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DRUG CLASS:

Chk2 inhibitor

4d
ACR-368-201: A Phase 2 Study of ACR-368 in Endometrial Adenocarcinoma (clinicaltrials.gov)
P2, N=401, Recruiting, Acrivon Therapeutics | Trial completion date: Apr 2027 --> Nov 2027 | Trial primary completion date: Oct 2026 --> May 2027
Trial completion date • Trial primary completion date
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TP53 (Tumor protein P53)
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TP53 mutation
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gemcitabine • prexasertib (ACR-368)
10d
ACR-368-201: A Phase 2 Study of ACR-368 in Endometrial Adenocarcinoma (clinicaltrials.gov)
P2, N=353, Recruiting, Acrivon Therapeutics | N=72 --> 353
Enrollment change
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gemcitabine • prexasertib (ACR-368)
1m
Enrollment change
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OncoSignature® Test
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gemcitabine • prexasertib (ACR-368)
2ms
New P1/2 trial
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gemcitabine • prexasertib (ACR-368)
4ms
CHK1 inhibition by prexasertib sensitizes cisplatin-resistant malignant tumor cells via checkpoint abrogation and STAT1-driven PD-L1 upregulation. (PubMed, Int Immunopharmacol)
Co-treatment with interferon-γ further amplified PD-L1 and γH2A.X expression, highlighting a link between CHK1 inhibition, DNA damage, and immune checkpoint modulation. These findings suggest that Prexasertib not only enhances the cytotoxic effects of cisplatin but also influences immune signaling, providing a mechanistic rationale for future exploration of combined DNA damage response inhibition with immune checkpoint blockade.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • IFNG (Interferon, gamma) • STAT1 (Signal Transducer And Activator Of Transcription 1)
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PD-L1 expression
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cisplatin • prexasertib (ACR-368)
6ms
Combined CHK1 and PD-L1 blockade as a novel therapeutic strategy against stemness and immunosuppression in ovarian cancer. (PubMed, Cancer Immunol Immunother)
Dual targeting of CHK1 and PD-L1 may improve OC treatment by simultaneously suppressing stemness and enhancing anti-tumor immunity.
Journal • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule) • CHEK1 (Checkpoint kinase 1)
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PD-L1 expression
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Tecentriq (atezolizumab) • prexasertib (ACR-368)
7ms
FSTL3 is a biomarker of poor prognosis and associated with immunotherapy resistance in ovarian cancer. (PubMed, J Exp Clin Cancer Res)
FSTL3 overexpression completely abrogated tumor response to PPC treatment (Prexasertib combined with PD-1 and CTLA-4 blockade) compared to controls, suggesting that FSTL3 may be involved in immunotherapy resistance. In conclusion, this study suggests a role for FSTL3 as a prognostic marker and as therapeutic target in HGSOC, where it may play a role in promoting a mesenchymal tumor phenotype, maintaining an immunosuppressive tumor microenvironment, and driving immunotherapy resistance.
Journal • PD(L)-1 Biomarker • IO biomarker
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KRAS (KRAS proto-oncogene GTPase) • CD8 (cluster of differentiation 8) • CCNE1 (Cyclin E1)
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KRAS G12
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prexasertib (ACR-368)
8ms
CHEK1 is a synthetic lethal interactor of FBXO7 in colonic epithelial cells. (PubMed, Mol Ther Oncol)
Furthermore, combining Prexasertib with 5-fluorouracil, a standard chemotherapeutic agent, produced a synergistic killing effect. These findings establish a novel synthetic lethal relationship between FBXO7 and CHEK1, suggesting that CHEK1 inhibition may provide a targeted therapeutic strategy for CRC patients with FBXO7 deficiencies, and highlighting the broader potential of exploiting SCF complex alterations in CRC therapy.
Journal
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CHEK1 (Checkpoint kinase 1) • CUL1 (Cullin 1)
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5-fluorouracil • prexasertib (ACR-368)
9ms
New P1/2 trial
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FLT3-ITD mutation
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lasmotinib (PHI-101)
9ms
Decoding the Genomic and Functional Landscape of Emerging Subtypes in Ovarian Cancer. (PubMed, Cancer Discov)
Strikingly, three HRP subtypes emerged, marked by unique structural alterations and gene expression patterns, tumor microenvironment interactions, and different chemotherapy responses. Finally, organoid experiments showed subtype-specific sensitivity to CHK1 inhibition, suggesting prexasertib as a potential targeted treatment for most currently untreatable HRP patients.
Journal • BRCA Biomarker • PARP Biomarker
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency)
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HRD
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prexasertib (ACR-368)
10ms
ACR-368-201: A Phase 2 Study of ACR-368 in Endometrial Adenocarcinoma (clinicaltrials.gov)
P2, N=353, Recruiting, Acrivon Therapeutics | Phase classification: P1/2 --> P2 | Trial completion date: Dec 2027 --> Apr 2027 | Trial primary completion date: Jul 2026 --> Oct 2026
Phase classification • Trial completion date • Trial primary completion date
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gemcitabine • prexasertib (ACR-368)