Using pyrimethamine to treat advanced head and neck cancer

Early Phase I Window of Opportunity Biomarker and Safety Trial to Test Pyrimethamine as an Inhibitor of NRF2 in HPV-unrelated, Locally Advanced Head and Neck Squamous Cell Carcinoma

Early Phase 1 Interventional Washington University School of Medicine · NCT05678348

This study is testing if the drug pyrimethamine, usually used for infections, can help treat advanced head and neck cancer by slowing down tumor growth.

Quick facts

PhaseEarly Phase 1
Study typeInterventional
Enrollment22 (estimated)
Ages18 Years and up
SexAll
SponsorWashington University School of Medicine Academic / other
Drugs / interventionsradiation
Locations1 site (Saint Louis, Missouri)
Trial IDNCT05678348 on ClinicalTrials.gov

What this trial studies

This clinical trial investigates the use of pyrimethamine, a drug traditionally used for treating infections, as a potential treatment for locally advanced head and neck squamous cell carcinoma (HNSCC) that is unrelated to HPV. The study focuses on the drug's ability to inhibit the NRF2 pathway, which is implicated in tumor progression and resistance to therapy. Participants will be evaluated for the drug's efficacy in reducing tumor activity by measuring its effects on dihydrofolate reductase (DHFR) and NRF2 pathway activity. The trial aims to provide insights into the antitumor activity of pyrimethamine in human tumors, a previously unexplored area.

Who should consider this trial

Good fit: Ideal candidates are adults aged 18 and older with locally advanced, HPV-unrelated head and neck squamous cell carcinoma.

Not a fit: Patients with early-stage head and neck cancer or those with HPV-related tumors may not benefit from this study.

Why it matters

Potential benefit: If successful, this treatment could offer a new therapeutic option for patients with advanced head and neck cancer.

How similar studies have performed: While pyrimethamine has shown promise in preclinical models, its application in human tumors is novel and has not been previously tested.

Eligibility criteria

Show full inclusion / exclusion criteria
Inclusion Criteria:

* Histologically or cytologically confirmed, locally advanced (Stage III-IV) head and neck squamous cell carcinoma (HNSCC) undergoing surgical-based treatment with curative intent that is HPV-unrelated disease, defined as SCC of the oral cavity, larynx, or hypopharynx, p16 negative SCC of the oropharynx.
* At least 18 years of age.
* ECOG performance status ≤ 1
* Normal bone marrow and organ function as defined below:

  * Leukocytes ≥ 3.0 K/cumm
  * Absolute neutrophil count ≥ 1.5 K/cumm
  * Platelets ≥ 100 K/cumm
  * Total bilirubin ≤ 1.5 x IULN
  * AST(SGOT)/ALT(SGPT) ≤ 3.0 x IULN
  * Creatinine clearance \> 50 mL/min by Cockcroft-Gault
* Able to swallow study drug
* The effects of pyrimethamine on the developing human fetus are unknown. For this reason and because it is in Pregnancy Category C, women of childbearing potential and men must agree to use adequate contraception (hormonal or barrier method of birth control, abstinence) prior to study entry and for the duration of study participation. Should a woman become pregnant or suspect she is pregnant while participating in this study, she must inform her treating physician immediately.
* Ability to understand and willingness to sign an IRB approved written informed consent document.
* Patient must be able to undergo a research biopsy prior to starting treatment, or have previously banked baseline tumor biopsy of at least 20 mg of frozen tissue collected under Tissue Acquisition Protocol (IRB 201102323).

Exclusion Criteria:

* Prior therapy for this cancer.
* A history of other malignancy with the exception of malignancies for which all treatment was completed at least 2 years before registration and the patient has no evidence of disease.
* Prior treatment with pyrimethamine in the year prior to HNSCC diagnosis.
* Currently receiving any other investigational agents.
* A history of allergic reactions attributed to compounds of similar chemical or biologic composition to pyrimethamine or other agents used in the study.
* Uncontrolled intercurrent illness including, but not limited to, ongoing or active infection, current use of systemic immunosuppressive medications, symptomatic congestive heart failure, unstable angina pectoris, or cardiac arrhythmia.
* Documented megaloblastic anemia due to folate deficiency.
* Treatment with anticoagulant or antiplatelet therapy in the year prior to HNSCC diagnosis.
* Pregnant and/or breastfeeding. Women of childbearing potential must have a negative pregnancy test within 7 days of Day 1.
* Patients with HIV are eligible unless their CD4+ T-cell counts are \< 350 cells/mcL or they have a history of AIDS-defining opportunistic infection within the 12 months prior to registration. Concurrent treatment with effective ART according to DHHS treatment guidelines is recommended.
* Active alcohol abuse in the opinion of the treating physician.
* Currently taking phenytoin

Where this trial is running

Saint Louis, Missouri

Study contacts

How to participate

  1. Review the eligibility criteria above with your treating physician.
  2. Visit the official trial page on ClinicalTrials.gov for the most current contact information and recruitment status.
  3. Contact the listed study coordinator or principal investigator to request pre-screening. Pre-screening is free and never obligates you to enroll.
Conditions Head and Neck CancerCancer of the Head and Neckhead and neck cancersquamous cell carcinomaNRF2pyrimethaminetreatment resistance
Last reviewed 2026-06-13 by the Find a Trial editorial team. Information on this page is for educational purposes and is not medical advice. Always consult qualified healthcare professionals about clinical trial participation.