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    DRUG CLASS:

    Topoisomerase II-alpha inhibitor

    Related drugs:
    2ms
    Study of Liposomal Annamycin in Combination With Cytarabine for the Treatment of Subjects With Acute Myeloid Leukemia (AML) (clinicaltrials.gov)
    P1/2, N=22, Completed, Moleculin Biotech, Inc. | Active, not recruiting --> Completed | N=63 --> 22
    Trial completion • Enrollment change
    |
    naxtarubicin (L-ANN)
    3ms
    Design, synthesis, and anticancer evaluation of new Quinazoline hybrids: DNA intercalation, topoisomerase IIα inhibition, and in silico studies. (PubMed, Bioorg Chem)
    Moreover, DNA intercalation of the most prominent compounds 7 and 10 was assessed using the DNA/methyl green assay using doxorubicin as a positive control...Moreover, topoisomerase IIα inhibitory assay of compounds 7 and 10, was conducted using etoposide as a positive control...It was shown that feasible binding interactions at the target site and eligible pharmacokinetic/toxicity profiles were attained for the investigated compounds. Accordingly, the synthesized compounds can be regarded as promising lead compounds with future optimization for cancer treatment.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein)
    |
    doxorubicin hydrochloride • etoposide IV
    8ms
    L-Annamycin for Injection in Combination with Cytarabine Injection As Second Line Therapy for Remission Induction in Adult Subjects with Refractory/relapsed AML (clinicaltrials.gov)
    P2/3, N=334, Recruiting, Moleculin Biotech, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    naxtarubicin (L-ANN)
    10ms
    Noncanonical inhibition of topoisomerase II alpha by oxidative stress metabolites. (PubMed, Redox Biol)
    Chemotherapy agents such as etoposide are poisons that trap TOP2A mid-cycle, covalently bound to cleaved DNA, leaving behind DNA double strand breaks and activating DNA damage response...HNE modifies multiple sites on human TOP2A in vitro, including alkylating Cys216 in the ATPase domain in a DNA-dependent fashion. Taken together, our data suggest an underappreciated role for TOP2A as a redox sensor in tumor cells, connecting oxidative stress to DNA damage signaling and thereby creating a target for redox-active drugs.
    Journal
    |
    TOP2A (DNA topoisomerase 2-alpha)
    |
    etoposide IV
    11ms
    L-Annamycin for Injection in Combination with Cytarabine Injection As Second Line Therapy for Remission Induction in Adult Subjects with Refractory/relapsed AML (clinicaltrials.gov)
    P2/3, N=334, Not yet recruiting, Moleculin Biotech, Inc.
    New P2/3 trial
    |
    naxtarubicin (L-ANN)
    1year
    Study of Liposomal Annamycin in Combination with Cytarabine for the Treatment of Subjects with Acute Myeloid Leukemia (AML) (clinicaltrials.gov)
    P1/2, N=63, Active, not recruiting, Moleculin Biotech, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed • Combination therapy
    |
    naxtarubicin (L-ANN)
    1year
    Study of Liposomal Annamycin for the Treatment of Subjects with Soft-Tissue Sarcomas (STS) with Pulmonary Metastases (clinicaltrials.gov)
    P1/2, N=36, Completed, Moleculin Biotech, Inc. | Active, not recruiting --> Completed | Phase classification: P1b/2 --> P1/2 | Trial completion date: May 2024 --> Aug 2024
    Trial completion • Phase classification • Trial completion date
    |
    naxtarubicin (L-ANN)
    over1year
    Dual inhibition of topoisomerase II and microtubule of podophyllotoxin derivative 5p overcomes cancer multidrug resistance. (PubMed, Eur J Pharmacol)
    In addition, 5p efficiently impaired tumor growth in KB xenograft mice. Conclusively, this work elucidated the dual inhibitor of topoisomerase II and microtubule of 5p and its mechanism of overcoming the multidrug resistance, indicating that 5p exerts the antitumor potentiality.
    Journal • PARP Biomarker
    |
    ABCB1 (ATP Binding Cassette Subfamily B Member 1) • CASP3 (Caspase 3) • CCNB1 (Cyclin B1) • GSDME (Gasdermin E) • H2AX (H2A.X Variant Histone)
    over1year
    Effects of Topoisomerase II alpha Inhibition on Oral Cancer Cell Metabolism and Cancer Stem Cell Function. (PubMed, Dent Res Oral Health)
    Oral carcinoma cell line SCC25 was cultured in complete DMEM/F12 media and treated with 5μM of Etoposide (Topoisomerase II inhibitor) for 48h...These results indicate that inhibition of TOP2A is more efficacious by decreasing the mitochondrial metabolic reprogramming and thereby downregulating the key anti-apoptotic and pro-survival mediators. Thus, TOP2A represents an ideal therapeutic target and offers a potential treatment strategy for OSCC.
    Journal • Cancer stem
    |
    TOP2A (DNA topoisomerase 2-alpha) • IL6 (Interleukin 6) • BIRC5 (Baculoviral IAP repeat containing 5) • SOX2 • POU5F1 (POU Class 5 Homeobox 1)
    |
    etoposide IV • etoposide oral