thioguanine

After 75 mg/m2/day mercaptopurine, myelosuppression necessitated a three-week delay prior to the next phase of therapy. With 60 mg/m2/day thioguanine in a subsequent phase of therapy, she was admitted twice for fever and neutropenia...In a larger cohort sequenced for suspicion of rare genetic disease, the frequency of NUDT15*6 was 0.15% among 1011 unrelated individuals. This brief report supports the recent update that patients with the NUDT15*1/*6 genotype should be classified as intermediate metabolizers.

P2, N=90, Not yet recruiting, SWOG Cancer Research Network

The TPMT and NUDT15 genes influence the side effects of 6-MP medications. Patients who have variations in both genes are at a higher risk of experiencing toxicity. High levels of 6-TGN are associated with TPMT variants, whereas low levels are linked to NUDT15 variants. This could facilitate more precise monitoring of toxicity.

P3, N=5949, Completed, National Cancer Institute (NCI) | Trial completion date: Oct 2026 --> Mar 2026 | Active, not recruiting --> Completed

P3, N=9350, Completed, Children's Oncology Group | Active, not recruiting --> Completed

P3, N=683, Recruiting, University Hospital Muenster | Trial completion date: Nov 2027 --> Apr 2030 | Trial primary completion date: Nov 2027 --> Apr 2030

P2, N=318, Completed, Alliance for Clinical Trials in Oncology | Active, not recruiting --> Completed

P2/3, N=25, Recruiting, Medical University Of Lodz | Not yet recruiting --> Recruiting

P3, N=9350, Active, not recruiting, Children's Oncology Group | Trial completion date: Mar 2028 --> Mar 2026

P2, N=222, Recruiting, National Cancer Institute (NCI) | Phase classification: P3 --> P2

P2, N=171, Completed, Incyte Corporation | Active, not recruiting --> Completed

Pharmacological inhibitors of specific USPs, such as pimozide, trifluoperazine, rottlerin, 6-thioguanine, and costunolide, are highlighted for their potential to inhibit proliferation, metastasis, induce apoptosis, and circumvent therapy resistance across breast cancer subtypes (triple-negative and HER-2 positive). The review highlights the complex and often contradictory roles of USPs in breast cancer and points to the immense promise of targeting these enzymes to develop new and efficacious anticancer therapies.