BibTex format
@article{Evans:2026:10.1038/s41416-026-03488-w,
author = {Evans, TRJ and Cook, N and El-Khoueiry, A and Pinato, DJ and Tran, NH and Hsiehchen, D and Mena, E and Meyer, T and Wu, J and Pathak, SM and Paoletti, C and Dutta, L and Okpara, CE and Lopez, JS},
doi = {10.1038/s41416-026-03488-w},
journal = {Br J Cancer},
pages = {736--746},
title = {A first-in-human, open-label multicentre Phase 1 study of the orally administered E7386 in patients with selected advanced neoplasms.},
url = {http://dx.doi.org/10.1038/s41416-026-03488-w},
volume = {135},
year = {2026}
}
RIS format (EndNote, RefMan)
TY - JOUR
AB - BACKGROUND: We present data from the Phase 1 open-label Study 101 of E7386, an oral protein-protein interaction inhibitor reported to block the CBP/β-catenin interaction, in patients with solid tumours. METHODS: Eligible patients (across the UK and US) aged ≥18 years had advanced/recurrent solid tumours (dose-escalation) or CTNNB1-mutated hepatocellular carcinoma (dose-expansion). Primary objectives were to assess safety/tolerability and determine the recommended Phase 2 dose (RP2D) of E7386. RESULTS: Thirty-eight patients received study drug (dose-escalation: n = 32; expansion: n = 6; dose-range: 5-120 mg twice daily [BID]); 60.5% received ≥3 prior anticancer medications. Dose-limiting toxicities (grade-2 lethargy and grade-2 decreased appetite) occurred in 1 patient (20 mg BID cohort). The RP2D was determined as 120 mg BID. Most (94.7%) patients experienced treatment-related adverse events (TRAEs), most frequently nausea (65.8%) and vomiting (60.5%), which were primarily grade 1/2 and well-managed with antiemetics. No grade 4/5 TRAEs were noted. Pharmacokinetic exposure increased with increasing dose, although large intersubject variability was observed. No objective responses were noted; stable disease (SD) was observed in 36.8% of patients, including SD ≥ 23 weeks in 18.8% of patients (dose-escalation). CONCLUSIONS: E7386 demonstrated a manageable safety profile, a dose-dependent pharmacokinetic profile, and some disease stabilisation in heavily pretreated patients with advanced solid tumours. TRIAL REGISTRATION: NCT03264664 https://clinicaltrials.gov/study/NCT03264664 .
AU - Evans,TRJ
AU - Cook,N
AU - El-Khoueiry,A
AU - Pinato,DJ
AU - Tran,NH
AU - Hsiehchen,D
AU - Mena,E
AU - Meyer,T
AU - Wu,J
AU - Pathak,SM
AU - Paoletti,C
AU - Dutta,L
AU - Okpara,CE
AU - Lopez,JS
DO - 10.1038/s41416-026-03488-w
EP - 746
PY - 2026///
SP - 736
TI - A first-in-human, open-label multicentre Phase 1 study of the orally administered E7386 in patients with selected advanced neoplasms.
T2 - Br J Cancer
UR - http://dx.doi.org/10.1038/s41416-026-03488-w
UR - https://www.ncbi.nlm.nih.gov/pubmed/42243349
VL - 135
ER -