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    DRUG:

    chiauranib (CS 2164)

    i
    Other names: CS 2164, CS2164, CS-2164
    Company:
    Chipscreen
    Drug class:
    c-KIT inhibitor, VEGFR inhibitor, PDGFR inhibitor, PDGFR α antagonist, CSF-1R inhibitor, Aurora kinase B inhibitor
    Related drugs:
    4ms
    Phase 3 Clinical Study of Chiauranib Capsule in Patients With Small-cell Lung Cancer (clinicaltrials.gov)
    P3, N=180, Recruiting, Chipscreen Biosciences, Ltd. | Trial primary completion date: Mar 2024 --> Dec 2024
    Trial primary completion date
    |
    chiauranib (CS 2164)
    4ms
    A Phase II Study of Chiauranib in Combine With Capecitabine in TNBC (clinicaltrials.gov)
    P2, N=38, Recruiting, Chipscreen Biosciences, Ltd. | Trial completion date: Aug 2024 --> Dec 2024 | Trial primary completion date: Mar 2024 --> Dec 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    capecitabine • chiauranib (CS 2164)
    4ms
    Chiauranib for Advanced Solid Malignant Tumors and Relapsed/Refractory SCLC. (clinicaltrials.gov)
    P1/2, N=36, Recruiting, Chipscreen Biosciences, Ltd. | Trial completion date: Apr 2024 --> May 2025 | Trial primary completion date: Mar 2024 --> Mar 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    chiauranib (CS 2164)
    4ms
    Chiauranib for Advanced or Unresectable Soft Tissue Sarcoma(STS) (clinicaltrials.gov)
    P2, N=40, Active, not recruiting, Chipscreen Biosciences, Ltd. | Recruiting --> Active, not recruiting | Trial completion date: Jun 2024 --> Dec 2024 | Trial primary completion date: Feb 2024 --> Dec 2024
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    chiauranib (CS 2164)
    4ms
    Mass Balance Study of [14C]Chiauranib (clinicaltrials.gov)
    P=N/A, N=6, Completed, Chipscreen Biosciences, Ltd. | Recruiting --> Completed | Trial primary completion date: Nov 2023 --> Mar 2024
    Trial completion • Trial primary completion date
    |
    chiauranib (CS 2164)
    4ms
    Chiauranib in Patients With Locally Advanced or Metastatic Pancreatic Ductal Adenocarcinoma (clinicaltrials.gov)
    P2, N=42, Not yet recruiting, Chipscreen Biosciences, Ltd.
    New P2 trial • Metastases
    |
    gemcitabine • albumin-bound paclitaxel • chiauranib (CS 2164)
    6ms
    A Study of AK104 in Combination With Chiauranib in Patients With Extensive Stage Small Cell Lung Cancer (clinicaltrials.gov)
    P1/2, N=36, Active, not recruiting, Akeso | Recruiting --> Active, not recruiting | Trial completion date: Dec 2025 --> Jan 2025
    Enrollment closed • Trial completion date
    |
    ATRX (ATRX Chromatin Remodeler)
    |
    Kaitanni (cadonilimab) • chiauranib (CS 2164)
    8ms
    Chiauranib for Advanced Solid Malignant Tumors and Relapsed/Refractory SCLC. (clinicaltrials.gov)
    P1/2, N=36, Recruiting, Chipscreen Biosciences, Ltd. | Phase classification: P1b/2 --> P1/2
    Phase classification • Metastases
    |
    chiauranib (CS 2164)
    over1year
    Inhibition of extranodal NK/T-cell lymphoma by Chiauranib through an AIF-dependent pathway and its synergy with L-asparaginase. (PubMed, Cell Death Dis)
    This study demonstrates Chiauranib's positive efficacy toward NKTL through the activation of the AIF-dependent apoptosis pathway for the first time. The novel and multi-targets of Chiauranib and the synergistic effect with L-asparaginase may provide a promising therapy for NKTL patients.
    Journal
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CASP8 (Caspase 8) • FAS (Fas cell surface death receptor)
    |
    BAX expression
    |
    chiauranib (CS 2164)
    almost2years
    Preclinical Studies of Chiauranib Show It Inhibits Transformed Follicular Lymphoma through the VEGFR2/ERK/STAT3 Signaling Pathway. (PubMed, Pharmaceuticals (Basel))
    Mechanistically, chiauranib suppresses the phosphorylation level of VEGFR2, which has an anti-t-FL effect by inhibiting the downstream MEK/ERK/STAT3 signaling cascade. In conclusion, chiauranib may be a potential therapy to treat t-FL, since it inhibits tumor growth and migration and induces apoptosis by altering the VEGFR2/ERK/STAT3 signaling pathway.
