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DRUG CLASS:

Chk1 inhibitor

2d
POTENTIATE: Study of the CHK1 Inhibitor BBI-355, an ecDNA-directed Therapy (ecDTx), and the RNR Inhibitor BBI-825, in Subjects With Tumors With Oncogene Amplifications (clinicaltrials.gov)
P1, N=85, Terminated, Boundless Bio, Inc. | Trial completion date: Mar 2027 --> Mar 2026 | Active, not recruiting --> Terminated | Trial primary completion date: Sep 2026 --> Mar 2026; Decision was made to halt the study based on overall clinical experience and market considerations. This decision was not driven by any safety signal.
Trial completion date • Trial termination • Trial primary completion date • First-in-human
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erlotinib • Lytgobi (futibatinib)
8d
Combination of CHK1 and CHK2 inhibitors exerts synergistic antitumor effects against neuroblastoma cells. (PubMed, Pediatr Res)
Combined CHK1/CHK2 inhibitor therapy shows a synergistic anti-tumor effect against neuroblastoma cells. Combination therapy impairs DNA damage response pathways and drives accelerated cell cycle progression in neuroblastoma cells. Combination therapy increases DNA damage, replication stress, and apoptosis marker expression. Combined CHK1/CHK2 inhibition holds therapeutic potential for the treatment of neuroblastoma.
Journal • PARP Biomarker
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MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • CASP3 (Caspase 3) • RPA2 (Replication Protein A2)
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MYCN amplification
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prexasertib (ACR-368) • PV-1019
15d
AI-driven multi-omics drug repurposing nominates AZD7762 as a multitarget inhibitor of IL22RA1 and FAM221A in esophageal squamous cell carcinoma. (PubMed, NPJ Precis Oncol)
Single-cell RNA sequencing analysis mapped the hub genes interleukin 22 receptor subunit alpha 1 (IL22RA1) and family with sequence similarity 221 member A (FAM221A) to epithelial cell populations and associated them with proliferative and DNA repair programs, supporting their role in tumor progression, supporting their role in ESCC progression. In vitro assays confirmed that IL22RA1 and FAM221A promote ESCC cell proliferation, migration, and invasion. Taken together, this AI-driven multi-omics framework delivers a prognostic model, defines biologically distinct ESCC subgroups, and nominates AZD7762 as a rational multitarget drug repurposing candidate, providing a precision oncology strategy.
Journal
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IL22 (Interleukin 22)
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AZD-7762
16d
The CHK1 inhibitor Prexasertib is effective against in vitro models of aggressive thyroid carcinomas with defective p53 function. (PubMed, Front Endocrinol (Lausanne))
Recently, we demonstrated that the response to Lenvatinib is associated with alterations in TP53 gene or protein. Moreover, Doxorubicin potentiated the Prexasertib effects in p53-defective thyroid cancer cells, yet at the lowest doses. This study unravels the potential of Prexasertib as a novel treatment option for aggressive thyroid cancers p53-defective and poorly responsive to tyrosine kinase inhibitors.
Preclinical • Journal
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CHEK2 (Checkpoint kinase 2)
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Lenvima (lenvatinib) • doxorubicin hydrochloride • prexasertib (ACR-368)
24d
ADGRF4 and ADGRL4 as novel prognostic biomarkers and potential therapeutic implications in stomach adenocarcinoma. (PubMed, BMC Gastroenterol)
ADGRF4 and ADGRL4 were significantly overexpressed in STAD and independently associated with poor prognosis. Expression of these genes was correlated with changes in tumor microenvironment and immune cell infiltration, indicating their potential association in STAD progression. These findings suggest that ADGRF4 and ADGRL4 could serve as novel prognostic biomarkers with potential therapeutic significance in gastric cancer.
Journal
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ELTD1 (Adhesion G Protein-Coupled Receptor L4)
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AZD-7762
1m
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)
1m
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)
2ms
Enrollment change
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OncoSignature® Test
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gemcitabine • prexasertib (ACR-368)
3ms
New P1/2 trial
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gemcitabine • prexasertib (ACR-368)
5ms
Enrollment closed • Enrollment change • First-in-human
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erlotinib • Lytgobi (futibatinib)
5ms
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)