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DRUG CLASS:

CBP 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
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)
26d
Discovery of CZL-077 as a potent, selective, and orally active p300/CBP bromodomain inhibitor with improved in vivo antitumor efficacy. (PubMed, Eur J Med Chem)
Compared to CCS1477, it shows comparable in vivo efficacy in the OPM-2 xenograft model and demonstrates more potent antitumor activity in the 22RV1 xenograft model, with tumor growth inhibition values of 56.2% and 72.8%, respectively. Overall, CZL-077 is a promising candidate for the treatment of human cancer as a p300/CBP BRD inhibitor.
Preclinical • Journal
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CREBBP (CREB binding protein)
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inobrodib (CCS1477)
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
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)
2ms
LEADER: Lenvatinib and Eribulin in Advanced Soft Tissue Sarcoma (clinicaltrials.gov)
P1/2, N=30, Completed, National Taiwan University Hospital | Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> Oct 2025
Trial completion • Trial completion date
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Lenvima (lenvatinib) • Halaven (eribulin mesylate)
2ms
A Phase II Clinical Study of Multimodal Ablation Combined With Systemic Drug Therapy for Advanced Solid Tumors. (clinicaltrials.gov)
P2, N=95, Recruiting, Fudan University | Not yet recruiting --> Recruiting | Phase classification: PN/A --> P2 | N=66 --> 95 | Trial completion date: May 2028 --> Dec 2028 | Initiation date: Apr 2025 --> Nov 2025 | Trial primary completion date: Jul 2026 --> Dec 2027
Enrollment open • Phase classification • Enrollment change • Trial completion date • Trial initiation date • Trial primary completion date
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Halaven (eribulin mesylate)
2ms
ESPERO: Eribulin With or Without Trastuzumab-biosimilar in Patients With HER2-overexpressed Recurrent or Stage IV Breast Cancer (clinicaltrials.gov)
P2, N=180, Recruiting, Seoul National University Hospital | Trial completion date: Dec 2026 --> Jun 2028 | Trial primary completion date: Dec 2026 --> Jun 2028
Trial completion date • Trial primary completion date
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HER-2 positive • HER-2 expression
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Halaven (eribulin mesylate) • Ontruzant (trastuzumab-dttb)
2ms
Predicting the Efficacy of Eribulin in Metastatic Breast Cancer by Assessing E-Cadherin and Vimentin Expression. (PubMed, Acta Histochem Cytochem)
Altered E-cadherin and/or vimentin expression was more frequently observed in responders (p = 0.013) and associated with longer progression-free survival (p = 0.048). These results suggest that eribulin efficacy may be predicted by altered E-cadherin and vimentin expression before treatment.
Journal
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CDH1 (Cadherin 1) • VIM (Vimentin)
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Halaven (eribulin mesylate)