    Preclinical • Journal
    |
    CSF1R (Colony stimulating factor 1 receptor)
    |
    chiauranib (CS 2164)
    almost2years
    Preclinical Studies of Chiauranib Inhibit Follicular Lymphoma through VEGFR2/ERK/STAT3 Signaling Pathway (ASH 2022)
    Finally, we found that the VEGFR2/ERK/STAT3 signaling pathway is closely related to an inhibitory effect of Chiauranib.In conclusion, by acting on VEGFR2, chiauranib is acting on the VEGFR2/ERK/STAT3 signaling pathway, thereby altering the expression level of STAT3 target genes, ultimately leading to decreased cell proliferation, increased apoptosis, slowed migration, and decreased angiogenesis. These findings provide a basis for further clinical exploration of chiauranib as a promising treatment for follicular lymphoma.
    Preclinical • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • CSF1R (Colony stimulating factor 1 receptor)
    |
    chiauranib (CS 2164)
    over2years
    A Phase II Study of Chiauranib in Combine With Capecitabine in TNBC (clinicaltrials.gov)
    P2, N=38, Recruiting, Chipscreen Biosciences, Ltd.
    New P2 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER negative • PGR negative
    |
    capecitabine • chiauranib (CS 2164)
    over2years
    Chiauranib for Relapsed/Refractory Small Cell Lung Cancer (clinicaltrials.gov)
    P1b/2, N=36, Recruiting, Chipscreen Biosciences, Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    ATRX (ATRX Chromatin Remodeler)
    |
    ATRX mutation
    |
    chiauranib (CS 2164)
    over3years
    Phase 3 Clinical Study of Chiauranib Capsule in Patients With Small-cell Lung Cancer (clinicaltrials.gov)
    P3, N=180, Recruiting, Chipscreen Biosciences, Ltd.
    New P3 trial
    |
    LIPI (Lipase I)
    |
    chiauranib (CS 2164)
    over3years
    CS2164 and Venetoclax Show Synergistic Antitumoral Activities in High Grade B-Cell Lymphomas With MYC and BCL2 Rearrangements. (PubMed, Front Oncol)
    In addition, MCL1 and BCL-XL, two well-characterized contributors for venetoclax resistance, were significantly lessened in the presence of CS2164 and venetoclax, thus leading to the accumulation of proapoptotic proteins BAX and PUMA and then initiating the intrinsic apoptosis pathway. Taken together, these findings suggest that the regimen of CS2164 and venetoclax is highly effective to eliminate HGBL-DHL cells in the preclinical setting, warranting further clinical investigations of this regimen for the treatment of unfavorable HGBL-DHL patients.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL2L1 (BCL2-like 1)
    |
    BCL2 expression • MYC expression • MYC rearrangement • BCL2 rearrangement
    |
    Venclexta (venetoclax) • chiauranib (CS 2164)
    almost4years
    Chiauranib selectively inhibits colorectal cancer with KRAS wild-type by modulation of ROS through activating the p53 signaling pathway. (PubMed, Am J Cancer Res)
    Colorectal cancer (CRC) is one of the top three most deadly cancers despite using chemotherapy based on oxaliplatin or irinotecan combined with targeted therapy. Further, KRAS mutation CRC cells are resistant to Chiauranib by increasing Nrf2 to stably elevate the basal antioxidant program and thereby lower intracellular ROS induced by Chiauranib. Our findings provide the rationale for further clinical evaluation of Chiauranib as a therapeutic agent in treating KRAS wild-type CRC.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    oxaliplatin • irinotecan • chiauranib (CS 2164)
    4years
    [VIRTUAL] Combination of CS2164 and Venetoclax Shows Synergistic Antitumor Effect in High-Grade B-Cell Lymphomas with ConcomitantMYCandBCL2Rearrangements (ASH 2020)
    The underlying mechanisms for the synergy of the two drugs included the blockade of Rad51 recombinase-dependent DNA repair, the perturbation of the delicate balance of BCL2 family proteins that induced mitochondrial membrane depolarization and subsequently led to the proapoptotic effect, as well as the inhibition of PI3K/AKT/mTOR pathway and MYC expression. In summary, these findings suggest that the regimen of CS2164 and venetoclax combination is highly effective to eliminate HGBCL-DHL cellsin vitroandin vivoand thus provide a rational treatment paradigm to strip HGBCL-DHL of its protection fromMYCandBCL2rearrangements.
    IO biomarker
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • RAD51 (RAD51 Homolog A)
    |
    MYC expression • BCL2 rearrangement
    |
    Venclexta (venetoclax) • chiauranib (CS 2164)
    4years
    Antitumor and immunomodulatory effects of a novel multitarget inhibitor, CS2164, in mouse hepatocellular carcinoma models. (PubMed, Anticancer Drugs)
    The work cannot be changed in any way or used commercially without permission from the journal. http://creativecommons.org/licenses/by-nc-nd/4.0/.
    Preclinical • Journal
    |
    CD8 (cluster of differentiation 8)
    |
    chiauranib (CS 2164)