Phase 1 Study of Safety and PK With A Combination of Omeprazole and Trimetazidine for Fatty Acid Oxidation Inhibition in Patients With Advanced Solid Tumors.
Wonyoung Choi, Jung W Chun, Sung H Sim et al.
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In 30 seconds
This Phase I, open-label, 3 + 3 dose-escalation study assessed safety, tolerability, pharmacokinetics, and preliminary antitumor activity of once-daily oral omeprazole plus trimetazidine, two fatty acid oxidation inhibitors, in 12 patients with advanced solid tumors. The maximum tolerated dose was not reached, and the recommended Phase 2 dose was 120 mg once daily for each agent. Treatment was generally well tolerated; stable disease was the best response in five patients, for a disease control rate of 41.7%.
Key findings
- The maximum tolerated dose was not reached; the recommended Phase 2 dose was 120 mg once daily for each agent.
- Most adverse events were Grade 1-2; flu-like symptoms occurred in 25.0%, and constipation, nausea, and dizziness each occurred in 16.7%.
- Stable disease was the best response in five patients (disease control rate 41.7%).
- Median progression-free survival was 1.66 months (95% CI, 1.18-3.55); median overall survival was 9.13 months (95% CI, 3.29-not reached).
Why it matters
The study provides early clinical evidence that two oral agents targeting fatty acid oxidation can be administered together in patients with advanced solid tumors, with pharmacokinetic findings differing between the drugs. The observed disease stabilization offers a preliminary signal for further investigation, but the small Phase I study is not designed to establish antitumor efficacy.
What to keep in mind
Only 12 patients were enrolled in this early-phase dose-escalation study; antitumor activity was preliminary, and the abstract reports no comparator group.