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    DRUG:

    basroparib (STP1002)

    i
    Company:
    Dong-A
    Drug class:
    TNKS inhibitor
    Related drugs:
    14d
    Basroparib overcomes acquired resistance to MEK inhibitors by inhibiting Wnt-mediated cancer stemness in KRAS-mutated colorectal cancer. (PubMed, Biochem Pharmacol)
    Mechanistically, basroparib suppressed Wnt-mediated cancer stemness, a bypass mechanism for acquired resistance to MEK inhibitors in KRAS-mutated CRC. This study provides the first preclinical evidence of the relevance of basroparib in treating CRC with acquired resistance to MEK inhibitors due to APC and KRAS mutations, possibly by reducing the Wnt-mediated cancer stemness.
    Preclinical • Journal
    |
    KRAS (KRAS proto-oncogene GTPase) • APC (APC Regulator Of WNT Signaling Pathway)
    |
    KRAS mutation • KRAS G12D • KRAS wild-type • KRAS G13D • KRAS G13
    |
    basroparib (STP1002)
    1year
    First-In-Human Dose-Escalation Study of STP1002 in Patients With Advanced-Stage Solid Tumors (clinicaltrials.gov)
    P1, N=32, Completed, ST Pharm Co., Ltd. | Active, not recruiting --> Completed
    Trial completion
    |
    basroparib (STP1002)
    over2years
    Tankyrase-selective inhibitor STP1002 shows preclinical antitumour efficacy without on-target toxicity in the gastrointestinal tract. (PubMed, Eur J Cancer)
    These results demonstrate that STP1002, a novel, orally active tankyrase inhibitor, shows preclinical antitumour efficacy without on-target toxicity in the GI tract. Our data provide a rationale for a clinical trial on STP1002 as a potential tankyrase-targeted drug in patients with APC-mutated CRC.
    Preclinical • Journal • PARP Biomarker
    |
    APC (APC Regulator Of WNT Signaling Pathway) • PARP1 (Poly(ADP-Ribose) Polymerase 1)
    |
    KRAS mutation • APC mutation
    |
    G007-LK • basroparib (STP1002)