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Ref Type Journal Article
PMID (41385966)
Authors Kondo S, Yamamoto N, Katsuya Y, Sato J, Mishima S, Kawazoe A, Oki E, Yamazaki K, Itoh S, Yokota T, Nagao S, Kimura T, Yamamuro S, Hayata N, Tamai T, Shitara K
Title E7386 in patients with advanced solid tumors: results from the dose-escalation part and an expansion part of a phase I study.
Journal Vol Issue Date Pages Journal Short Title
ESMO open 10 12 2025 Dec 105893 ESMO Open
URL
Abstract Text E7386 is an orally active inhibitor reported to block the CBP/β-catenin interaction. We present data from the dose-escalation and expansion part 1 of Study 103 (phase I) of E7386 in patients with advanced, unresectable, or recurrent (A/U/R) solid tumors.This open-label study was conducted in Japan. In dose-escalation, eligible patients aged ≥20 years were diagnosed with A/U/R solid tumors with no alternative standard/effective therapies. In the expansion part, eligible patients were diagnosed with A/U/R colorectal cancer (two or more prior systemic anticancer therapies) or other gastrointestinal tumors (one or more prior systemic anticancer therapy). The primary objective was assessment of safety and tolerability. Secondary objectives were assessment of pharmacokinetic (PK) and antitumor activity. Efficacy was assessed by investigators using RECIST v1.1.Fifty-five enrolled patients (dose-escalation: n = 36; expansion: n = 19) received one or more dose of E7386. The most frequent tumor was colorectal cancer (dose-escalation: 55.6%; expansion: 84.2%). Over half of those enrolled received more than three prior systemic anticancer medications. In dose-escalation, dose-limiting toxicities (grade 3 decreased appetite) occurred in two patients [160 mg twice daily (b.i.d.) cohort]; the recommended dose was 120 mg b.i.d. Most patients (dose-escalation/expansion) experienced treatment-emergent adverse events (TEAEs; 97.2%/94.7%): the most frequent TEAEs were nausea (83.3%/84.2%) and vomiting (61.1%/73.7%). These were primarily low-grade in severity and well managed with antiemetics in patients receiving up to 120 mg b.i.d. No patients died due to TEAEs. In dose-escalation, two patients achieved partial response (PR): one with small bowel carcinoma (APC/KRAS/TP53 mutations); one with a desmoid tumor (APC mutation). No PRs were observed in the expansion part. PK exposure increased with doses (range: 10-160 mg b.i.d.) following single and repeat-dose administrations, although large inter-subject variability was observed.In heavily pretreated patients with advanced solid tumors, E7386 demonstrated a manageable safety profile and a dose-dependent PK profile. PRs were noted in patients with small bowel carcinoma or desmoid tumor.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
APC inact mut desmoid tumor predicted - sensitive E7386 Case Reports/Case Series Actionable In a Phase I trial, E7386 treatment demonstrated manageable safety and resulted in 2 partial responses in 55 patients with advanced solid tumors, including a partial response with treatment lasting 7.5 months in a patient with small bowel carcinoma and a partial response with treatment lasting 3.5 years in a patient with desmoid tumor (PMID: 41385966; NCT03833700). 41385966
APC inact mut small intestine carcinoma predicted - sensitive E7386 Case Reports/Case Series Actionable In a Phase I trial, E7386 treatment demonstrated manageable safety and resulted in 2 partial responses in 55 patients with advanced solid tumors, including a partial response with treatment lasting 7.5 months in a patient with small bowel carcinoma and a partial response with treatment lasting 3.5 years in a patient with desmoid tumor (PMID: 41385966; NCT03833700). 41385966