Therapy Detail

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Therapy Name G007-LK
Synonyms
Therapy Description

G007-LK inhibits tankyrase, which leads to stabilization of AXIN, thereby resulting in degradation of beta-catenin and decreased growth of APC-deficient tumors (PMID: 23539443, PMID: 32575464).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
G007-LK Tankyrase Inhibitor 11 G007-LK inhibits tankyrase, which leads to stabilization of AXIN, thereby resulting in degradation of beta-catenin and decreased growth of APC-deficient tumors (PMID: 23539443, PMID: 32575464).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
APC S1197* APC S1278* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, treatment with G007-LK decreased active beta-catenin levels and Tcf/LEF activity, and reduced growth of a colorectal cancer cell line harboring APC S1197* and APC S1278* in culture (PMID: 28179481). 28179481
APC R499* colorectal cancer sensitive G007-LK Preclinical - Patient cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC R499* in culture (PMID: 37968472). 37968472
APC L1302Rfs*3 colorectal cancer resistant G007-LK Preclinical - Cell culture Actionable In a preclinical study, a patient-derived colorectal cancer cell line harboring APC L1302Rfs*3 was resistant to G007-LK treatment, as demonstrated by failure to inhibit viability in culture (PMID: 37968472). 37968472
APC R876* colorectal cancer sensitive G007-LK Preclinical - Patient cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC R876* in culture (PMID: 37968472). 37968472
APC V830Gfs*12 APC T1556Nfs*3 colorectal cancer resistant G007-LK Preclinical - Cell culture Actionable In a preclinical study, a patient-derived colorectal cancer cell line harboring APC V830Gfs*12 and T1556Nfs*3, along with PIK3CA E542K, was resistant to G007-LK treatment, as demonstrated by failure to inhibit viability in culture (PMID: 37968472). 37968472
APC S1465Wfs*3 APC T1556Nfs*3 colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC S1465Wfs*3 and T1556Nfs*3 in culture (PMID: 37968472). 37968472
APC W553* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited growth of a patient-derived colorectal cancer cell line harboring APC W553* in culture (PMID: 28179481). 28179481
APC K670* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC K670* in culture (PMID: 37968472). 37968472
APC S1421Rfs*52 colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC S1421Rfs*52 in culture (PMID: 37968472). 37968472
APC R499* APC E1295* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC E1295* and R499* in culture (PMID: 37968472). 37968472
APC Q1406* colorectal cancer predicted - sensitive G007-LK Preclinical Actionable In a preclinical study, G007-LK treatment altered gene expression pattern and inhibited growth of mouse intestinal organoids expressing APC Q1045* (corresponding to Q1046* in human) in culture (PMID: 31337618). 31337618
APC Q1378* colorectal cancer sensitive G007-LK Preclinical - Patient cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC Q1378* in culture (PMID: 37968472). 37968472
APC Y935* APC L1489Yfs*18 colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC L1489Yfs*18 and Y935* in culture (PMID: 37968472). 37968472
APC I1287Rfs*3 colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC I1287Rfs*3 in culture (PMID: 37968472). 37968472
APC L852* colorectal cancer predicted - resistant G007-LK Preclinical Actionable In a preclinical study, G007-LK treatment did not alter gene expression pattern or affect growth in intestinal organoids established from mouse models of colorectal cancer driven by APC L850* (corresponding to L852* in human), and had no effect on tumor cell growth and differentiation in APC L850* mouse models (PMID: 31337618). 31337618
APC Q1367* colorectal cancer resistant G007-LK Preclinical - Patient cell culture Actionable In a preclinical study, a patient-derived colorectal cancer cell line harboring APC Q1367* was resistant to G007-LK treatment, as demonstrated by failure to inhibit viability in culture (PMID: 37968472). 37968472
APC L1489* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC L1489* in culture (PMID: 37968472). 37968472
APC I1164fs colorectal cancer sensitive G007-LK Preclinical - Patient cell culture Actionable In a preclinical study, G007-LK inhibited growth of a patient-derived colorectal cancer cell line harboring APC I1164fs in culture (PMID: 28179481). 28179481
