Partruvix (pamiparib) / BeOne Medicines - LARVOL DELTA

A novel 18F-labeled brain penetrant PET ligand for imaging poly(ADP-ribose) polymerase-1 (SNMMI 2025) - "Blocking studies with AZD9574, Olaparib, Rucaparib, Veliparib, and Pamiparib significantly reduced intracellular radiotracer uptake, while no significant reduction was observed with UPF-1035, a PARP2-specific inhibitor (Fig. The radiotracer 18F-AZD9574 was synthesized following a previously established protocol (Fig. 1A). Western blot analysis confirmed substantial PARP1 expression in the U87-MG (glioblastoma), 22Rv1 (prostate), PSN-1 (pancreatic), MDA-MB-436 (breast), and MDA-MB-231 (breast) cancer cell lines (Fig."

Brain Cancer • Breast Cancer • Glioblastoma • Oncology • Pancreatic Cancer • Solid Tumor • PARP1 • PARP2

Imaging Parthanatos in Animal Models of Parkinson’s disease (SNMMI 2025) - "In vitro PARP1 immunostaining and autoradiography (AR) using the PARP radioligand [18F]BGB290 were used to compare with the PET imaging results... Immunostaining revealed elevated PARP1 expression in the striatum of the PFF-injected mice (Figure 1A). The PET imaging showed higher SUV at the ipsilateral (Ipsi) striatum of the PFF-injected mice compared to the contralateral striatum, while the hippocampus showed no significant changes between the two groups, consistent with the spreading pattern of α-syn in this animal model. Increased DVRs were observed in striatum-Ipsi (42%, p < 0.05) and the whole brain (20%, p < 0.05)."

Preclinical • CNS Disorders • Movement Disorders • Parkinson's Disease

SPRING: Study of Precision Treatment for Rare Tumours in China Guided by PDO and NGS (clinicaltrials.gov) - P2 | N=200 | Not yet recruiting | Sponsor: Peking University Shenzhen Hospital

Biomarker • New P2 trial • Oncology

Cabozantinib and Pamiparib for the Treatment of Advanced of Refractory Solid Tumors (clinicaltrials.gov) - P1 | N=44 | Active, not recruiting | Sponsor: M.D. Anderson Cancer Center | Trial completion date: Jun 2025 ➔ Jun 2026 | Trial primary completion date: Jun 2025 ➔ Jun 2026

Trial completion date • Trial primary completion date • Oncology • Solid Tumor • ARID1A • BRCA1 • BRCA2 • CHEK1 • CHEK2 • EMSY • PARP1 • PTEN • RAD50

A prospective, single-arm, phase 2 trial exploring the use of pamiparib combined with surufatinib as neoadjuvant therapy for advanced, unresectable ovarian cancer (PASSION). (ASCO 2025) - P2 | "Pamiparib and surufatinib show promising efficacy and manageable toxicity in advanced OC, reshaping the tumor microenvironment and promoting immune infiltration."

Clinical • Metastases • P2 data • Anemia • Leukopenia • Neutropenia • Oncology • Ovarian Cancer • Solid Tumor • CSF1R • FGFR1 • FLT1

Neoadjuvant pamiparib in patients with newly diagnosed advanced ovarian cancer: A single-arm, prospective phase II trial. (ASCO 2025) - "The treatment regimen comprises paclitaxel (175 mg/m^2, Day 1) and carboplatin (AUC 5, Day 2) every three weeks for up to six cycles. The preliminary results suggest that the addition of pamiparib to neoadjuvant chemotherapy plus bevacizumab offers promising efficacy and acceptable safety in newly diagnosed advanced ovarian cancer. Further data will be provided as the study progresses."

Clinical • Metastases • P2 data • Anemia • Endometrial Cancer • Fallopian Tube Cancer • Leukopenia • Neutropenia • Oncology • Ovarian Cancer • Peritoneal Cancer • Solid Tumor • Thrombocytopenia • MUC16

BRIGHT: Biomarker-driven Targeted Therapy in Patients With Recurrent Platinum-resistant Epithelial Ovarian Cancer (clinicaltrials.gov) - P2 | N=108 | Completed | Sponsor: Tongji Hospital | Not yet recruiting ➔ Completed | N=160 ➔ 108 | Trial completion date: Dec 2027 ➔ Feb 2025 | Trial primary completion date: Jun 2024 ➔ Feb 2025

Biomarker • Enrollment change • Platinum resistant • Trial completion • Trial completion date • Trial primary completion date • Epithelial Ovarian Cancer • Oncology • Ovarian Cancer • Solid Tumor • BRCA1

BGB-A317-290-LTE1: Study of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies (clinicaltrials.gov) - P3 | N=430 | Enrolling by invitation | Sponsor: BeiGene | N=300 ➔ 430

