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DRUG CLASS:

Aurora kinase B inhibitor

3d
Enrollment closed • Enrollment change
13d
Molecular mechanism of S100P promotes hepatocellular carcinoma by regulating MYBL2-mediated transcription of AURKB. (PubMed, Cell Signal)
HCC cells with low S100P expression showed significantly greater sensitivity to the AURKB inhibitor AZD1152-HQPA than control cells, with a 61% decrease in IC₅₀. This study reveals the S100P/MYBL2/AURKB axis as a key driver of HCC and a predictor of targeted therapy response, supporting precision treatment strategies.
Journal
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AURKB (Aurora Kinase B) • MYBL2 (MYB Proto-Oncogene Like 2) • S100P (S100 calcium binding protein P)
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barasertib-HQPA (AZD2811)
19d
Treatment monitoring by biomarker analysis in a Phase I dose-expansion study of AZD2811 for relapsed/refractory small-cell lung cancer. (PubMed, Br J Cancer)
A personalised surveillance strategy may provide a novel avenue to monitor SCLC, supporting further investigation and potential broader clinical application.
P1 data • Journal
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AURKB (Aurora Kinase B)
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barasertib-HQPA (AZD2811)
1m
Chiauranib in Patients With Locally Advanced or Metastatic Pancreatic Ductal Adenocarcinoma (clinicaltrials.gov)
P2, N=42, Active, not recruiting, Chipscreen Biosciences, Ltd. | Recruiting --> Active, not recruiting | Trial completion date: Jul 2026 --> Oct 2026 | Trial primary completion date: Feb 2026 --> May 2026
Enrollment closed • Trial completion date • Trial primary completion date
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gemcitabine • albumin-bound paclitaxel • Auraza (chiauranib)
2ms
Design, synthesis, and Lead optimization of novel Quinazoline-based FLT3 inhibitors with potent anti-acute myelogenous leukemia activity. (PubMed, Bioorg Med Chem Lett)
Guided by a scaffold-hopping strategy based on G-749 (denfivontinib), a series of quinazoline-based derivatives was designed and synthesized to explore structure-activity relationships (SAR)...Mechanism studies indicated that W4 induced G0/G1 cell cycle arrest and apoptosis, accompanied by a reduction in intracellular reactive oxygen species levels and a loss of mitochondrial membrane potential. Collectively, these results identified W4 as a potent FLT3 inhibitor and provided valuable SAR insights for further scaffold optimization.
Journal
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FLT3 (Fms-related tyrosine kinase 3) • KIT (KIT proto-oncogene, receptor tyrosine kinase)
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FLT3 mutation
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denfivontinib (SKI-G-801)
2ms
New P3 trial
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gemcitabine • Loqtorzi (toripalimab-tpzi) • albumin-bound paclitaxel • Auraza (chiauranib)
3ms
New P1/2 trial
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Loqtorzi (toripalimab-tpzi)
4ms
Cellular and molecular determinants of lymph node metastasis in papillary thyroid carcinoma: Integrated multi-omics profiling and machine learning models. (PubMed, Comput Biol Chem)
Computational analysis suggests that the high-risk group is potentially sensitive to targeted drugs such as ZM447439. Furthermore, in vitro experiments confirmed that FN1 silencing significantly suppresses the migration and proliferation of PTC cells. This study systematically deciphers the functional adaptive reprogramming during PTC LNM, providing novel insights and tools for LNM prediction and targeted therapy.
Journal
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FN1 (Fibronectin 1) • SDC4 (Syndecan 4)
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ZM 447439
4ms
TAZMAN: Study of AZD2811 + Durvalumab in ES-SCLC (clinicaltrials.gov)
P2, N=31, Active, not recruiting, AstraZeneca | Trial completion date: Dec 2025 --> Dec 2026
Trial completion date
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cisplatin • carboplatin • Imfinzi (durvalumab) • etoposide IV • barasertib-HQPA (AZD2811)
6ms
EP0042-101: Study to Evaluate the Safety and Tolerability of EP0042 (clinicaltrials.gov)
P1/2, N=70, Recruiting, Ellipses Pharma | Trial completion date: Dec 2025 --> Dec 2026
Trial completion date
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Venclexta (venetoclax) • azacitidine • EP0042
6ms
Long noncoding RNA TMPO-AS1 upregulates chromosomal passenger complex expression to promote cell proliferation in lung cancer via sponging microRNA let-7b-5p. (PubMed, Cell Div)
Lung adenocarcinoma patients have poorer prognosis due to higher levels of CPCs, TMPO-AS1, and E2F1. A sponge complex between TMPO-AS1 and hsa-let-7b-5p may contribute to the tumor progression, and targeting CPCs with natural compounds could offer therapeutic potential. Highlights 1. The overexpression of chromosomal passenger complex genes, AURKB, BIRC5, CDCA8, and INCENP is significantly associated with poor prognosis in lung adenocarcinoma (LUAD), particularly among smokers. 2. The competing endogenous RNA (ceRNA) axis, which involves the long non-coding RNA TMPO-AS1 and the miRNA hsa-let-7b-5p, regulates the expression of these CPC genes. TMPO-AS1 shows a positive correlation with CPC genes, while hsa-let-7b-5p shows a negative correlation. 3. Survival analysis indicates that the combined expression of CPC genes, TMPO-AS1, hsa-let-7b-5p, and E2F1 may serve as a reliable prognostic biomarker panel for LUAD in smokers. 4. Hesperidin exhibits a strong binding affinity to CPC proteins, particularly AURKB, when compared to Barasertib, Docetaxel, and Paclitaxel, highlighting its potential as a therapeutic agent. 5. The overexpression of CPC genes, E2F1, and TMPO-AS1 in LUAD is strongly associated with reduced infiltration of CD4⁺ T cells, indicating their role in promoting an immunosuppressive tumor microenvironment.
Journal
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BIRC5 (Baculoviral IAP repeat containing 5) • CD4 (CD4 Molecule) • AURKB (Aurora Kinase B) • CDCA8 (Cell Division Cycle Associated 8) • E2F1 (E2F transcription factor 1) • MIRLET7B (MicroRNA Let-7b) • TMPO-AS1 (TMPO Antisense RNA 1)
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paclitaxel • docetaxel • barasertib (AZD1152)
7ms
DGKα inhibition enhances the antitumor effect of chiauranib on transformed follicular lymphoma. (PubMed, Ann Hematol)
Besides, downregulating the levels of c-Myc, BCL-xL and MCL-1 also contributed to the synergistic effects of the combined regimen on t-FL. Taken together, these findings suggest that the synergy between the DGKα inhibitor ritanserin and multi-targeted inhibitor chiauranib might represent a promising option for the treatment of t-FL.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1) • BCL2L1 (BCL2-like 1)
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Auraza (chiauranib)