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Therapy Name | TPX-0131 |
Synonyms | |
Therapy Description |
TPX-0131 is a small molecule that binds completely within the ATP-binding pocket of Alk, which may lead to inhibition of ALK signaling, proliferation, and tumor growth (PMID: 34158340). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
TPX-0131 | TPX 0131|TPX0131|Zotizalkib | ALK Inhibitor 33 | TPX-0131 is a small molecule that binds completely within the ATP-binding pocket of Alk, which may lead to inhibition of ALK signaling, proliferation, and tumor growth (PMID: 34158340). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
EML4 - ALK ALK G1202R | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, TPX-0131 inhibited Alk autophosphorylation and proliferation of transformed cells expressing ALK G1202R in the context of EML4-ALK in culture and resulted in complete tumor growth inhibition in a mouse cell line xenograft model (PMID: 34158340). | 34158340 |
EML4 - ALK ALK L1196M ALK G1202R | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK L1196M and ALK G1202R compound mutation in the context of EML4-ALK in culture, and resulted in complete tumor growth regression in a cell line xenograft model (PMID: 34158340). | 34158340 |
EML4 - ALK ALK L1198F ALK G1202R | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK L1198F and ALK G1202R compound mutation in the context of EML4-ALK in culture, and resulted in complete tumor growth regression in a cell line xenograft model (PMID: 34158340). | 34158340 |
EML4 - ALK | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK C1156Y ALK G1202R | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK C1156Y and ALK G1202R compound mutation in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK C1156Y ALK G1202R | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 treatment inhibited Alk phosphorylation and viability of transformed cells expressing EML4-ALK with ALK G1202R and C1156Y in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK C1156Y ALK I1171N | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171N and C1156Y were resistant to TPX-0131 in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK C1156Y ALK L1198F | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK C1156Y and ALK L1198F compound mutation in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK C1237Y | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing EML4-ALK and ALK C1237Y were resistant to TPX-0131 in culture (PMID: 38448512). | 38448512 |
EML4 - ALK ALK E1129V ALK G1202R | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 treatment inhibited Alk phosphorylation and viability of transformed cells expressing EML4-ALK with ALK G1202R and E1129V in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK E1129V ALK I1171N | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171N and E1129V were resistant to TPX-0131 in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK F1174C ALK G1202R | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R and F1174C were resistant to TPX-0131 in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK F1174I ALK G1202R | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R and F1174I were resistant to TPX-0131 in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK G1202R | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 treatment inhibited Alk phosphorylation and viability of transformed cells expressing EML4-ALK with ALK G1202R in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK G1202R ALK G1269A | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK G1202R and ALK G1269A compound mutation in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK G1202R ALK L1204V ALK G1269A | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK G1202R, ALK L1204V, and ALK G1269A compound mutation in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK G1269A | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK G1269A in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK G1269S | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK G1269S in the context of EML4-ALK were resistant to TPX-0131 in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK I1171N | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171N were resistant to TPX-0131 in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK I1171N | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK I1171N in the context of EML4-ALK were resistant to TPX-0131 in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK I1171N ALK D1203N | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 did not inhibit viability of cells expressing EML4-ALK, ALK I1171N, and ALK D1203N in culture (PMID: 39269178). | 39269178 |
EML4 - ALK ALK I1171N ALK L1198F | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK I1171N and ALK L1198F compound mutation in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK I1171N ALK L1256F | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171N and L1256F were resistant to TPX-0131 in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK I1171S | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK I1171S in the context of EML4-ALK were resistant to TPX-0131 in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK I1171T | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK I1171T in the context of EML4-ALK were resistant to TPX-0131 in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK L1196M | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK L1196M in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK L1196M ALK G1202R | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 treatment inhibited Alk phosphorylation and viability of transformed cells expressing EML4-ALK with ALK G1202R and L1196M in culture (PMID: 36201110). | 36201110 |
