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DRUG CLASS:

β-catenin inhibitor

2d
Therapeutic Strategies to Overcome Payload Resistance of Trastuzumab Deruxtecan in HER2-Positive Cancers. (PubMed, Cancer Sci)
Moreover, BB-1701, a novel HER2-ADC containing eribulin as a payload, to which N87 AR cells are sensitive, exhibited antitumor effects in N87 AR cells in vitro and in vivo. These findings indicate that ABC transporter-mediated drug efflux is an important mechanism underlying T-DXd resistance in HER2-positive gastric and lung cancer models. Furthermore, our study suggests that both targeting drug efflux pathways and utilizing alternative payloads may be effective strategies for overcoming T-DXd resistance in HER2-positive gastric and lung cancers.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
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HER-2 positive • HER-2 amplification • HER-2 expression
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Enhertu (fam-trastuzumab deruxtecan-nxki) • Halaven (eribulin mesylate) • BB-1701
8d
DPTX3186 in Wnt Pathway Activated Solid Tumors (clinicaltrials.gov)
P1, N=40, Recruiting, Dewpoint Therapeutics | Not yet recruiting --> Recruiting
Enrollment open • First-in-human
8d
New P2 trial
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HR positive • HR positive + HER-2 positive
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Nerlynx (neratinib) • Enhertu (fam-trastuzumab deruxtecan-nxki) • fulvestrant • Halaven (eribulin mesylate)
11d
Tegavivint for the Treatment of Relapsed or Refractory Leukemia (clinicaltrials.gov)
P1, N=9, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Dec 2025 --> Feb 2027 | Trial primary completion date: Dec 2025 --> Feb 2027
Trial completion date • Trial primary completion date
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decitabine • tegavivint (BC2059)
20d
DPTX3186 in Wnt Pathway Activated Solid Tumors (clinicaltrials.gov)
P1, N=40, Not yet recruiting, Dewpoint Therapeutics
New P1 trial
28d
Eribulin in Angiosarcoma and Epithelioid Hemangioendothelioma (EHE) (clinicaltrials.gov)
P2, N=13, Active, not recruiting, Massachusetts General Hospital | Trial completion date: Sep 2025 --> Feb 2026
Trial completion date
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Halaven (eribulin mesylate)
28d
Clinical trial of safety and antitumor activity of farletuzumab ecteribulin in patients with platinum-resistant ovarian cancer: Phase I expansion results. (PubMed, Int J Gynaecol Obstet)
FZEC showed promising antitumor activity, and the observed adverse events were generally manageable, with the exception of ILD, in patients with PROC.
P1 data • Journal • Platinum resistant
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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)
1m
Tegavivint With Gemcitabine in Patients With Relapsed or Refractory Osteosarcoma (clinicaltrials.gov)
P1, N=24, Not yet recruiting, Emory University | Initiation date: Oct 2025 --> Jan 2026
Trial initiation date
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gemcitabine • tegavivint (BC2059)
1m
Atezolizumab, Cobimetinib, and Eribulin in Treating Patients With Chemotherapy Resistant Metastatic Inflammatory Breast Cancer (clinicaltrials.gov)
P2, N=37, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Dec 2025 --> Dec 2027 | Trial primary completion date: Dec 2025 --> Dec 2027
Trial completion date • Trial primary completion date
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PD-L1 (Programmed death ligand 1) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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HER-2 positive
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Tecentriq (atezolizumab) • Cotellic (cobimetinib) • Halaven (eribulin mesylate)
1m
E7386 in patients with advanced solid tumors: results from the dose-escalation part and an expansion part of a phase I study. (PubMed, ESMO Open)
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.
P1 data • Journal
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KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • APC (APC Regulator Of WNT Signaling Pathway)
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TP53 mutation • KRAS mutation
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E7386
1m
Adaptive Chemotherapy for the Treatment of Advanced Breast Cancer (clinicaltrials.gov)
P3, N=192, Recruiting, Sun Yat-sen University | Enrolling by invitation --> Recruiting
Enrollment status
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gemcitabine • Halaven (eribulin mesylate) • vinorelbine tartrate • utidelone IV (UTD1)
1m
OSU-20298: Osimertinib and Tegavivint as First-Line Therapy for the Treatment of Metastatic EGFR-Mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
P1, N=24, Recruiting, Ohio State University Comprehensive Cancer Center | Trial primary completion date: Jul 2025 --> Jul 2026
Trial primary completion date
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR L861Q • EGFR G719X • EGFR S768I
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Tagrisso (osimertinib) • tegavivint (BC2059)