DO-5 / DeuterOncology - LARVOL DELTA

Preliminary Safety and PK of the MET-TKI Do-2 in Advanced Solid Tumors With MET Aberrations: Phase I Study (IASLC-WCLC 2025) - "The primary endpoint was safety and tolerability; secondary objectives included PK of DO-2, the primary metabolites DO-5 and M3 and anti-tumor activity according to RECIST 1.1. The dose limiting toxicity (DLT) observation period was 4 weeks. Response assessment was performed every 8 weeks."

Clinical • Metastases • P1 data • Oncology • Solid Tumor

A High-Fat Meal Optimizes the Pharmacokinetic Profile of DO-2, a Novel MET-Kinase Inhibitor for NSCLC (IASLC-WCLC 2025) - P1 | "DO-2 is a deuterated version of JNJ-38877605, redesigned to reduce toxic metabolite (M5) formation via AOX-1...Total exposures (AUC 0-24h ) to DO-2, DO-5 and M3 are similar with and without food. Since an 8-10 hour ToT is ideal for efficacy and toxicity, food optimizes the pharmacokinetic profile of DO-2, which is further evaluated in the extension phase of the phase 1 study in patients (NCT05752552). Possibly, EGCG could reduce M3 formation and should be studied further."

PK/PD data • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • MET

Preliminary Safety and Pharmacokinetics of the MET-TKI DO-2 in Patients with Advanced Solid Tumors Harboring MET Aberrations: A Phase I Study (EORTC-NCI-AACR 2024) - "Plasma levels of the parent compound DO-2, an active metabolite DO-5 and an inactive metabolite M3 show linear dose-exposure relationships (Cmax and AUC0-24). Encouraging signs of clinical benefit and prolonged disease control observed with no evidence of peripheral edema or liver enzyme elevations. BID dosing is currently being explored further."

Clinical • Metastases • P1 data • PK/PD data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • MET

Quantification and clinical validation of the selective MET kinase inhibitor DO-2 and its metabolites DO-5 and M3 in human plasma. (PubMed, J Pharm Biomed Anal) - "All values for accuracy, within-run and between-run precisions met the criteria set by the Food and Drug Administration. The method was effectively employed in the analysis of samples obtained from a clinical trial."

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