Enrollment change • Oncology • Solid Tumor

Research Progress of M6A Methylation Modification in Immunotherapy of Colorectal Cancer. (PubMed, Curr Cancer Drug Targets) - "This review has sys-tematically summarized the latest clinical application of six authorized PARPi, including olaparib, rucaparib, niraparib, talazoparib, fuzuloparib and pamiparib, in monotherapy and combination therapies with chemotherapy, radiotherapy, and immunotherapy, in different kinds of cancer. Furthermore, probable challenges in PARPi application and drug resistance mechanisms have also been discussed. Despite these challenges, further development of new PARP1 inhibitors appears promising as a valuable approach to cancer treatment."

Journal • Colorectal Cancer • Oncology • Solid Tumor

Population Pharmacokinetic Modeling of Total and Unbound Pamiparib in Glioblastoma Patients: Insights into Drug Disposition and Dosing Optimization. (PubMed, Pharmaceutics) - " The total and unbound pamiparib plasma PK are well characterized by a linear one-compartment model, with creatinine clearance as the significant covariate on V/F. Model simulations support further clinical investigation into dose reduction to optimize the benefit-to-risk ratio of pamiparib, particularly in combination therapies."

Journal • PK/PD data • Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Solid Tumor

Engaging an engineered PARP-2 catalytic domain mutant to solve the complex structures harboring approved drugs for structure analyses. (PubMed, Bioorg Chem) - "Consequently, the complex structures of Fluzoparib, Pamiparib, Rucaparib, and Niraparib within PARP-2 were achieved. It suggested that the residues adjacent to Asp766 in the HD and ASL domains and the αJ-αF and ASL-αD interfaces were closely related to the selectivity and trapping mechanism. These results would provide some insights for the design and development of novel PARP-1/2 inhibitors with improved pharmacodynamic properties."

Journal • Oncology • PARP1 • PARP2

Pamiparib-induced replication stress augments the efficacy of temozolomide in GBM PDX models (AACR 2025) - "In conclusion, pamiparib enhances TMZ efficacy in a subset of primary GBM. While further in vivo validation is needed, TLS deficiency may be a key determinant of pamiparib-mediated sensitization."

Clinical • Glioblastoma • Oncology • MGMT • MRE11A

Biomarker-driven targeted therapy in patients with recurrent platinum-resistant epithelial ovarian cancer (BRIGHT): protocol for an open-label, multicenter, umbrella study. (PubMed, Int J Gynecol Cancer) - P2 | "To evaluate the efficacy and safety of biomarker-driven combinatorial therapies of pamiparib, tislelizumab, bevacizumab, and nab-paclitaxel in platinum-resistant, recurrent ovarian cancer. Recruitment is estimated to be completed by 2024 and results may be published by 2027. ClinicalTrials.gov: NCT05044871."

Biomarker • Clinical protocol • IO biomarker • Journal • Platinum resistant • Epithelial Ovarian Cancer • Oncology • Ovarian Cancer • Ovarian Clear Cell Cancer • Solid Tumor • BRCA1 • BRCA2 • CD8

BGB-290-302: Maintenance Treatment With BGB-290 Versus Placebo in Participants With Platinum-sensitive Recurrent Ovarian Cancer (clinicaltrials.gov) - P3 | N=224 | Active, not recruiting | Sponsor: BeiGene | Trial completion date: Jun 2026 ➔ Jun 2027 | Trial primary completion date: Jun 2025 ➔ Jun 2026

Platinum sensitive • Trial completion date • Trial primary completion date • Oncology • Ovarian Cancer • Solid Tumor

Pamiparib in combination with surufatinib in patients with platinum-resistant ovarian cancer who received prior PARP inhibitors: a multicenter, single-arm, phase Ib/II trial (POST-PARPi Trial) (SGO 2025) - No abstract available

Clinical • Combination therapy • P1/2 data • Oncology • Ovarian Cancer • Solid Tumor

Distribution of pamiparib, a novel inhibitor of poly(ADP-ribose)-polymerase (PARP), in tumor tissue analyzed by multimodal imaging. (PubMed, J Pharm Anal) - "Image 1."

Journal • Oncology

Pamiparib Plus Surufatinib Shows Modest Activity in Platinum-Resistant Ovarian Cancer (OncLive) - P1/2 | N=38 | NCT05494580 | "The combination of pamiparib and surufatinib elicited responses with the potential for enrichment according to circulating tumor DNA (ctDNA) assessment in patients with platinum-resistant ovarian cancer who received prior PARP inhibitors, according to data from the single-arm, phase 1b/2 POST-PARPi trial (NCT05494580) presented during the 2025 SGO Annual Meeting on Women’s Cancer. At a data cutoff of June 20, 2024, and median follow-up of 7.3 months (range, 1.0-18.1), the 6-month progression-free survival (PFS) rate was 46.7% (95% CI, 24.4%-66.2%). The median overall survival (OS) was 14.7 months (95% CI, 9.9-not evaluable). The objective response rate (ORR) among the overall population (n = 29) was 6.9% (95% CI, 0.8%-22.8%)."

