P1/2, N=120, Recruiting, Pathos AI, Inc. | N=252 --> 120

E7386 demonstrated a manageable safety profile, a dose-dependent pharmacokinetic profile, and some disease stabilisation in heavily pretreated patients with advanced solid tumours.

CZL-149 displays favorable drug-like properties and metabolic profile, achieving 107% oral bioavailability in mice. Importantly, CZL-149 outperformed NEO2734 in both antitumor efficacy (TGI = 78%) and safety in vivo, highlighting its potential as an advanced preclinical candidate worthy of further development.

We find that use of the dual histone acetyltransferase p300/CBP bromodomain inhibitor CCS1477 (inobrodib), together with venetoclax and gilteritinib, virtually eliminates leukemia stem cells in an aggressive preclinical model of DNMT3A/FLT3-mutant AML by impairing pro-oncogenic survival and proliferation factors to effectively block leukemogenesis. This work identifies potential clinical utility of a targeted, triplet combination therapy for treatment of AML.

These results suggest that [14C]E7386-related material is predominantly excreted in feces after oral administration. Overall, IV administration and oral administration of a single E7386 dose was tolerable in healthy participants, and adverse events were manageable.

P3, N=246, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University | Active, not recruiting --> Recruiting | Trial completion date: Mar 2031 --> Jun 2029 | Trial primary completion date: Sep 2030 --> Dec 2028

P2, N=76, Recruiting, Fifth Affiliated Hospital, Sun Yat-Sen University; Fifth Affiliated Hospital, Sun Yat-Sen University

In vivo, eribulin or NUP62 silencing significantly suppressed tumor growth in xenograft models. Our findings establish the NUP62-KEAP1-NRF2 axis as a master regulator of ferroptosis in BC, positioning eribulin as a promising therapeutic agent for NUP62-high tumors.

FZEC demonstrated modest antitumor activity, and observed AEs were generally manageable in patients with heavily pretreated NSCLC. NCT03386942.

P1, N=50, Recruiting, Aurigene Discovery Technologies Limited | Trial primary completion date: Jun 2025 --> Jan 2027

P1, N=50, Active, not recruiting, TOLREMO therapeutics AG | Recruiting --> Active, not recruiting

Targeting β-catenin interactions with co-activators p300/CBP using selective inhibitors (IQ-1 and ICG-001) effectively mitigated Wnt-driven ARSI resistance, restoring sensitivity to therapy in preclinical models...The identified Wnt signature holds potential as a biomarker for predicting and monitoring therapeutic outcomes. Concurrent targeting of AR and Wnt signaling represents a promising strategy to overcome treatment resistance, particularly in patients with Wnt-activating mutations.