A new experimental compound, ITRI-148, may represent a meaningful shift in how advanced prostate cancer is treated, particularly in patients who develop resistance to current androgen receptor (AR)-targeted therapies. Resistance to drugs like enzalutamide is frequently driven by AR splice variants such as AR-V7, which lack the ligand-binding domain (LBD) targeted by existing therapies, allowing […]
A new generation of PSMA-targeted T-cell engagers is emerging with a clear goal: preserve the potency seen in hematologic malignancies while overcoming the safety and efficacy barriers that have limited success in solid tumors. A preclinical candidate, ProTCE-PSMA, presented ahead of IND filing in early 2026, illustrates how rapidly this field is evolving beyond first-generation […]
Early-phase data from the ZL-1310-002 trial introduce a potentially important new therapeutic option for patients with advanced neuroendocrine carcinomas (NECs), a group of aggressive malignancies with very limited treatment options after platinum-based chemotherapy. Among these, neuroendocrine prostate cancer (NEPC) represents one of the most clinically challenging subtypes, characterized by rapid progression, resistance to androgen receptor–targeted […]
ACE‑106 (ACE‑86225106) is a highly selective PARP1 inhibitor designed to improve the therapeutic index compared with first‑generation pan‑PARP inhibitors, which broadly inhibit both PARP1 and PARP2 while causing substantial hematologic toxicity. The updated first‑in‑human data from the open‑label, dose‑escalation study show that ACE‑106 is well tolerated, with no dose‑limiting toxicities, no grade 4–5 treatment‑related adverse […]
Current AR therapies like enzalutamide target the inactive, unliganded AR conformation (AROFF) by binding its androgen pocket, preventing activation but leaving already active, agonist-bound AR (ARON), the real driver of tumor transcription and proliferation, untouched. This allows resistant tumors to adapt through AR gene amplification, mutations in the ligand-binding domain, or alternative activation pathways, leading […]
Metastatic castration-resistant prostate cancer (mCRPC) remains one of the most challenging stages of prostate cancer, marked by poor prognosis and limited durable treatment options. The radioligand therapy 177Lu-PSMA-617 (Pluvicto) has emerged as a significant advance, demonstrating an overall survival benefit in selected patients. However, clinical responses vary widely, highlighting an urgent need for biomarkers that […]
225Ac-J591 (Actinium-225 rosopatamab tetraxetan) uses a radioactive particle linked to an antibody that targets PSMA, a protein found on prostate cancer cells, and it is being studied in a phase 1 clinical trial. Unlike more commonly used PSMA treatments that rely on small molecules, this approach uses an antibody, which behaves differently in the body. […]
AM109 is designed as a bispecific agent that links a PSMA‑targeting humanized antibody to a CD137 (4‑1BB)‑targeting affibody, effectively creating a molecular bridge between prostate cancer cells and T cells in the tumor microenvironment. The rationale is straightforward: by restricting CD137 activation to sites where PSMA is expressed, the therapy aims to drive potent anti‑tumor […]
211AtPSMA-5 emerges as a promising targeted alpha therapy for metastatic castration-resistant prostate cancer, particularly in patients who have exhausted standard treatments like androgen receptor pathway inhibitors, docetaxel, and cabazitaxel. This approach leverages astatine-211, a cyclotron-produced alpha emitter generated by bombarding abundant bismuth targets with alpha beams. The compound’s design mirrors established PSMA ligands such as […]
A new study from Wuhan University and the Renmin Hospital of Wuhan University has reported a promising preclinical strategy for advanced prostate cancer, especially castration-resistant prostate cancer (CRPC). The work was published online in Angewandte Chemie International Edition, one of the leading international journals in chemistry. The study describes a new nano-PROTAC platform designed to […]