APC L665* APC R1450* colorectal cancer resistant G007-LK Preclinical - Cell culture Actionable In a preclinical study, a colorectal cancer cell line harboring APC L665* and APC R1450* demonstrated low levels of Tcf/LEF activity, and was resistant to treatment with G007-LK in culture (PMID: 28179481). 28179481
APC S299Tfs*7 APC R805* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC R805* and S299Tfs*7 in culture (PMID: 37968472). 37968472
APC E853* APC T1556fs colorectal cancer resistant G007-LK Preclinical - Cell culture Actionable In a preclinical study, a colorectal cancer cell line harboring APC E853* and APC T1556fs (reported as APC T1556fs*3) demonstrated low levels of Tcf/LEF activity, and was resistant to treatment with G007-LK in culture (PMID: 28179481). 28179481
APC S1356* colorectal cancer sensitive G007-LK Preclinical - Patient cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC S1356* in culture (PMID: 37968472). 37968472
APC L665Ifs*8 APC R1450* colorectal cancer resistant G007-LK Preclinical - Cell culture Actionable In a preclinical study, a patient-derived colorectal cancer cell line harboring APC L665Ifs*8 and R1450* was resistant to G007-LK treatment, as demonstrated by failure to inhibit viability in culture (PMID: 37968472). 37968472
APC S811* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, treatment with G007-LK decreased active beta-catenin levels and Tcf/LEF activity, and reduced growth of a colorectal cancer cell line harboring APC S811* in culture (PMID: 28179481). 28179481
APC E633* APC E1494* APC Q1529* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC E1494*, E633*, and Q1529* in culture (PMID: 37968472). 37968472
APC R216* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, a patient-derived colorectal cancer cell line harboring APC R216* demonstrated sensitivity to G007-LK in culture (PMID: 28179481). 28179481
APC E582fs colorectal cancer predicted - resistant G007-LK Preclinical Actionable In a preclinical study, G007-LK treatment did not inhibit growth of mouse intestinal organoids expressing APC E580fs (corresponding to E582fs in human) in culture (PMID: 31337618). 31337618
APC L954* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC L954* in culture (PMID: 37968472). 37968472
APC Q886* colorectal cancer conflicting G007-LK Preclinical Actionable In a preclinical study, G007-LK treatment did not alter gene expression pattern or affect growth in mouse intestinal organoids expressing APC Q884* (corresponding to Q886* in human) in culture (PMID: 31337618). 31337618
APC Q886* colorectal cancer conflicting G007-LK Preclinical - Patient cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC Q886* in culture (PMID: 37968472). 37968472
CTNNB1 S33F colorectal cancer predicted - resistant G007-LK Preclinical Actionable In a preclinical study, G007-LK treatment did not alter gene expression pattern or affect growth in mouse intestinal organoids expressing CTNNB1 S33F (corresponding to S33F in human) in culture (PMID: 31337618). 31337618
APC G1116Efs*6 colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC G1116Efs*6 in culture (PMID: 37968472). 37968472
APC N1819fs APC wild-type colorectal cancer resistant G007-LK Preclinical - Cell culture Actionable In a preclinical study, a colorectal cancer cell line harboring APC N1819fs (reported as N1819fs*7) and a wild-type copy of APC demonstrated low levels of Tcf/LEF activity, and was resistant to treatment with G007-LK in culture (PMID: 28179481). 28179481
APC dec exp colorectal cancer predicted - sensitive G007-LK Preclinical Actionable In a preclinical study, G007-LK treatment altered gene expression pattern and induced growth arrest in intestinal organoids established from mouse models of colorectal cancer driven by APC knockdown, decreased proliferation and promoted differentiation in APC knockdown mouse models (PMID: 31337618). 31337618
APC inact mut colon cancer sensitive G007-LK Preclinical - Cell line xenograft Actionable In a preclinical study, G007-LK inhibited growth of APC-mutant colorectal cancer cell lines in culture and in xenograft models (PMID: 23539443). 23539443

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries


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