^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG CLASS:

CBP inhibitor

1m
Pyraclostrobin Exposure Triggers Renal Injury by Activating Wnt/β-Catenin Signaling Pathway-Mediated Renal Fibrosis in Mice. (PubMed, J Appl Toxicol)
Inhibition with ICG-001 significantly attenuated PY-induced fibrosis, confirming Wnt/β-catenin-dependent effects. These findings provide mechanistic insight into PY-induced renal injury and fibrosis.
Preclinical • Journal
|
MYC (V-myc avian myelocytomatosis viral oncogene homolog) • CCND1 (Cyclin D1) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL10 (Interleukin 10) • KIM1 (Kidney injury molecule 1) • TGFB1 (Transforming Growth Factor Beta 1) • LCN2 (Lipocalin-2) • IL1B (Interleukin 1, beta) • CTGF (Connective tissue growth factor)
|
foscenvivint (PRI724)
1m
Src and β-catenin control a senescence-fibrotic phenotype in uterine fibroid cells. (PubMed, Sci Rep)
Furthermore, the senolytic Src inhibitor dasatinib reduced senescence and fibrosis markers and attenuated β-catenin activity, suggesting that Src acts upstream of β-catenin in this context. Inhibition of β-catenin using ICG001 or PRI724 suppressed senescence and fibrosis markers and reduced downstream targets including CTGF and cyclin D1. These findings reveal a mechanistic link between mechanical stiffness, cellular senescence, and fibrosis in uterine fibroids, and identify Src and β-catenin as potential therapeutic targets.
Journal
|
CCND1 (Cyclin D1) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • CTGF (Connective tissue growth factor)
|
dasatinib • foscenvivint (PRI724)
2ms
Enrollment change
|
Nubeqa (darolutamide)
2ms
A first-in-human, open-label multicentre Phase 1 study of the orally administered E7386 in patients with selected advanced neoplasms. (PubMed, Br J Cancer)
E7386 demonstrated a manageable safety profile, a dose-dependent pharmacokinetic profile, and some disease stabilisation in heavily pretreated patients with advanced solid tumours.
P1 data • Journal • First-in-human
|
CTNNB1 (Catenin (cadherin-associated protein), beta 1)
|
E7386
3ms
Discovery of CZL-149: A Novel, Highly Potent, and Orally Bioavailable Dual Inhibitor Targeting BET and p300/CBP Bromodomains with Strong Antitumor Efficacy. (PubMed, J Med Chem)
CZL-149 displays favorable drug-like properties and metabolic profile, achieving 107% oral bioavailability in mice. Importantly, CZL-149 outperformed NEO2734 in both antitumor efficacy (TGI = 78%) and safety in vivo, highlighting its potential as an advanced preclinical candidate worthy of further development.
Journal
|
CREBBP (CREB binding protein)
|
EP31670
3ms
P300/CBP inhibition with inobrodib in combination with gilteritinib and venetoclax targets leukemia stem cells in epigenetic mutant AML. (PubMed, Sci Adv)
We find that use of the dual histone acetyltransferase p300/CBP bromodomain inhibitor CCS1477 (inobrodib), together with venetoclax and gilteritinib, virtually eliminates leukemia stem cells in an aggressive preclinical model of DNMT3A/FLT3-mutant AML by impairing pro-oncogenic survival and proliferation factors to effectively block leukemogenesis. This work identifies potential clinical utility of a targeted, triplet combination therapy for treatment of AML.
Journal • IO biomarker
|
FLT3 (Fms-related tyrosine kinase 3) • BCL2 (B-cell CLL/lymphoma 2) • DNMT3A (DNA methyltransferase 1)
|
FLT3 mutation
|
Venclexta (venetoclax) • Xospata (gilteritinib) • inobrodib (CCS1477)
3ms
A Phase 1 Oral Mass Balance and Combined Intravenous [14C] Microtracer Study to Characterize the Absorption, Metabolism, Excretion, and Pharmacokinetics of Antitumor Drug E7386 in Humans. (PubMed, J Clin Pharmacol)
These results suggest that [14C]E7386-related material is predominantly excreted in feces after oral administration. Overall, IV administration and oral administration of a single E7386 dose was tolerable in healthy participants, and adverse events were manageable.
Clinical • P1 data • PK/PD data • Journal
|
CREBBP (CREB binding protein)
|
E7386
4ms
Phase III Trial of Camrelizumab+Apatinib+Eribulin vs. Physician's Choice Chemotherapy in Advanced Triple-Negative Breast Cancer (clinicaltrials.gov)
P3, N=246, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University | Active, not recruiting --> Recruiting | Trial completion date: Mar 2031 --> Jun 2029 | Trial primary completion date: Sep 2030 --> Dec 2028
Enrollment open • Trial completion date • Trial primary completion date
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
|
ER positive • HER-2 negative • ER negative • HER-2 negative + AR positive + ER positive • HER-2 negative + ER positive
|
AiRuiKa (camrelizumab) • AiTan (rivoceranib) • eribulin mesylate
4ms
A multicenter, single-arm phase II clinical study of eribulin combined with inituzumab and pyrotinib in the treatment of HER2-positive advanced breast cancer (ChiCTR2600121825)
P2, N=76, Recruiting, Fifth Affiliated Hospital, Sun Yat-Sen University; Fifth Affiliated Hospital, Sun Yat-Sen University
New P2 trial
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 expression
|
Irene (pyrotinib) • eribulin mesylate • TheraCIM (nimotuzumab)
4ms
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
|
KEAP1 (Kelch Like ECH Associated Protein 1) • NUP62 (Nucleoporin 62)
|
eribulin mesylate
4ms
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
|
FOLR1 ( Folate receptor alpha )
|
FOLR1 expression
|
eribulin mesylate • farletuzumab ecteribulin (MORAb-202)
4ms
A Study Evaluating the Safety and Efficacy of AUR107 in Patients With Relapsed Advanced Malignancies (SHAKTI-1) (clinicaltrials.gov)
P1, N=50, Recruiting, Aurigene Discovery Technologies Limited | Trial primary completion date: Jun 2025 --> Jan 2027
Trial primary completion date • First-in-human
|
AUR-107