^
    15d
    Testing the Combination of APG-1252 (Pelcitoclax) and Cobimetinib in Recurrent Ovarian and Endometrial Cancers (clinicaltrials.gov)
    P1, N=42, Active, not recruiting, National Cancer Institute (NCI) | Recruiting --> Active, not recruiting
    Enrollment closed
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    BRAF (B-raf proto-oncogene)
    |
    Cotellic (cobimetinib) • pelcitoclax (APG-1252)
    19d
    Phase1b/2 Trial Of AZA + APG1252 In Patients With High-Risk AML (clinicaltrials.gov)
    P1/2, N=52, Not yet recruiting, M.D. Anderson Cancer Center
    New P1/2 trial
    |
    BCL2 (B-cell CLL/lymphoma 2) • BCL2L1 (BCL2-like 1) • MECOM (MDS1 And EVI1 Complex Locus)
    |
    pelcitoclax (APG-1252)
    2ms
    A Phase 1 Study Of FLAG Chemotherapy In Combination With Lisaftoclax And Pelcitoclax In Patients With Relapsed/Refractory T-Cell Acute Lymphoblastic Leukemia (clinicaltrials.gov)
    P1, N=24, Not yet recruiting, M.D. Anderson Cancer Center
    New P1 trial
    |
    clonoSEQ
    |
    cytarabine • pelcitoclax (APG-1252) • lisaftoclax (APG-2575) • fludarabine IV
    3ms
    APG-1252 enhances the anticancer role of paclitaxel in non-small-cell lung cancer cells by suppressing the extracellular regulated protein kinases/myeloid cell leukemia 1 pathway. (PubMed, Anticancer Drugs)
    APG-1252 enhanced the anticancer role of PTX in NSCLC cells by suppressing the ERK/MCL-1 pathway. This work provided the theoretical basis for the APG-1252 application.
    Journal
    |
    MCL1 (Myeloid cell leukemia 1)
    |
    paclitaxel • pelcitoclax (APG-1252)
    7ms
    A Study of APG-1252 Plus Osimertinib(AZD9291) in EGFR TKI Resistant NSCLC Patients (clinicaltrials.gov)
    P1, N=80, Active, not recruiting, Ascentage Pharma Group Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    EGFR mutation • EGFR exon 19 deletion • EGFR T790M
    |
    Tagrisso (osimertinib) • pelcitoclax (APG-1252)
    7ms
    ADAPT/A2: ALLG AMLM28/A2 (ADAPT): Achieving Durable remissions via Adaptive Pro-survival Targeting in acute myeloid leukaemia (AML)) – VEN/AZA/Pelcitoclax. A therapeutic arm of the ALLG AMLM28 ADAPT Study-Master Protocol. (ACTRN12625000994482)
    P1/2, N=50, Not yet recruiting, Australasian Leukaemia and Lymphoma Group
    New P1/2 trial
    |
    TP53 (Tumor protein P53)
    |
    TP53 mutation
    |
    Venclexta (venetoclax) • azacitidine • pelcitoclax (APG-1252)
    11ms
    A Study of APG-1252 Plus Osimertinib(AZD9291) in EGFR TKI Resistant NSCLC Patients (clinicaltrials.gov)
    P1, N=80, Recruiting, Ascentage Pharma Group Inc. | Trial completion date: Jun 2025 --> Jun 2026 | Trial primary completion date: Dec 2024 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    EGFR mutation • EGFR exon 19 deletion • EGFR T790M
    |
    Tagrisso (osimertinib) • pelcitoclax (APG-1252)
    12ms
    Albumin nanocomplex of BCL-2/xL inhibitor reduced platelet toxicity and improved anticancer efficacy in myeloproliferative neoplasm and lymphoma. (PubMed, Biomaterials)
    Furthermore, Nano-1252 exhibited preferential accumulation in lymphoid organs, leading to enhanced anticancer efficacy in Mantle Cell Lymphoma (MCL) and Myeloproliferative Neoplasms (MPNs) mouse models. Our study not only develops a potential formulation to overcome the current translational barrier of APG-1252 but also reveals novel properties of the well-established albumin nanoformulation, thereby expanding its clinical applications.
    Journal
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    pelcitoclax (APG-1252)
    1year
    A Study of Pelcitoclax (APG-1252) in Patients With Neuroendocrine Tumors (clinicaltrials.gov)
    P1, N=2, Terminated, Ascentage Pharma Group Inc. | N=60 --> 2 | Recruiting --> Terminated; Company Strategy
    Enrollment change • Trial termination
    |
    BCL2L2 (BCL2 Like 2)
    |
    pelcitoclax (APG-1252)
    1year
    Combinatorial screen with apoptosis pathway targeted agents alrizomadlin, pelcitoclax, and dasminapant in multi-cell type tumor spheroids. (PubMed, SLAS Discov)
    Apoptosis, or programmed cell death, plays a critical role in maintaining tissue homeostasis by eliminating damaged or abnormal cells. Additionally, interactions were observed from combinations of the apoptosis pathway targeted agents with other agents, including PARP inhibitors, the XPO1 inhibitor eltanexor, and the PI3K inhibitor copanlisib. Enhanced activity was also observed from combinations of the apoptosis pathway targeted agents with MAPK pathway targeted agents, including the MEK inhibitor cobimetinib as well as adagrasib and MRTX1133, which specifically target the KRAS G12C and G12D variants, respectively.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase) • BCL2 (B-cell CLL/lymphoma 2) • BCL2L1 (BCL2-like 1)
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    KRAS G12C • KRAS G12D • KRAS G12
    |
    Cotellic (cobimetinib) • Krazati (adagrasib) • Aliqopa (copanlisib) • alrizomadlin (APG-115) • MRTX1133 • pelcitoclax (APG-1252) • eltanexor (KPT-8602)
    over1year
    A clinical study of olverembatinib in combination with APG-1252 for the treatment of relapsed/refractory Philadelphia chromosome-positive acute lymphoblastic leukemia or T-cell acute lymphoblastic lymphoma (ChiCTR2400094086)
    P1, N=12, Shanghai Children's Medical Center, School of Medicine, Shanghai Jiao Tong University; Shanghai Children's Medical Center, School of Medicine, Shangha
    New P1 trial
    |
    Nailike (olverembatinib) • pelcitoclax (APG-1252)
    over1year
    Testing the Combination of APG-1252 (Pelcitoclax) and Cobimetinib in Recurrent Ovarian and Endometrial Cancers (clinicaltrials.gov)
    P1, N=42, Recruiting, National Cancer Institute (NCI) | Trial completion date: Jun 2026 --> Feb 2027 | Trial primary completion date: Jun 2026 --> Feb 2027
    Trial completion date • Trial primary completion date
    |
    BRAF (B-raf proto-oncogene) • BCL2L1 (BCL2-like 1)
    |
    Cotellic (cobimetinib) • pelcitoclax (APG-1252)