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DRUG CLASS:

PARP2 inhibitor

6d
Genetic and metabolic inflammation signatures in chronic inflammatory demyelinating polyneuropathy: the role of IL18 polymorphisms and short-chain fatty acids. (PubMed, Front Mol Neurosci)
In contrast, IL18 promoter variation showed various associations: rs1946518 G allele correlated with peroneal nerve shorter compound motor action potential (CMAP) distal latency and lower ulnar nerve sensory nerve action potential (SNAP) amplitude...We confirmed the presence of acetate, propionate, and butyrate in human CSF and demonstrated serum-CSF equivalence for these SCFAs, while stool concentrations were higher, as expected. Collectively, IL18 polymorphisms and SCFAs readouts emerge as biologically grounded candidates for patient stratification in CIDP; these findings warrant validation in larger, multicenter cohorts integrating electrophysiology with CSF/serum biomarkers and microbiome profiling.
Journal
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TNFA (Tumor Necrosis Factor-Alpha) • IL2 (Interleukin 2) • IL18 (Interleukin 18)
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Akeega (abiraterone/niraparib)
7d
Identification of New Cyclocircadins from Cyclocybe erebia and Their Effects on the Circadian Rhythm of Human Osteosarcoma Cells. (PubMed, J Nat Prod)
Cyclocircadins A, C, D, and F-H delayed the phase of the circadian rhythm, and reduced the amplitude of bioluminescence oscillations. In addition, cyclocircadins A, C, F, and G tended to lengthen the circadian period, whereas cyclocircadin E tended to shorten it. Cyclocircadins A and F-H were more active at lower concentrations than cyclocircadins C-E, indicating that structural variations in the seven-membered ring are critical for their activity.
Journal
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PER2 (Period Circadian Regulator 2)
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Akeega (abiraterone/niraparib)
14d
cis-Clerodane-type diterpenoids from Tinospora crispa and their anticancer potential. (PubMed, Arch Pharm Res)
Their structures were elucidated by 1D and 2D NMR spectroscopy, high-resolution mass spectrometry (HR-ESIMS), interproton distance analysis using NOE peak amplitude normalization for improved cross-relaxation (PANIC), Snatzke's method, and computational ECD and DP4⁺ probability calculations...Overall, compound 3 exhibited the most consistent and potent cell-line specific anticancer effects across both models, highlighting its potential as a promising lead candidate for further anticancer drug development. Collectively, these results suggest concentration-dependent anticancer activity of T. crispa diterpenoids in liver and lung cancer models and further support compound 3 as promising leading candidate targeting key survival signaling pathways in cancer.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3)
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Akeega (abiraterone/niraparib)
15d
Comparison of postprocessing metrics in multimetabolic APT-weighted CEST and 2-deoxy-D-glucose-CEST-MRI for differentiating breast cancer subtypes in a murine model. (PubMed, Eur Radiol Exp)
Advanced multimetabolic APTw-CEST and 2-deoxy-D-glucose-CEST postprocessing metrics allowed adequate preclinical murine BC subtyping. AREX showed potential for 2-deoxy-D-glucose-CEST in tumor characterization; however, APTw-CEST remains superior. MTRasym failed to distinguish between tumor subtypes in CEST-MRI.
Clinical • Preclinical • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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Akeega (abiraterone/niraparib)
19d
A brain-driven neural circuit contributes to tissue regeneration in joint cartilage. (PubMed, Ann Rheum Dis)
Our findings unveil a brain-cartilage circuit that regulates cartilage regeneration, providing valuable insights into the inherent limitations of tissue regeneration and suggesting a promising treatment strategy for enhancing cartilage regeneration.
Journal
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ADRB2 (Adrenoceptor Beta 2) • PRG4 (Proteoglycan 4)
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Akeega (abiraterone/niraparib)
22d
Characteristics of auditory event-related potential and prediction of IDH1 mutation in patients with insular glioma. (PubMed, Quant Imaging Med Surg)
The IDH1-wt group showed higher amplitude of MMN evoked by novel stimulus at Fz and Cz and longer latency of the P300 component evoked by a deviant stimulus at Fz. The combination of AERP parameters yielded a more effective means to predict IDH1 mutation status in patients with insular glioma, which may provide guidance for the surgical intervention of this disease.
