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

Wnt signalling pathway inhibitor

7d
Histone lactylation-driven feedback loop modulates pyrimidine metabolism to promote oral carcinogenesis. (PubMed, Cell Death Dis)
Moreover, the Wnt/β-catenin inhibitor XAV939 reduced lactate production and H3K18la levels. Here, we demonstrate that the glycolysis/H3K18la/TK1/β-catenin positive feedback loop exacerbates dysfunction in OSCC initiation. These findings reveal a novel link between epigenetic regulation and lactate-driven metabolic reprogramming, which may lead to the development of innovative lactylation treatment approaches for OSCC therapy.
Journal
|
LDHA (Lactate dehydrogenase A) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • RHOA (Ras homolog family member A) • TK1 (Thymidine Kinase 1)
|
XAV-939
13d
Mechanism of KLF4 Inhibition of epithelial-mesenchymal transition in gastric cancer cells. (PubMed, Open Life Sci)
Following transfection, the Wnt signaling pathway inhibitor XAV-939 and agonist SKL2001 were administered to the KLF4-overexpressing cells...Results demonstrated that KLF4 overexpression inhibits EMT in gastric cancer cells through the Wnt/β-catenin signaling pathway. Thus, this study concludes that KLF4 may modulate EMT in gastric cancer cells via the Wnt/β-catenin pathway.
Journal
|
KLF4 (Kruppel-like factor 4)
|
XAV-939
14d
MAGI3 deficiency unleashes β-catenin conformational change to drive metastatic progression and mTOR inhibitor resistance in ccRCC. (PubMed, Cell Death Dis)
Combining Everolimus with the Wnt inhibitor XAV-939 slashed viability and invasion in resistant cells. Its loss defines a metastatic, therapy-resistant subtype targetable by dual mTOR/Wnt blockade. Therefore, MAGI3 expression may stratify patients for personalized therapy.
Journal
|
CTNNB1 (Catenin (cadherin-associated protein), beta 1)
|
everolimus • XAV-939
14d
SM04690-OA-07: A Long-Term Safety and Efficacy Study of Lorecivivint in Subjects With Osteoarthritis of the Knee (clinicaltrials.gov)
P3, N=276, Terminated, Biosplice Therapeutics, Inc. | Completed --> Terminated; Study OA-07 was designed to be conducted until the Sponsor closed it. Study OA-07 was administratively closed at Visit 6E (Week 100), with no safety concerns, one year into the open-label study as described in the protocol.
Trial termination
19d
IFIT3-DVL interaction promotes malignant progression of lung squamous cell carcinoma and large-cell lung carcinoma via canonical WNT signaling. (PubMed, J Biol Chem)
DVL2 knockdown or XAV-939 significantly abrogates above effects mediated by IFIT3 (p <0.05). Overall, we demonstrated a novel signal transduction pathway where IFIT3 interacts with DVL2 to stabilize cytosolic β-catenin and promote β-catenin nuclear translocation via DVL2 phosphorylation, enhancing canonical WNT signaling activity and providing a potential target for clinical intervention in LUSC and LCLC.
Journal
|
MYC (V-myc avian myelocytomatosis viral oncogene homolog) • CCND1 (Cyclin D1) • CDK4 (Cyclin-dependent kinase 4) • MMP2 (Matrix metallopeptidase 2) • CDC42 (Cell Division Cycle 42) • DVL1 (Dishevelled Segment Polarity Protein 1)
|
XAV-939
27d
New P1/2 trial
|
BRAF (B-raf proto-oncogene)
|
MSI-H/dMMR • BRAF mutation • RAS wild-type
|
tegavivint (BC2059)
1m
Study of E7386 in Participants With Selected Advanced Neoplasms (clinicaltrials.gov)
P1, N=60, Active, not recruiting, Eisai Inc. | Trial completion date: Mar 2026 --> Mar 2027 | Trial primary completion date: Mar 2026 --> Mar 2027
Trial completion date • Trial primary completion date
|
CTNNB1 (Catenin (cadherin-associated protein), beta 1)
|
E7386
1m
Tegavivint With Gemcitabine in Patients With Relapsed or Refractory Osteosarcoma (clinicaltrials.gov)
P1, N=24, Recruiting, Emory University | Not yet recruiting --> Recruiting
Enrollment open
|
gemcitabine • tegavivint (BC2059)
1m
Oral Streptococcus salivarius Couples Neutrophil IRGM1 Signaling to NET Formation and Colorectal Cancer Metastasis. (PubMed, Adv Sci (Weinh))
Functional validation experiments show that conditional deletion of IRGM1 or pharmacological inhibition of downstream signaling using XAV-939 markedly attenuates S. salivarius-induced NET formation, indicating the requirement of this pathway in the metastatic process. Furthermore, clinical sample analyses reveal that S. salivarius is significantly enriched in the tongue coating and feces of patients with CRC and is elevated within the tumor microenvironment. Together, these findings identify IRGM1-IQGAP1-mediated Wnt5a-PI3K/AKT signaling as a mechanistic link between oral microbiota and neutrophil-driven immune responses in cancer metastasis.
Journal
|
IQGAP1 (IQ Motif Containing GTPase Activating Protein 1)
|
XAV-939
1m
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
|
EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability)
|
BRAF V600E • MSI-H/dMMR • BRAF V600 • KRAS wild-type • NRAS wild-type
|
paclitaxel • Lenvima (lenvatinib) • doxorubicin hydrochloride • E7386
1m
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
|
RNF43 (Ring Finger Protein 43) • APC (APC Regulator Of WNT Signaling Pathway) • AXIN1 (Axin 1) • ZNRF3 (Zinc And Ring Finger 3)
|
E7386