EML4 - ALK ALK L1196M ALK L1198F | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK L1196M and ALK L1198F compound mutation in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK L1196P | Advanced Solid Tumor | resistant | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing EML4-ALK and ALK L1196P were resistant to TPX-0131 in culture (PMID: 38448512). | 38448512 |
EML4 - ALK ALK L1198F | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK L1198F in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
EML4 - ALK ALK L1198F ALK G1202R ALK G1269A | Advanced Solid Tumor | sensitive | TPX-0131 | Preclinical - Cell culture | Actionable | In a preclinical study, TPX-0131 inhibited proliferation of transformed cells expressing ALK L1198F, ALK G1202R, and ALK G1269A compound mutation in the context of EML4-ALK in culture (PMID: 34158340). | 34158340 |
ALK C1156Y | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK C1156Y in an in vitro assay (PMID: 34158340). | 34158340 |
ALK C1156Y ALK L1198F | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK C1156Y and ALK L1198F compound mutation in an in vitro assay (PMID: 34158340). | 34158340 |
ALK D1203N | Advanced Solid Tumor | decreased response | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, ALK D1203N demonstrated reduced sensitivity to TPX-0131 in an in vitro kinase assay (PMID: 34158340). | 34158340 |
ALK D1203N ALK E1210K | Advanced Solid Tumor | decreased response | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, ALK D1203N and E1210K compound mutation demonstrated reduced sensitivity to TPX-0131 in an in vitro kinase assay (PMID: 34158340). | 34158340 |
ALK E1210K | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK E1210K in an in vitro assay (PMID: 34158340). | 34158340 |
ALK F1174C | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK F1174C in an in vitro assay (PMID: 34158340). | 34158340 |
ALK F1174L | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK F1174L in an in vitro assay (PMID: 34158340). | 34158340 |
ALK F1174S | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK F1174S in an in vitro assay (PMID: 34158340). | 34158340 |
ALK F1245C | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK F1245C in an in vitro assay (PMID: 34158340). | 34158340 |
ALK G1202del | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK G1202del in an in vitro assay (PMID: 34158340). | 34158340 |
ALK G1269A | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK G1269A in an in vitro assay (PMID: 34158340). | 34158340 |
ALK G1269S | Advanced Solid Tumor | decreased response | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, ALK G1269S demonstrated reduced sensitivity to TPX-0131 in an in vitro kinase assay (PMID: 34158340). | 34158340 |
ALK I1171N | Advanced Solid Tumor | decreased response | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, ALK I1171N demonstrated reduced sensitivity to TPX-0131 in an in vitro kinase assay (PMID: 34158340). | 34158340 |
ALK L1152P | Advanced Solid Tumor | decreased response | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, ALK L1152P demonstrated reduced sensitivity to TPX-0131 in an in vitro kinase assay (PMID: 34158340). | 34158340 |
ALK L1152R | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK L1152R in an in vitro assay (PMID: 34158340). | 34158340 |
ALK L1196M | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK L1196M in an in vitro assay (PMID: 34158340). | 34158340 |
ALK L1196M ALK L1198F | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK L1196M and ALK L1198F compound mutation in an in vitro assay (PMID: 34158340). | 34158340 |
ALK L1198F | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK L1198F in an in vitro assay (PMID: 34158340). | 34158340 |
ALK L1198F ALK G1202R | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK G1202R and L1198F compound mutation in an in vitro assay (PMID: 34158340). | 34158340 |
ALK R1275Q | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK R1275Q in an in vitro assay (PMID: 34158340). | 34158340 |
ALK S1206C ALK E1210K | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK S1206C and ALK E1210K compound mutation in an in vitro assay (PMID: 34158340). | 34158340 |
ALK S1206R | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK S1206R in an in vitro assay (PMID: 34158340). | 34158340 |
ALK T1151dup | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK T1151dup in an in vitro assay (PMID: 34158340). | 34158340 |
ALK T1151M | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK T1151M in an in vitro assay (PMID: 34158340). | 34158340 |
ALK V1180L | Advanced Solid Tumor | predicted - sensitive | TPX-0131 | Preclinical - Biochemical | Actionable | In a preclinical study, TPX-0131 inhibited kinase activity of ALK V1180L in an in vitro assay (PMID: 34158340). | 34158340 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT04849273 | Phase Ib/II | TPX-0131 | A Study of TPX-0131, a Novel Oral ALK Tyrosine Kinase Inhibitor, in Patients With ALK+ Advanced or Metastatic NSCLC | Terminated | USA | AUS | 1 |
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