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DRUG CLASS:

CBP inhibitor

4d
New P2 trial
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor)
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HER-2 amplification • HER-2 negative • PIK3CA mutation • HER-2 negative + HR negative
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Halaven (eribulin mesylate) • Itovebi (inavolisib)
5d
Efficacy and safety of eribulin plus gemcitabine as second-line treatment for recurrent HER2-negative breast cancer: a phase II, single-arm, open-label trial. (PubMed, Commun Med (Lond))
Eribulin plus gemcitabine is effective and well-tolerated in patients with HER2-negative metastatic breast cancer needing second-line or later treatment, providing a valuable treatment option.
P2 data • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
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gemcitabine • Halaven (eribulin mesylate)
6d
Enrollment change
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Tagrisso (osimertinib) • docetaxel • Krazati (adagrasib)
7d
E7386-J081-102: A Study of E7386 in Combination With Other Anticancer Drug(s) in Participants With Solid Tumor (clinicaltrials.gov)
P1/2, N=301, Active, not recruiting, Eisai Inc. | Recruiting --> Active, not recruiting | Trial completion date: Aug 2027 --> Mar 2027 | Trial primary completion date: Aug 2027 --> Mar 2027
Enrollment closed • Trial completion date • Trial primary completion date
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EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability)
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BRAF V600E • MSI-H/dMMR • BRAF V600 • KRAS wild-type • NRAS wild-type
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paclitaxel • Lenvima (lenvatinib) • doxorubicin hydrochloride • E7386
8d
A Study of E7386 in Participants With Advanced Solid Tumor Including Colorectal Cancer (CRC) (clinicaltrials.gov)
P1, N=70, Active, not recruiting, Eisai Co., Ltd. | Trial completion date: Jan 2026 --> Mar 2027 | Trial primary completion date: Jan 2026 --> Mar 2027
Trial completion date • Trial primary completion date
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RNF43 (Ring Finger Protein 43) • APC (APC Regulator Of WNT Signaling Pathway) • AXIN1 (Axin 1) • ZNRF3 (Zinc And Ring Finger 3)
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E7386
8d
Enhanced Antitumor Activity and Induction of Immunogenic Cell Death in NUT Carcinoma Cells by Combining Oncolytic Viruses with the Dual Inhibitor NEO2734. (PubMed, Viruses)
To investigate multimodal therapeutic approaches that combine epigenetic modulation with immunogenic and cytotoxic effects of oncolytic viruses (OVs), we evaluated two recombinant OVs, including the herpes simplex virus talimogene laherparepvec (T-VEC) and a measles vaccine virus (MeV-GFP), in combination with NEO2734 in four distinct NC cell lines. Evaluation of immunogenic cell death (ICD) markers displayed elevated ATP and HMGB1 levels and increased surface calreticulin with T-VEC and NEO2734 combinations. Overall, these findings indicate that combining OVs with BET/p300 inhibitors elicits potent antitumor responses, supports synergistic interactions and immunogenicity, and warrants further investigation in multimodal therapeutic strategies for NC.
Journal • IO biomarker
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HMGB1 (High Mobility Group Box 1) • BRD4 (Bromodomain Containing 4) • CALR (Calreticulin) • NUTM1 (NUT Midline Carcinoma Family Member 1)
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Imlygic (talimogene laherparepvec) • EP31670
8d
Effects of Eribulin on Epithelial-Mesenchymal Plasticity in Patient-Derived Breast Cancer Cultures and Excised Tissues. (PubMed, Cancers (Basel))
Our data highlight the presence of contextual parameters which govern the degree of EMT regulation by eribulin.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • CDH1 (Cadherin 1)
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doxorubicin hydrochloride • Halaven (eribulin mesylate)
10d
BCTOP-T-M01: Precise Treatment for BLIS Subtype of TNBC in the First-line Treatment of Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
P3, N=134, Recruiting, Fudan University | N=192 --> 134 | Trial completion date: Feb 2026 --> Nov 2026 | Trial primary completion date: Aug 2025 --> May 2026
Enrollment change • Trial completion date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 expression
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Avastin (bevacizumab) • carboplatin • capecitabine • albumin-bound paclitaxel • Halaven (eribulin mesylate)
11d
ATP-binding cassette subfamily A member 5 suppresses pancreatic ductal adenocarcinoma progression and chemoresistance by promoting β-catenin ubiquitin-dependent degradation. (PubMed, Drug Resist Updat)
Collectively, our study demonstrates that ABCA5 is a potential therapeutic target for PDAC and provides a theoretical basis for a new combination therapy of ABCA5 regulation with gemcitabine and WNT inhibitor.
Journal
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CTNNB1 (Catenin (cadherin-associated protein), beta 1) • ABCA5 (ATP Binding Cassette Subfamily A Member 5)
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gemcitabine • foscenvivint (PRI724)
18d
Discovery of ZX079 as a Dual PROTAC Degrader Targeting BRD4/CBP in Acute Myeloid Leukemia. (PubMed, J Med Chem)
The lead compound, 10k (ZX079), induces potent, dose- and time-dependent degradation of BRD4 and CBP and demonstrates superior suppression of oncogenic transcription and inhibition of AML cell proliferation compared with the dual BET/CBP inhibitor NEO2734. In vivo, 10k significantly reduces tumor growth in an AML xenograft model with TGI over 90%. Collectively, these findings highlight dual degradation of BRD4 and CBP as a promising strategy for AML.
Journal
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BRD4 (Bromodomain Containing 4)
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EP31670
28d
Enrollment open
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dexamethasone • pomalidomide • inobrodib (CCS1477)
29d
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