Therapy Detail
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| Therapy Name | AZD1480 |
| Synonyms | |
| Therapy Description |
AZD1480 is an ATP-competitive inhibitor of JAK1 and JAK2, which reduces STAT3 activation, potentially resulting in decreased tumor growth (PMID: 22027691, PMID: 24158701) and has been also shown to inhibit ALK, LTK, FGFR1-3, RET and TRKA-C kinases (PMID: 29312610). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| AZD1480 | AZD-1480 | JAK1 Inhibitor - ATP competitive 5 JAK2 Inhibitor - ATP competitive 15 | AZD1480 is an ATP-competitive inhibitor of JAK1 and JAK2, which reduces STAT3 activation, potentially resulting in decreased tumor growth (PMID: 22027691, PMID: 24158701) and has been also shown to inhibit ALK, LTK, FGFR1-3, RET and TRKA-C kinases (PMID: 29312610). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| RET M918T | medullary thyroid carcinoma | sensitive | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD1480 reduced phosphorylation of RET and downstream effectors, and inhibited growth and increased apoptosis of a medullary thyroid cancer cell line harboring RET M918T in culture (PMID: 23056499). | 23056499 |
| RET C634W | thyroid cancer | sensitive | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, AZD1480 reduced phosphorylation of RET and downstream effectors, and inhibited growth and increased apoptosis of a thyroid cancer cell line harboring RET C634W in culture (PMID: 23056499). | 23056499 |
| JAK2 V617F JAK2 Y931C | hematologic cancer | resistant | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 Y931C double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 I960V | hematologic cancer | resistant | AZD1480 | Preclinical | Actionable | In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 I960V double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 R938L | hematologic cancer | resistant | AZD1480 | Preclinical | Actionable | In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 R938L double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 G935R | hematologic cancer | resistant | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 G935R double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). | 21926964 |
| CSF3R T618I CSF3R Q741* | hematologic cancer | predicted - resistant | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells co-expressing CSF3R T618I and CSF3R Q741* were resistant to treatment with AZD1480 in culture (PMID: 28031554). | 28031554 |
| CSF3R T618I CSF3R W791* | hematologic cancer | predicted - resistant | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells co-expressing CSF3R T618I and CSF3R W791* were resistant to treatment with AZD1480 in culture (PMID: 28031554). | 28031554 |
| JAK2 V617F JAK2 M929I | hematologic cancer | predicted - sensitive | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 M929I double mutation were sensitive to treatment with AZD1480 in culture, demonstrating growth inhibition (PMID: 21926964). | 21926964 |
| CSF3R W791* | hematologic cancer | predicted - sensitive | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing CSF3R W791* were sensitive to treatment with AZD1480 in culture, demonstrating decreased cell survival (PMID: 28031554). | 28031554 |
| CSF3R Q741* | hematologic cancer | predicted - sensitive | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing CSF3R Q741* were sensitive to treatment with AZD1480 in culture, demonstrating decreased cell survival (PMID: 28031554). | 28031554 |
| JAK2 V617F JAK2 E985K | hematologic cancer | resistant | AZD1480 | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 E985K double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). | 21926964 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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