Tag Archive for: PARP inhibitor

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

/in , , /by

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 […]

Read more

BRCAAway OS Update: Abiraterone + Olaparib Extends Survival by 5 Years in HRRm mCRPC

/in , , /by

The BRCAAway trial brings strong new data on treating metastatic castration-resistant prostate cancer, or mCRPC, in patients with specific DNA repair defects known as homologous recombination repair mutations, or HRRm. This phase 2 study tested abiraterone alone, olaparib alone, or the two drugs together as first-line therapy. It focused on patients with germline or somatic […]

Read more

EvoPAR-PR01: Saruparib (AZD5305) Phase III Trial in Metastatic Castration-Sensitive Prostate Cancer

/in , , /by

Saruparib (AZD5305), a next-generation PARP1-selective inhibitor, represents a promising evolution in prostate cancer therapy, particularly for metastatic castration-sensitive disease (mCSPC), through the ongoing phase III EvoPAR-PR01 trial. Unlike first-generation PARP inhibitors (PARPi) such as olaparib that target both PARP1 and PARP2, saruparib specifically inhibits and traps PARP1 on DNA damage sites, sparing PARP2 to potentially […]

Read more

SPR1020: a Promising PARP1-Selective Inhibitor in Advanced Solid Tumors (Including mCRPC)

/in , , , /by

A  first-in-human Phase 1/2 trial of SPR1020, a highly selective PARP1 inhibitor, dosed its inaugural patient, igniting hope for patients with advanced solid tumors harboring DNA repair deficiencies. This open-label, multicenter study employs a classic 3+3 dose-escalation design to pinpoint the recommended Phase II dose or maximum tolerated dose, transitioning seamlessly into expansion cohorts tailored […]

Read more

BrUOG360 Phase Ib/II Trial: Copanlisib Plus Rucaparib for mCRPC With HRD

/in , , , /by

Copanlisib combined with rucaparib demonstrates tolerability and early signals of activity in metastatic castration-resistant prostate cancer (mCRPC), according to results from the BrUOG360 phase Ib/II trial published in late 2025. ​Metastatic castration-resistant prostate cancer with homologous recombination deficiency (HRD) responds to PARP inhibitors like rucaparib, but many patients develop resistance through alternative DNA repair pathways. […]

Read more