Phase I/II and window-of-opportunity study of pamiparib and metronomic temozolomide for recurrent isocitrate dehydrogenase mutant gliomas

Document Type

Article

Publication Date

2-1-2026

Publication Title

Neuro Oncol

Keywords

Humans, Temozolomide, Female, Glioma, Isocitrate Dehydrogenase, Middle Aged, Male, Brain Neoplasms, Adult, Neoplasm Recurrence, Local, Mutation, Antineoplastic Combined Chemotherapy Protocols, Aged, Maximum Tolerated Dose, Administration, Metronomic, Prognosis, Follow-Up Studies, Young Adult, Survival Rate, Antineoplastic Agents, Alkylating

Abstract

BACKGROUND: Preclinical studies demonstrate activity of poly(adenosine 5'-diphosphate-ribose) polymerase (PARP) inhibitors in isocitrate dehydrogenase (IDH) mutant gliomas. We investigated safety, tolerability, pharmacokinetics, and efficacy of the PARP inhibitor pamiparib in conjunction with metronomic low-dose temozolomide in patients with recurrent IDH mutant (IDHmt) gliomas in a multicenter Phase I/II/window of opportunity study.

METHODS: Patients received pamiparib in conjunction with daily temozolomide. Following Phase I determination of maximum tolerated dose (MTD), we enrolled 2 patient cohorts (Arm A, multiple prior chemotherapy regimens; Arm B, single prior regimen) in a 2-stage design. Exploratory cohorts examined grade 4 IDHmt patients and intratumoral pharmacokinetics of pamiparib. The primary endpoint was objective radiographic response (ORR) by RANO criteria.

RESULTS: Sixty-six subjects were enrolled. We established pamiparib 60 mg twice daily with temozolomide 20 mg daily as the phase II dose. In non-enhancing and enhancing tumor, pamiparib exhibited an unbound tumor/plasma ratio of 0.92 and 0.98, respectively. 0/15 Arm A and 1/24 Arm B patients achieved a centrally confirmed partial response. Median progression-free survival for Arm A was 5.9 months (95% CI, 1.2-14.8 months), and for Arm B was 9.7 months (95% CI, 5.7-21.7 months). Grade 3+ anemia and neutropenia affected 24% and 33% of patients, respectively. Twenty-two of 66 patients (33.3%) discontinued study treatment for reasons other than tumor progression.

CONCLUSIONS: Pamiparib appeared to achieve sufficient pharmacologically active concentrations in both enhancing and non-enhancing tumors. While some patients achieved prolonged progression-free survival, combination with temozolomide did not produce a meaningful ORR in IDHmt recurrent gliomas. Cumulative hematologic toxicity was substantial and impacted long-term tolerability.

Medical Subject Headings

Humans; Temozolomide; Female; Glioma; Isocitrate Dehydrogenase; Middle Aged; Male; Brain Neoplasms; Adult; Neoplasm Recurrence, Local; Mutation; Antineoplastic Combined Chemotherapy Protocols; Aged; Maximum Tolerated Dose; Administration, Metronomic; Prognosis; Follow-Up Studies; Young Adult; Survival Rate; Antineoplastic Agents, Alkylating

PubMed ID

41099363

ePublication

ePub ahead of print

Volume

28

Issue

2

First Page

485

Last Page

494

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