Early Results for ACE‑106 (ACE‑86225106): A Selective PARP1 Inhibitor for HRR‑Mutant Cancers

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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 […]

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Helicon Peptides: Degrading Active AR to Overcome Prostate Cancer Resistance

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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 […]

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ctDNA and Fragmentomics Reveal New Predictors of Survival in 177 Lu-PSMA–617 mCRPC

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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 […]

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Phase 1 225Ac-J591 Trial: Strong Activity in Advanced Prostate Cancer, with Improved Outcomes Using a Fractionated Dosing Approach

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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. […]

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AM109: A PSMA‑Targeted CD137 Bispecific Antibody for Metastatic Castration‑Resistant Prostate Cancer (mCRPC / mAPMR)

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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 […]

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Astatine-211 PSMA-5: Scalable Alpha Therapy for Refractory Prostate Cancer

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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 […]

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A nano-PROTAC on the horizon: combining targeted protein degradation and ferroptosis for advanced prostate cancer

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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 […]

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Deutenzalutamide in mCRPC: Meaningful Benefit in the HC‑1119‑04 Trial

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Nature reports the results of the HC‑1119‑04 trial, a randomized, multicenter, double‑blind, placebo‑controlled phase 3 study of deutenzalutamide (HC‑1119) in metastatic castration‑resistant prostate cancer (mCRPC) after treatment with abiraterone and docetaxel. The trial was conducted in China and enrolled 417 patients, with 276 randomized to deutenzalutamide 80 mg once daily and 141 to placebo. All […]

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