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DRUG CLASS:

CBP inhibitor

5d
Enrollment open
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pomalidomide • inobrodib (CCS1477)
5d
Discovery of Novel CBP/p300 and BRD4 Dual-Target PROTACs with Potent Antitumor Activity in Prostate Cancer. (PubMed, J Med Chem)
Both compounds displayed potent antiproliferative activity across multiple cancer cell lines, with higher potency than NEO2734, paclitaxel (PTX), and ARV-771. In a PC-3 xenograft mouse model, compound 29c achieved dose-dependent tumor growth inhibition (TGI) of up to 81.5% at a low dose of 0.2 mg/kg, administered every other day, significantly surpassing the efficacy of NEO2734 and PTX at higher doses. Together, 29c, a highly efficient CBP/p300 and BRD4 dual-target degrader, demonstrates significant therapeutic potential in prostate cancer and warrants further development.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BRD4 (Bromodomain Containing 4)
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paclitaxel • EP31670
12d
Identifying immune-related predictive factors for post-eribulin therapy in patients with HER2-negative advanced breast cancer- a multicenter retrospective study. (PubMed, Int J Clin Oncol)
An ALC ≥ 1000/μL at ERI completion was associated with an improved post-ERI OS (OS2). It is suggested that not only the factors at the initiation of ERI, but also the immunological status at the end of ERI, may have prognostic value after ERI.
Retrospective data • Journal
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
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ER positive • HER-2 negative • HER-2 negative + ER positive
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Halaven (eribulin mesylate)
12d
New trial
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Lenvima (lenvatinib) • irinotecan • Halaven (eribulin mesylate) • Puyouheng (pucotenlimab)
12d
New P3 trial
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Focus V (anlotinib) • doxorubicin hydrochloride • Halaven (eribulin mesylate)
12d
A Single-Arm, Multicenter Clinical Study of Eribulin Mesylate in Combination with Ivonescimab as First-Line Treatment for Unresectable Locally Advanced or Metastatic Triple-Negative Breast Cancer (ChiCTR2600117652)
P2, N=50, Not yet recruiting, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University; Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University
New P2 trial
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HER-2 (Human epidermal growth factor receptor 2) • PGR (Progesterone receptor)
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HER-2 negative • ER negative
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Halaven (eribulin mesylate) • Yidafan (ivonescimab)
12d
New P2 trial
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Lenvima (lenvatinib) • irinotecan • Halaven (eribulin mesylate) • Puyouheng (pucotenlimab)
21d
A Japanese Multicenter Database Study of Retroperitoneal Sarcoma: Outcomes of Patients Receiving Eribulin Therapy. (PubMed, Asia Pac J Clin Oncol)
We separately described outcomes and treatment patterns of patients with resectable and unresectable RPS. Our findings suggest that eribulin should be considered a treatment option for unresectable RPS in clinical practice.
Journal
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CRP (C-reactive protein)
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Halaven (eribulin mesylate)
25d
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
1m
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)
2ms
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)
2ms
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)