P1/2 data • Ovarian Cancer

SYNTHESIS OF FLUORO AND NITRO PYRAZOLINE DERIVATIVES: ANTICANCER AND MOLECULAR DOCKING STUDIES. (PubMed, Chempluschem) - "In the PARP inhibition assay, 4c showed considerable inhibition compared to pamiparib. Molecular docking studies further support this by revealing a high binding affinity of 4c for the PARP enzyme. The results suggest that pyrazoline derivatives have the potential to be developed into effective anticancer agents."

Journal • Breast Cancer • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Study of Pamiparib in Newly Diagnosed and RGBM (clinicaltrials.gov) - P1 | N=45 | Active, not recruiting | Sponsor: Nader Sanai | Recruiting ➔ Active, not recruiting | N=30 ➔ 45 | Trial completion date: Jun 2025 ➔ Jul 2026 | Trial primary completion date: Jan 2025 ➔ Jul 2024

Enrollment change • Enrollment closed • Trial completion date • Trial primary completion date • Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Solid Tumor

BGB-290-104: A Study Assessing Pamiparib With Radiation and/or Temozolomide (TMZ) in Participants With Newly Diagnosed or Recurrent Glioblastoma (clinicaltrials.gov) - P1/2 | N=116 | Completed | Sponsor: BeiGene USA, Inc. | Phase classification: P1b/2 ➔ P1/2

Phase classification • Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Solid Tumor

A Phase II Single-Arm, Open-Label Trial of Pamiparib in Metastatic Castration-Resistant Prostate Cancer (mCRPC) Patients with Deleterious Germline or Somatic BRCA1/2 Alterations or Homologous Recombination Deficiency (HRD): Interim Analysis of Efficacy and Safety Results (EAU 2025) - No abstract available

Clinical • Metastases • P2 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • BRCA1 • BRCA2 • HRD

Clinical Application of PARP1 Inhibitors and Challenges in Cancer Therapy. (PubMed, Curr Cancer Drug Targets) - "This review has systematically summarized the latest clinical application of six authorized PARPi, including olaparib, rucaparib, niraparib, talazoparib, fuzuloparib and pamiparib, in monotherapy and combination therapies with chemotherapy, radiotherapy, and immunotherapy, in different kinds of cancer. Furthermore, probable challenges in PARPi application and drug resistance mechanisms have also been discussed. Despite these challenges, further development of new PARP1 inhibitors appears promising as a valuable approach to cancer treatment."

Journal • Oncology

Mechanistic Modeling of Spatial Heterogeneity of Drug Penetration and Exposure in the Human Central Nervous System and Brain Tumors. (PubMed, Clin Pharmacol Ther) - "The model was validated by comparisons of model predictions and clinically observed data of six drugs (abemaciclib, ribociclib, pamiparib, olaparib, temuterkib, and ceritinib) in glioblastoma patients. The 9-CNS model is a first-of-its kind, mechanism-based computational modeling platform that enables early reliable prediction of spatial CNS and tumor pharmacokinetics based on plasma concentration-time profiles. It provides a valuable tool to assist rational drug development and treatment for brain cancer."

Heterogeneity • Journal • Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Solid Tumor

BGB-290-103: Study to Assess Safety, Tolerability and Clinical Activity of BGB-290 in Combination With Temozolomide (TMZ) in Participants With Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - P1 | N=139 | Completed | Sponsor: BeiGene | Phase classification: P1b ➔ P1

Metastases • Phase classification • Breast Cancer • Esophageal Cancer • Gastric Cancer • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer • AR • BRCA • HRD

A phase II single-arm, open-label trial of pamiparib in metastatic castration-resistant prostate cancer (mCRPC) patients with deleterious germline or somatic BRCA1/2 alterations or homologous recombination deficiency (HRD): Interim analysis of efficacy and safety results (ESMO Asia 2024) - P2 | "ORR and PSA response rate was 20% and 100%, respectively. Conclusions The results suggest that pamiparib demonstrates significant antitumor activity as a monotherapy for mCRPC pts with deleterious germline or somatic BRCA1/2 alterations or HRD score 43."

Clinical • Metastases • P2 data • Breast Cancer • Genito-urinary Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Solid Tumor • BRCA • BRCA1 • BRCA2 • HRD