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). |
Filtering
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- Use simple literal full or partial string matches
- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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 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 E582fs | colorectal cancer | predicted - resistant | G007-LK | Preclinical | Actionable | In a preclinical study, G007-LK treatment did not inhibited growth of mouse intestinal organoids expressing APC E580fs (corresponding to E582fs in human) in culture (PMID: 31337618). | 31337618 |
| 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 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 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 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 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 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 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 |
| 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 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 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 Q886* | 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 APC Q884* (corresponding to Q886* in human) in culture (PMID: 31337618). | 31337618 |
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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- Click on any column header arrows to sort by that column
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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