerging clinical data for BT5528 suggest that novel approaches to targeting EphA2 can achieve efficacy without the safety issues that plagued earlier agents. Here, we review EphA2 as a target and the historical and current clinical development of EphA2-targeting therapeutic agents.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.