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DRUG CLASS:

β-catenin inhibitor

1d
NUP62 promotes breast cancer progression and inhibits ferroptosis by stabilizing NRF2 in a KEAP1-dependent way. (PubMed, iScience)
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.
Journal
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KEAP1 (Kelch Like ECH Associated Protein 1) • NUP62 (Nucleoporin 62)
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Halaven (eribulin mesylate)
5d
Safety and Antitumor Activity of Farletuzumab Ecteribulin in Patients With NSCLC: Phase I Expansion Results. (PubMed, JTO Clin Res Rep)
FZEC demonstrated modest antitumor activity, and observed AEs were generally manageable in patients with heavily pretreated NSCLC. NCT03386942.
P1 data • Journal
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FOLR1 ( Folate receptor alpha )
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FOLR1 expression
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Halaven (eribulin mesylate) • farletuzumab ecteribulin (MORAb-202)
9d
Role of the cross-regulation between Wnt pathway activation and androgen receptor signaling in prostate cancer treatment resistance. (PubMed, Cell Death Differ)
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.
Journal
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RNF43 (Ring Finger Protein 43) • ZNRF3 (Zinc And Ring Finger 3)
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foscenvivint (PRI724)
14d
New P2 trial
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 negative
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Focus V (anlotinib) • Halaven (eribulin mesylate)
26d
New P1/2 trial
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HER-2 positive • HER-2 amplification
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capecitabine • Halaven (eribulin mesylate) • Tukysa (tucatinib) • Ziihera (zanidatamab-hrii)
26d
CSF1R Inhibition with Chemotherapy Relieves Systemic Immune Suppression in Patients with Metastatic Triple-Negative Breast Cancer and Boosts anti-PD-1 Efficacy in Transgenic Mammary Tumors. (PubMed, Clin Cancer Res)
These clinical and preclinical findings provide rationale for therapies to increase therapeutic index of aPD-1 therapy by diminishing presence of T cell-suppressive myelomonocytic cells to improve outcomes for patients with refractory disease.
Journal • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
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Halaven (eribulin mesylate) • Turalio (pexidartinib)
1m
New trial • Real-world evidence
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 negative
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Halaven (eribulin mesylate)
1m
Enrollment closed
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gemcitabine • paclitaxel • docetaxel • Halaven (eribulin mesylate) • Trodelvy (sacituzumab govitecan-hziy)
1m
New P1/2 trial
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BRAF (B-raf proto-oncogene)
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MSI-H/dMMR • BRAF mutation • RAS wild-type
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tegavivint (BC2059)
1m
Targeting phosphodiesterase 10A disrupts MAPK signaling pathways in the tumor microenvironment to unleash antitumor immunity. (PubMed, bioRxiv)
Mechanistically, ADT-030 disrupts multiple components of the mitogen-activated protein kinase (MAPK) signaling network in both tumor cells and MDSCs, leading to induction of apoptosis in these populations. These findings highlight the multi-faceted impact of PDE10A inhibition as a therapeutic strategy that not only disrupts tumor-intrinsic oncogenic signaling to inhibit tumor progression but also reshapes the tumor immune microenvironment to unleash antitumor immunity.
Journal
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CD8 (cluster of differentiation 8) • BATF3 (Basic Leucine Zipper ATF-Like Transcription Factor 3)
1m
Enrollment closed • First-in-human
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HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
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HER-2 positive • HR positive • HER-2 negative • PIK3CA mutation • HR positive + HER-2 negative
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Halaven (eribulin mesylate) • izorlisib (MEN1611)
2ms
Study of E7386 in Participants With Selected Advanced Neoplasms (clinicaltrials.gov)
P1, N=60, Active, not recruiting, Eisai Inc. | Trial completion date: Mar 2026 --> Mar 2027 | Trial primary completion date: Mar 2026 --> Mar 2027
Trial completion date • Trial primary completion date
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CTNNB1 (Catenin (cadherin-associated protein), beta 1)
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E7386