Journal
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IDH1 (Isocitrate dehydrogenase (NADP(+)) 1)
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IDH1 mutation • IDH wild-type
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Akeega (abiraterone/niraparib)
27d
CJNJ-67652000 and Prednisone for Treatment of Metastatic Castration-Resistant Prostate Cancer and SPOP Gene Mutations (clinicaltrials.gov)
P2, N=8, Active, not recruiting, Mayo Clinic | Recruiting --> Active, not recruiting | N=30 --> 8 | Trial completion date: Mar 2027 --> Mar 2026 | Trial primary completion date: Mar 2027 --> Mar 2026
Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
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SPOP (Speckle Type BTB/POZ Protein)
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Akeega (abiraterone/niraparib)
1m
Effects of different intensities of electroacupuncture and manual acupuncture at "Shangjuxu" (ST37) on acute inflammatory visceral pain and their relationship with α7nAChR/PI3K/AKT signaling pathway (PubMed, Zhen Ci Yan Jiu)
Both MA and 2 mA EA (not 3, 4, 6 mA EA) stimulation of ST37 have a similar analgesic effect in acute inflammatory visceral pain rats, which may be related to their function in suppressing the activities of α7nAChR/PI3K/AKT signaling pathway.
Journal
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AKT1 (V-akt murine thymoma viral oncogene homolog 1) • TNFA (Tumor Necrosis Factor-Alpha) • IL1B (Interleukin 1, beta)
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Akeega (abiraterone/niraparib)
2ms
CJNJ-67652000 and Prednisone for Treatment of Metastatic Castration-Resistant Prostate Cancer and SPOP Gene Mutations (clinicaltrials.gov)
P2, N=30, Recruiting, Mayo Clinic | Trial completion date: Sep 2025 --> Mar 2027 | Trial primary completion date: Sep 2025 --> Mar 2027
Trial completion date • Trial primary completion date
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SPOP (Speckle Type BTB/POZ Protein)
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Akeega (abiraterone/niraparib)
5ms
Discovery of a novel benzofuran-7-carboxamide-based PARP1/c-Met dual inhibitor for addressing c-Met amplification-mediated PARP1i acquired-resistance. (PubMed, Eur J Med Chem)
In this study, we report the development of a novel PARP1/c-Met dual inhibitor derived from the benzofuran-7-carboxamide moiety of the PARP1 inhibitor Mefuparib. Compared with compound 16 obtained in the previous study, compound S12 was identified as a highly potent dual inhibitor with lower molecule weight and better solubility, demonstrating robust inhibitory activity against both PARP1 (IC50 = 21.8 nM) and c-Met (IC50 = 30.2 nM). Importantly, S12 exhibited remarkable anti-tumor efficacy in the HCT116OR xenograft models, suggesting that targeting both PARP1 and c-Met represents an effective therapeutic strategy to overcome PARP1 inhibitor resistance mediated by c-Met amplification.
Preclinical • Journal
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MET (MET proto-oncogene, receptor tyrosine kinase)
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MET amplification
8ms
A dose exploration and dose expansion phase Ib/II study to evaluate oral HTMC0435 tablets in combination with platinum and etoposide in patients with extensive stage small cell lung cancer (ChiCTR2500100955)
P1/2, N=74, Recruiting, The First Affiliated Hospital of Zhengzhou University; Shanghai Yidian Pharmaceutical Technology Development Co., Ltd.
New P1/2 trial
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cisplatin • carboplatin • etoposide IV
1year
CJNJ-67652000 and Prednisone for Treatment of Metastatic Castration-Resistant Prostate Cancer and SPOP Gene Mutations (clinicaltrials.gov)
P2, N=30, Recruiting, Mayo Clinic | Trial completion date: Dec 2025 --> Sep 2025 | Trial primary completion date: Dec 2025 --> Sep 2025
Trial completion date • Trial primary completion date
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SPOP (Speckle Type BTB/POZ Protein)
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SPOP mutation
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Zejula (niraparib) • abiraterone acetate • Akeega (abiraterone/niraparib)